Query Query
Results
Date
6 substances in Reaxys
2018-06-23 10h:55m:17s (UTC)
H 2N
1. Query
Search as: As drawn ) AND (IDE.XRN=970319) OR (IDE.XRN=3912379) OR (IDE.XRN=4623759) OR (IDE.XRN=18581811) OR (IDE.XRN=18665544) OR (IDE.XRN=18692515))
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Reaxys ID 970319 View in Reaxys
1/6 CAS Registry Number: 122-09-8 Chemical Name: Phentermin; Phentermine Linear Structure Formula: C10H15N Molecular Formula: C10H15N Molecular Weight: 149.236 Type of Substance: isocyclic InChI Key: DHHVAGZRUROJKS-UHFFFAOYSA-N Note:
H 2N
Substance Label (18) Label References 4a
Mancinelli, Andrea; Alamillo, Carla; Albert, Joan; Ariza, Xavier; Etxabe, Haizea; Farràs, Jaume; Garcia, Jordi; Granell, Jaume; Quijada, F. Javier; Organometallics; vol. 36; nb. 4; (2017); p. 911 - 919, View in Reaxys
7
Angeli, Andrea; Vaiano, Fabio; Mari, Francesco; Bertol, Elisabetta; Supuran, Claudiu T.; Journal of Enzyme Inhibition and Medicinal Chemistry; vol. 32; nb. 1; (2017); p. 1253 - 1259, View in Reaxys
1e
Patent; HELSINN HEALTHCARE SA; Giuliano, Claudio; Daina, Antoine; Pietra, Claudio; (254 pag.); US2017/275301; (2017); (A1) English, View in Reaxys
D
Yuan, Ming; Chen, Li; Wang, Junwei; Chen, Shenjie; Wang, Kongchao; Xue, Yongbo; Yao, Guangmin; Luo, Zengwei; Zhang, Yonghui; Organic Letters; vol. 17; nb. 2; (2015); p. 346 - 349, View in Reaxys
Formula 1
Patent; Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui; EP2829266; (2015); (A1) English, View in Reaxys; Patent; Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; Gao, Chunseng; Zhong, Wu; Wang, Yuli; Yang, Meiyan; Shan, Li; Zhou, Xinbo; Zheng, Zhibing; Wang, Xiaokui; US2015/44295; (2015); (A1) English, View in Reaxys
1d
Tanaka; Yamamura; Nakane; Kitamura; Chemical Communications; vol. 51; nb. 66; (2015); p. 13110 - 13112, View in Reaxys
2d
Tanaka, Shinji; Saburi, Hajime; Murase, Takanori; Yoshimura, Masahiro; Kitamura, Masato; Journal of Organic Chemistry; vol. 71; nb. 12; (2006); p. 4682 - 4684, View in Reaxys; Rodrguez, Aleix; Albert, Joan; Ariza, Xavier; Garcia, Jordi; Granell, Jaume; Farrs, Jaume; La Mela, Andrea; Nicols, Ernesto; Journal of Organic Chemistry; vol. 79; nb. 20; (2014); p. 9578 - 9585, View in Reaxys
3k
Albert, Joan; Ariza, Xavier; Calvet, Teresa; Font-Bardia, Merce; Garcia, Jordi; Granell, Jaume; Lamela, Andrea; Lopez, Blanca; Martinez, Manuel; Ortega, Laura; Rodriguez, Aleix; Santos, David; Organometallics; vol. 32; nb. 2; (2013); p. 649 - 659, View in Reaxys
15
Huang, Xianhai; Palani, Anandan; Xiao, Dong; Aslanian, Robert; Shih, Neng-Yang; Organic Letters; vol. 6; nb. 25; (2004); p. 4795 - 4798, View in Reaxys; Ito, Nobuhiro; Watahiki, Tsutomu; Maesawa, Tsuneaki; Maegawa, Tomohiro; Sajiki, Hironao; Synthesis; nb. 9; (2008); p. 1467 - 1478; Art.No: F03608SS, View in Reaxys
49
Lewin, Anita H.; Navarro, Hernan A.; Wayne Mascarella; Bioorganic and Medicinal Chemistry; vol. 16; nb. 15; (2008); p. 7415 - 7423, View in Reaxys
12
Lee, Peter J.; Chen, Weibin; Gebler, John C.; Analytical Chemistry; vol. 76; nb. 16; (2004); p. 4888 - 4893, View in Reaxys
phen
Tao, Rui; Fray, Anne; Aspley, Sue; Brammer, Richard; Heal, David; Auerbach, Sidney; European Journal of Pharmacology; vol. 445; nb. 1-2; (2002); p. 69 - 81, View in Reaxys
9b
Gai; Grigg; Collard; Muir; Chemical Communications; nb. 18; (2001); p. 1712 - 1713, View in Reaxys
3d (free base)
Jirgensons; Kauss; Kalvinsh; Gold; Synthesis; nb. 12; (2000); p. 1709 - 1712, View in Reaxys
8
Adams, Mortimer H.; Ameer, Farouk; Green, Ivan R.; Syce, James A.; Synthetic Communications; vol. 29; nb. 14; (1999); p. 2419 - 2430, View in Reaxys
Merck 7415
Wojnicki, Francis H. E.; Rothman, Richard B.; Rice, Kenner C.; Glowa, John R.; Journal of Pharmacology and Experimental Therapeutics; vol. 288; nb. 2; (1999); p. 550 - 560, View in Reaxys
amine a
Deyrup; Nowicki; Richards; Otero; Harrison; Baker; Naunyn-Schmiedeberg's Archives of Pharmacology; vol. 359; nb. 3; (1999); p. 168 - 177, View in Reaxys
PTM
Nakahara, Yuji; Kikura, Ruri; Archives of Toxicology; vol. 70; nb. 12; (1996); p. 841 - 849, View in Reaxys
Patent-Specific Data (5) Prophetic ComReferences pound
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Patent; Pathway Therapeutics Inc.; US2012/252802; (2012); (A1) English, View in Reaxys Patent; SUN PHARMA ADVANCED RESEARCH COMPANY LTD; WO2008/111096; (2008); (A2) English, View in Reaxys Patent; Caron, Marc G.; Sotnikova, Tatyana D.; Gainetdinov, Raul R.; US2007/27208; (2007); (A1) English, View in Reaxys Patent; AstraZeneca AB; US6369064; (2002); (B1) English, View in Reaxys prophetic product
Patent; University of Florida; US4771059; (1988); (A) English, View in Reaxys
Druglikeness (1) 1 of 1
LogP
2.179
H Bond Donors
1
H Bond Acceptors
1
Rotatable Bonds
2
TPSA
26.02
Lipinski Number
4
Veber Number
2
Derivative (7) Comment (Derivative)
Derivative
References
phentermine hydro- Jirgensons; Kauss; Kalvinsh; Gold; Synthesis; nb. 12; (2000); p. 1709 - 1712, View in Reaxys chloride Hydrochlorid: F: 200grad; IR, NMR
Marquardt; Edwards; The Journal of organic chemistry; vol. 37; nb. 11; (1972); p. 1861 - 1863, View in Reaxys
Hydrochlorid: IR
Mesley; Evans; Journal of Pharmacy and Pharmacology; vol. 22; (1970); p. 321,325-329, View in Reaxys
Hydrochlorid C10H15N*HCl. Duennschichtchromatogra. Verh. u. Nachweisreaktionen
Palitzsch et al.; Pharmazie; vol. 23; (1968); p. 246,248, View in Reaxys
Hydrochlorid = Wilpo
New Drugs; American Journal of Pharmacy and the Sciences Supporting Public Health (1937-1978); vol. 134; (1962); p. 6,21, View in Reaxys
Hydrochlorid. F:200-201grad(Tho mas-Hoover-Apparat; unkorr.)
Shetty; Journal of Organic Chemistry; vol. 26; (1961); p. 3002, View in Reaxys
Pikrat. F:109-110grad(Tho mas-Hoover-Apparat;unkorr.)
Shetty; Journal of Organic Chemistry; vol. 26; (1961); p. 3002, View in Reaxys
Boiling Point (7) Boiling Point [°C]
Pressure (Boiling Point) [Torr]
References
68
7.5
Wannagat, U.; Damrath, V.; Harder, U.; Monatshefte fuer Chemie; vol. 125; nb. 11; (1994); p. 1159 - 1170, View in Reaxys
110
20
Christol et al.; Bulletin de la Societe Chimique de France; (1961); p. 2317, View in Reaxys
106.5 - 107
31
Girault-Vexlearschi; Bulletin de la Societe Chimique de France; (1956); p. 589,596, View in Reaxys
86 - 88
13
Moed et al.; Recueil des Travaux Chimiques des Pays-Bas; vol. 74; (1955); p. 919,922, View in Reaxys
94
15
Kornblum; Iffland; Journal of the American Chemical Society; vol. 71; (1949); p. 2137,2138,2140, View in Reaxys
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89 - 90
10
Zenitz; Macks; Moore; Journal of the American Chemical Society; vol. 70; (1948); p. 955, View in Reaxys
203 - 205
760
Mentzer; Comptes Rendus Hebdomadaires des Seances de l'Academie des Sciences; vol. 213>1941>581; p. 583, View in Reaxys
Refractive Index (3) Refractive Index Wavelength (ReTemperature (Refractive Index) [nm] fractive Index) [°C]
References
1.5125
589
20
Wannagat, U.; Damrath, V.; Harder, U.; Monatshefte fuer Chemie; vol. 125; nb. 11; (1994); p. 1159 - 1170, View in Reaxys
1.5132
589
20
Kornblum; Iffland; Journal of the American Chemical Society; vol. 71; (1949); p. 2137,2138,2140, View in Reaxys
1.513
589
20
Zenitz; Macks; Moore; Journal of the American Chemical Society; vol. 70; (1948); p. 955, View in Reaxys
Chromatographic Data (3) Chromatographic References data HPLC (High performance liquid chromatography)
Paíga, Paula; Rodrigues, Manuela J.E.; Correia, Manuela; Amaral, Joana S.; Oliveira, M. Beatriz P.P.; DelerueMatos, Cristina; European Journal of Pharmaceutical Sciences; vol. 99; (2017); p. 219 - 227, View in Reaxys
LC (Liquid chromatography)
Jeong, Eun Sook; Kim, So-Hee; Cha, Eun-Ju; Lee, Kang Mi; Kim, Ho Jun; Lee, Sang-Won; Kwon, Oh-Seung; Lee, Jaeick; Rapid Communications in Mass Spectrometry; vol. 29; nb. 4; (2015); p. 367 - 384, View in Reaxys; Jeong, Eun Sook; Kim, So-Hee; Cha, Eun-Ju; Lee, Kang Mi; Kim, Ho Jun; Lee, Sang-Won; Kwon, Oh-Seung; Lee, Jaeick; Rapid Communications in Mass Spectrometry; vol. 29; nb. 4; (2015); p. 367 - 384, View in Reaxys
UPLC (Ultra performance liquid chromatography)
Lin, Huei-Ru; Liao, Chao-Chuan; Lin, Tzu-Chieh; Rapid Communications in Mass Spectrometry; vol. 28; nb. 19; (2014); p. 2043 - 2053, View in Reaxys
Crystal Property Description (2) Colour & Other Location Properties colourless
yellow
References Mancinelli, Andrea; Alamillo, Carla; Albert, Joan; Ariza, Xavier; Etxabe, Haizea; Farràs, Jaume; Garcia, Jordi; Granell, Jaume; Quijada, F. Javier; Organometallics; vol. 36; nb. 4; (2017); p. 911 - 919, View in Reaxys
supporting informa- Albert, Joan; Ariza, Xavier; Calvet, Teresa; Font-Bardia, Merce; Garcia, Jordi; Granell, tion Jaume; Lamela, Andrea; Lopez, Blanca; Martinez, Manuel; Ortega, Laura; Rodriguez, Aleix; Santos, David; Organometallics; vol. 32; nb. 2; (2013); p. 649 - 659, View in Reaxys
Dissociation Exponent (2) 1 of 2
Dissociation Exponent (pK)
9.33 - 10.12
Temperature (Dissociation Exponent) [°C]
26
Solvent (Dissociation Exponent)
methanol; H2O
Type (Dissociation Exponent)
a1/apparent
Comment (Dissociation Exponent)
Ratio of solvents: 10 to 80 percent v/v MeOH
Canals; Valko; Bosch; Hill; Roses; Analytical Chemistry; vol. 73; nb. 20; (2001); p. 4937 - 4945, View in Reaxys 2 of 2
Dissociation Exponent (pK)
10.13
Temperature (Dissociation Exponent) [°C]
20
Solvent (Dissociation Exponent)
H2O
Method (Dissociation Exponent)
potentiometric
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Type (Dissociation Exponent)
a/thermodynamic
Girault-Vexlearschi; Bulletin de la Societe Chimique de France; (1956); p. 589,596, View in Reaxys Enthalpies of Other Phase Transitions (1) Comment (Enthal- References pies of Other Phase Transitions) Enthalpies of other phase transition(s) given
Gobble, Chase; Rath, Nigam; Chickos, James; Journal of Chemical and Engineering Data; vol. 58; nb. 9; (2013); p. 2600 - 2609, View in Reaxys
Further Information (5) Description (FurReferences ther Information) Further information Cartoni et al.; Bollettino Chimico Farmaceutico; vol. 115; (1976); p. 347,350, View in Reaxys Further information Reisch; Alfes; Moellmann; Die Pharmazie; vol. 23; nb. 5; (1968); p. 245 - 246, View in Reaxys Further information Palitzsch et al.; Pharmazie; vol. 23; (1968); p. 246,248, View in Reaxys Further information New Drugs; American Journal of Pharmacy and the Sciences Supporting Public Health (1937-1978); vol. 134; (1962); p. 6,21, View in Reaxys Further information Shetty; Journal of Organic Chemistry; vol. 26; (1961); p. 3002, View in Reaxys Liquid/Liquid Systems (MCS) (1) 1 of 1
Description (Liquid/Liquid Distribution between solvent 1 + 2 Systems (MCS)) Mihailova; Testa; European Journal of Medicinal Chemistry; vol. 13; nb. 1; (1978); p. 49 - 52, View in Reaxys
Partition octan-1-ol/water (MCS) (2) 1 of 2
log POW
-0.55
pH
7.4
Location
supporting information
Comment (Partition octan-1-ol/water (MCS))
aq.buffer
Rankovic, Zoran; Journal of Medicinal Chemistry; vol. 60; nb. 14; (2017); p. 5943 - 5954, View in Reaxys 2 of 2
log POW
2.09
Location
supporting information
Rankovic, Zoran; Journal of Medicinal Chemistry; vol. 60; nb. 14; (2017); p. 5943 - 5954, View in Reaxys NMR Spectroscopy (9) 1 of 9
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectroscopy)
chloroform-d1
Frequency (NMR Spectro- 400 scopy) [MHz] Mancinelli, Andrea; Alamillo, Carla; Albert, Joan; Ariza, Xavier; Etxabe, Haizea; Farràs, Jaume; Garcia, Jordi; Granell, Jaume; Quijada, F. Javier; Organometallics; vol. 36; nb. 4; (2017); p. 911 - 919, View in Reaxys 2 of 9
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
13C
Solvents (NMR Spectroscopy)
chloroform-d1
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Frequency (NMR Spectro- 101 scopy) [MHz] Mancinelli, Andrea; Alamillo, Carla; Albert, Joan; Ariza, Xavier; Etxabe, Haizea; Farràs, Jaume; Garcia, Jordi; Granell, Jaume; Quijada, F. Javier; Organometallics; vol. 36; nb. 4; (2017); p. 911 - 919, View in Reaxys 3 of 9
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectroscopy)
chloroform-d1
Frequency (NMR Spectro- 400 scopy) [MHz] Location
supporting information
Albert, Joan; Ariza, Xavier; Calvet, Teresa; Font-Bardia, Merce; Garcia, Jordi; Granell, Jaume; Lamela, Andrea; Lopez, Blanca; Martinez, Manuel; Ortega, Laura; Rodriguez, Aleix; Santos, David; Organometallics; vol. 32; nb. 2; (2013); p. 649 - 659, View in Reaxys 4 of 9
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
13C
Solvents (NMR Spectroscopy)
chloroform-d1
Frequency (NMR Spectro- 101 scopy) [MHz] Location
supporting information
Albert, Joan; Ariza, Xavier; Calvet, Teresa; Font-Bardia, Merce; Garcia, Jordi; Granell, Jaume; Lamela, Andrea; Lopez, Blanca; Martinez, Manuel; Ortega, Laura; Rodriguez, Aleix; Santos, David; Organometallics; vol. 32; nb. 2; (2013); p. 649 - 659, View in Reaxys 5 of 9
Description (NMR Spectroscopy)
Chemical shifts; Spectrum
Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectroscopy)
chloroform-d1
Temperature (NMR Spectroscopy) [°C]
24.94
Frequency (NMR Spectro- 400 scopy) [MHz] Location
supporting information
Gildner, Peter G.; Gietter, Amber A. S.; Cui, Di; Watson, Donald A.; Journal of the American Chemical Society; vol. 134; nb. 24; (2012); p. 9942 - 9945, View in Reaxys 6 of 9
Description (NMR Spectroscopy)
Chemical shifts; Spectrum
Nucleus (NMR Spectroscopy)
13C
Solvents (NMR Spectroscopy)
chloroform-d1
Temperature (NMR Spectroscopy) [°C]
24.94
Frequency (NMR Spectro- 101 scopy) [MHz] Location
supporting information
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Gildner, Peter G.; Gietter, Amber A. S.; Cui, Di; Watson, Donald A.; Journal of the American Chemical Society; vol. 134; nb. 24; (2012); p. 9942 - 9945, View in Reaxys 7 of 9
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectroscopy)
CDCl3
Frequency (NMR Spectro- 600 scopy) [MHz] Tanaka, Shinji; Saburi, Hajime; Murase, Takanori; Yoshimura, Masahiro; Kitamura, Masato; Journal of Organic Chemistry; vol. 71; nb. 12; (2006); p. 4682 - 4684, View in Reaxys 8 of 9
Description (NMR Spectroscopy)
Spectrum
Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectroscopy)
CDCl3
Frequency (NMR Spectro- 600 scopy) [MHz] Tanaka, Shinji; Saburi, Hajime; Murase, Takanori; Yoshimura, Masahiro; Kitamura, Masato; Journal of Organic Chemistry; vol. 71; nb. 12; (2006); p. 4682 - 4684, View in Reaxys 9 of 9
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectroscopy)
CCl4
Wannagat, U.; Damrath, V.; Harder, U.; Monatshefte fuer Chemie; vol. 125; nb. 11; (1994); p. 1159 - 1170, View in Reaxys IR Spectroscopy (3) 1 of 3
Description (IR Spectroscopy)
ATR (attenuated total reflectance); Bands
Solvent (IR Spectroscopy)
neat (no solvent, solid phase)
Location
supporting information
Albert, Joan; Ariza, Xavier; Calvet, Teresa; Font-Bardia, Merce; Garcia, Jordi; Granell, Jaume; Lamela, Andrea; Lopez, Blanca; Martinez, Manuel; Ortega, Laura; Rodriguez, Aleix; Santos, David; Organometallics; vol. 32; nb. 2; (2013); p. 649 - 659, View in Reaxys 2 of 3
Description (IR Spectroscopy)
Bands
Location
supporting information
Comment (IR Spectroscopy)
film
Gildner, Peter G.; Gietter, Amber A. S.; Cui, Di; Watson, Donald A.; Journal of the American Chemical Society; vol. 134; nb. 24; (2012); p. 9942 - 9945, View in Reaxys 3 of 3
Description (IR Spectroscopy)
IR
Mesley; Evans; Journal of Pharmacy and Pharmacology; vol. 22; (1970); p. 321,325-329, View in Reaxys Mass Spectrometry (11) Description (Mass Location Spectrometry)
Comment (Mass Spectrometry)
electrospray ionisation (ESI); spectrum
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
References Jeong, Eun Sook; Kim, So-Hee; Cha, Eun-Ju; Lee, Kang Mi; Kim, Ho Jun; Lee, Sang-Won; Kwon, Oh-Seung; Lee, Jaeick; Rapid Communications in Mass Spectrometry; vol. 29; nb. 4; (2015); p. 367 - 384,
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View in Reaxys; Paíga, Paula; Rodrigues, Manuela J.E.; Correia, Manuela; Amaral, Joana S.; Oliveira, M. Beatriz P.P.; Delerue-Matos, Cristina; European Journal of Pharmaceutical Sciences; vol. 99; (2017); p. 219 227, View in Reaxys high resolution mass spectrometry (HRMS); electrospray ionisation (ESI); time-offlight mass spectra (TOFMS); spectrum
Mancinelli, Andrea; Alamillo, Carla; Albert, Joan; Ariza, Xavier; Etxabe, Haizea; Farràs, Jaume; Garcia, Jordi; Granell, Jaume; Quijada, F. Javier; Organometallics; vol. 36; nb. 4; (2017); p. 911 - 919, View in Reaxys
liquid chromatography mass spectrometry (LCMS); electrospray ionisation (ESI); spectrum
Jeong, Eun Sook; Kim, So-Hee; Cha, Eun-Ju; Lee, Kang Mi; Kim, Ho Jun; Lee, Sang-Won; Kwon, Oh-Seung; Lee, Jaeick; Rapid Communications in Mass Spectrometry; vol. 29; nb. 4; (2015); p. 367 - 384, View in Reaxys
liquid chromatography mass spectrometry (LCMS); CID (collision-induced dissociation); spectrum
Lin, Huei-Ru; Liao, Chao-Chuan; Lin, Tzu-Chieh; Rapid Communications in Mass Spectrometry; vol. 28; nb. 19; (2014); p. 2043 - 2053, View in Reaxys
electrospray ionisa- supporting information (ESI); high res- tion olution mass spectrometry (HRMS); spectrum
Albert, Joan; Ariza, Xavier; Calvet, Teresa; Font-Bardia, Merce; Garcia, Jordi; Granell, Jaume; Lamela, Andrea; Lopez, Blanca; Martinez, Manuel; Ortega, Laura; Rodriguez, Aleix; Santos, David; Organometallics; vol. 32; nb. 2; (2013); p. 649 - 659, View in Reaxys
IT (ion trap); CID (collision-induced dissociation); Spectrum
Oberacher, Herbert; Pitterl, Florian; Siapi, Eleni; Steele, Barry R.; Letzel, Thomas; Grosse, Sylvia; Poschner, Bernhard; Tagliaro, Franco; Gottardo, Rossella; Chacko, Silvi A.; Josephs, Jonathan L.; Journal of Mass Spectrometry; vol. 47; nb. 2; (2012); p. 263 - 270, View in Reaxys
HRMS (High resolution mass spectrometry); Spectrum
supporting information
Gildner, Peter G.; Gietter, Amber A. S.; Cui, Di; Watson, Donald A.; Journal of the American Chemical Society; vol. 134; nb. 24; (2012); p. 9942 - 9945, View in Reaxys
ESI (Electrospray ionisation); Spectrum
supporting information
Gildner, Peter G.; Gietter, Amber A. S.; Cui, Di; Watson, Donald A.; Journal of the American Chemical Society; vol. 134; nb. 24; (2012); p. 9942 - 9945, View in Reaxys
HRMS (High resolution mass spectrometry); TOFMS (Time of flight mass spectrum); ESI (Electrospray ionisation); LCMS (Liquid chromatography mass spectrometry); Spectrum
Vonaparti; Lyris; Angelis; Panderi; Koupparis; Tsantili-Kakoulidou; Peters; Nielen; Georgakopoulos; Rapid Communications in Mass Spectrometry; vol. 24; nb. 11; (2010); p. 1595 - 1609, View in Reaxys
LCMS (Liquid chromatography mass spectrometry); ESI (Electrospray ionisation); Tandem mass spectrometry; Spectrum
mol peak
Thoerngren, John-Olof; Oestervall, Fredrik; Garle, Mats; Journal of Mass Spectrometry; vol. 43; nb. 7; (2008); p. 980 - 992, View in Reaxys
Reisch et al.; Journal of Pharmacy and Pharmacology; vol. 20; (1968); p. 81,85, View in Reaxys; Cartoni et al.; Bollettino Chimico Farmaceutico; vol. 115; (1976); p. 347,350, View in Reaxys Use (379) Use Pattern
Location
References
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Pharmaceuticals
Page/Page column 22
Patent; Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui; EP2829266; (2015); (A1) English, View in Reaxys
lowering blood pressure
Page/Page column 22
Patent; Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui; EP2829266; (2015); (A1) English, View in Reaxys
manufacture of a Page/Page column medicament for re- 22 ducing body weight
Patent; Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui; EP2829266; (2015); (A1) English, View in Reaxys
manufacture of a medicament for treatment of coronary heart disease
Page/Page column 22
Patent; Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui; EP2829266; (2015); (A1) English, View in Reaxys
manufacture of a medicament for treatment of diabetes
Page/Page column 22
Patent; Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui; EP2829266; (2015); (A1) English, View in Reaxys
manufacture of a medicament for treatment of hyperlipidemia
Page/Page column 22
Patent; Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui; EP2829266; (2015); (A1) English, View in Reaxys
manufacture of a medicament for treatment of hypertension
Page/Page column 22
Patent; Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui; EP2829266; (2015); (A1) English, View in Reaxys
realizing antihypertension
Page/Page column 22
Patent; Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui; EP2829266; (2015); (A1) English, View in Reaxys
realizing blood fat reduction
Page/Page column 22
Patent; Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui; EP2829266; (2015); (A1) English, View in Reaxys
realizing weight loss
Page/Page column 22
Patent; Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui; EP2829266; (2015); (A1) English, View in Reaxys
reducing blood fat
Page/Page column 22
Patent; Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui; EP2829266; (2015); (A1) English, View in Reaxys
treatment of mental or nervous diseases
Page/Page column 22
Patent; Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui; EP2829266; (2015); (A1) English, View in Reaxys
Anti-obesity agent
Page/Page column 55
Patent; AUSPEX PHARMACEUTICAL, INC.; GANT, Thomas, G.; SHAHBAZ, Manoucherhr; WO2010/48358; (2010); (A2) English, View in Reaxys
Appetite-regulating agent
Page/Page column 55
Patent; AUSPEX PHARMACEUTICAL, INC.; GANT, Thomas, G.; SHAHBAZ, Manoucherhr; WO2010/48358; (2010); (A2) English, View in Reaxys
Obesity
Page/Page column 55
Patent; AUSPEX PHARMACEUTICAL, INC.; GANT, Thomas, G.; SHAHBAZ, Manoucherhr; WO2010/48358; (2010); (A2) English, View in Reaxys
dopamine reuptake inhibitor
Patent; OREXIGEN THERAPEUTICS, INC.; WO2006/17504; (2006); (A1) English, View in Reaxys; Patent; Orexigen Therapeutics, Inc; US2008/113026; (2008); (A1) English, View in Reaxys
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2018-06-23 10:56:32
Weight loss
Patent; OREXIGEN THERAPEUTICS, INC.; WO2007/16108; (2007); (A1) English, View in Reaxys; Patent; Orexigen Therapeutics, Inc; US2008/113026; (2008); (A1) English, View in Reaxys
Suppressing appetite
Patent; Orexigen Therapeutics, Inc; US2008/113026; (2008); (A1) English, View in Reaxys
Obesity-related conditions
Patent; Orexigen Therapeutics, Inc; US2008/113026; (2008); (A1) English, View in Reaxys
in combination with dapagliflozin or its propylene glycol hydrate
Patent; Bristol-Myers Squibb; US2008/234366; (2008); (A1) English, View in Reaxys
antiobesity agent
Patent; PHARMACOPEIA DRUG DISCOVERY, INC.; WO2006/44293; (2006); (A2) English, View in Reaxys; Patent; Avestha Gengraine Technologies Pvt. Ltd.; US2008/20971; (2008); (A1) English, View in Reaxys; Patent; Bristol-Myers Squibb; US2008/234366; (2008); (A1) English, View in Reaxys
in combination with SGLT2 inhibitor
Patent; BRISTOL-MYERS SQUIBB; US2008/234367; (2008); (A1) English, View in Reaxys
obesity
Patent; OREXIGEN THERAPEUTICS, INC.; WO2006/17504; (2006); (A1) English, View in Reaxys; Patent; GELESIS, INC.; WO2007/112436; (2007); (A2) English, View in Reaxys; Patent; BRISTOL-MYERS SQUIBB; US2008/234367; (2008); (A1) English, View in Reaxys
anti-obesity agent
Patent; BRISTOL-MYERS SQUIBB; US2008/234367; (2008); (A1) English, View in Reaxys
anorectic agent
Patent; PHARMACOPEIA DRUG DISCOVERY, INC.; WO2006/44293; (2006); (A2) English, View in Reaxys; Patent; Bristol-Myers Squibb; US2008/234366; (2008); (A1) English, View in Reaxys; Patent; BRISTOL-MYERS SQUIBB; US2008/234367; (2008); (A1) English, View in Reaxys
Weight control
Patent; ALPEX PHARMA S.A.; US2008/206327; (2008); (A1) English, View in Reaxys
epilepsy
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys; Patent; Tam, Peter Y.; Wilson, Leland F.; US2008/103179; (2008); (A1) English, View in Reaxys
diabetes
Patent; Tam, Peter Y.; Wilson, Leland F.; US2008/103179; (2008); (A1) English, View in Reaxys
hypertension
Patent; Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; Koehler-Stec, Ellen-Marie; US2006/58224; (2006); (A1) English, View in Reaxys; Patent; Tam, Peter Y.; Wilson, Leland F.; US2008/103179; (2008); (A1) English, View in Reaxys
pulmonary hypertension
Patent; Tam, Peter Y.; Wilson, Leland F.; US2008/103179; (2008); (A1) English, View in Reaxys
migraine
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys; Patent; Tam, Peter Y.; Wilson, Leland F.; US2008/103179; (2008); (A1) English, View in Reaxys
sleep apnea
Patent; Tam, Peter Y.; Wilson, Leland F.; US2008/103179; (2008); (A1) English, View in Reaxys
depression
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys; Patent; Tam, Peter Y.; Wilson, Leland F.; US2008/103179; (2008); (A1) English, View in Reaxys
impulse control disorders
Patent; Tam, Peter Y.; Wilson, Leland F.; US2008/103179; (2008); (A1) English, View in Reaxys
alcohol addiction
Patent; Tam, Peter Y.; Wilson, Leland F.; US2008/103179; (2008); (A1) English, View in Reaxys
sympathomimetic agent
Patent; Tam, Peter Y.; Wilson, Leland F.; US2008/103179; (2008); (A1) English, View in Reaxys
second agent of the composition with antiepileptic agent
Patent; Tam, Peter Y.; Wilson, Leland F.; US2008/103179; (2008); (A1) English, View in Reaxys
second agent of the composition with
Patent; Tam, Peter Y.; Wilson, Leland F.; US2008/103179; (2008); (A1) English, View in Reaxys
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10/98
2018-06-23 10:56:32
anticonvulsant sulfamate or sulfonylurea compound Antiobesity
Patent; Sattigeri, Jitendra A.; Andappan, Murugaiah M.S.; Kishore, Kaushal; Sethi, Sachin; Kandalkar, Sachin Ramesh; Pal, Chanchal Kumar; Mahajan, Dipak C.; Ahmed, Shahadat; Parkale, Santhosh Sadashiv; Srinivasan, T.; Sharma, Lalima; Bansal, Vinay S.; Chugh, Anita; Davis, Joseph Alexanand; US2008/300251; (2008); (A1) English, View in Reaxys
Anti-obesity agent
Patent; Bhanot, Sanjay; Dobie, Kenneth W.; US2005/261233; (2005); (A1) English, View in Reaxys; Patent; IRM LLC; WO2005/113506; (2005); (A1) English, View in Reaxys; Patent; JOHN I. HASS, INC.; WO2006/55985; (2006); (A1) English, View in Reaxys; Patent; BRISTOL-MYERS SQUIBB COMPANY; WO2006/71752; (2006); (A1) English, View in Reaxys; Patent; PROTEMIX CORPORATION LIMITED; WO2006/104397; (2006); (A1) English, View in Reaxys; Patent; NOVARTIS AG; NOVARTIS PHARMA GmbH; WO2007/41366; (2007); (A1) English, View in Reaxys; Patent; Bristol-Myers Squibb Company; US2007/99913; (2007); (A1) English, View in Reaxys; Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55728; (2007); (A1) English, View in Reaxys; Patent; IRM LLC; WO2007/89557; (2007); (A2) English, View in Reaxys; Patent; IRM LLC; WO2007/89667; (2007); (A1) English, View in Reaxys; Patent; Bristol-Myers Squibb Company; US2008/9533; (2008); (A1) English, View in Reaxys; Patent; IRM LLC; WO2005/113519; (2005); (A1) English, View in Reaxys
anti-diabetic agent
Page/Page column 10; 32
Patent; Bristol-Myers Squibb Company; US2008/9534; (2008); (A1) English, View in Reaxys
Anorectic agent
Page/Page column 10; 32
Patent; Bristol-Myers Squibb Company; US2008/9534; (2008); (A1) English, View in Reaxys
Insulin resistance
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys; Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Antiobesity agent
Patent; Novo Nordisk, A/S; US6972294; (2005); (B1) English, View in Reaxys; Patent; NOVO NORDISK A/S; WO2007/144394; (2007); (A2) English, View in Reaxys
Appetite suppressant
Patent; Bhanot, Sanjay; Dobie, Kenneth W.; US2005/261233; (2005); (A1) English, View in Reaxys; Patent; POMYTKIN, Igor Anatolievich; SOLOVIEV, Sergey Pavlovich; WO2007/69932; (2007); (A1) English, View in Reaxys
metabolic syndrome
Patent; Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; Koehler-Stec, Ellen-Marie; US2006/58224; (2006); (A1) English, View in Reaxys; Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Anti-obesity compound
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2006/67428; (2006); (A2) English, View in Reaxys; Patent; PFIZER PRODUCTS INC.; WO2006/90250; (2006); (A1) English, View in Reaxys; Patent; ASTRAZENECA AB; WO2007/64272; (2007); (A1) English, View in Reaxys
food-related disorders
Patent; LABORATORIOS DEL DR. ESTEVE, S.A.; EP1743636; (2007); (A1) English, View in Reaxys
Antiobesity compound
Patent; MERCK and CO., INC.; WO2006/127530; (2006); (A2) English, View in Reaxys; Patent; MERCK FROSST CANADA LTD.; WO2007/134457; (2007); (A1) English, View in Reaxys
cannabinoid 1 (CB1) receptor modulator; lipase inhibitor
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Food-related disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Digestive metabolism
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Regulate food intake
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Modulate energy expenditure
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Reduce central anorexigenic effects
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
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11/98
2018-06-23 10:56:32
Reduce peripheral anorexigenic effects
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
bulimia
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
anorexia
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
cachexia
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
drug-induced obesity
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
appetence disorder
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
appetite disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
eating disorders associated with excessive food intake
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
type Il diabetus mellitus
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
non-insuline dependent diabetes mellitus
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Improve cardiovascular
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Improve metabolic risk factor
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Elevated triglycerides
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Lower HDL cholesterol
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Impaired fasting glucose
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Dyslipidemia
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
weight independent aspects of metabolic syndrome
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Restenosis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Psychosis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
alcohol abuse
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
nicotine abuse
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
drug abuse
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
medicament abuse
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
schizophrenia
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
anxiety
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
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12/98
2018-06-23 10:56:32
neurodegenerative disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Morbus Parkinson
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Morbus Huntington
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Morbus Alzheimer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Multiple Sclerosis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
cerebellar disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
spinocerebellar disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
cognitive disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
cranial trauma
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
panic attacks
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
peripheric neuropathy
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
glaucoma
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Raynaud's disease
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
tremblement disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
compulsive disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
senile dementia
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
thymic disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
tardive dyskinesia
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
bone disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
osteoporosis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Paget's disease of bone
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
brain cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
bone cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
lip cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
mouth cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
13/98
2018-06-23 10:56:32
esophageal cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
stomach cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
liver cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
bladder cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
pancreas cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
ovary cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
cervical cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
lung cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
breast cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
skin cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
colon cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
bowl cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
prostate cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
colcon cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
bowel cancer
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
medicament-induced movement disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
dystonia
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
endotoxemic shock
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
stroke
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
hemorrhagic shock
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
hypotension
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
insomnia
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
immunologic disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
sclerotic plaques
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
diarrhea
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
asthma
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
14/98
2018-06-23 10:56:32
memory disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
pruritus
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
pain
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
potentiation of the analgesic effect of narcotic
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
influencing intestinal transit
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
potentiation of the non-narcotic analgesics effect of narcotic
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
dementia
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
memory loss
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
vascular dementia
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
mild cognitive impairment
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
frontotemporal dementia
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Pick's disease
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
binge eating disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
juvenile obesity
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
drug induced obesity
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
atypical depression
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
behavioural addictions
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
attention deficit disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Tourette's syndrome
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
suppression of reward- related behaviours
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
conditioned place avoidance
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
suppression of cocaine-induced conditioned place preference
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
suppression of morphine-induced conditioned place preference
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
15/98
2018-06-23 10:56:32
impulsivity
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
sexual dysfunction
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
erectile difficulty
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
female sexual dysfunction
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
seizure disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
nausea
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
emesis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
neuroinflammatory disease
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
demyelinisation related disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Guillan-Barre syndrome
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
viral encephalitis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
cerebrovascular accidents
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Neurological disorder
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
muscle spasticity
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
traumatic brain injury
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
spinal cord injury
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
inflammation
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
immunomodulatory disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
cutaneous T-cell lymphoma
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
rheumatoid arthritis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
systemic lupus erythematosus
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
sepsis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
sarcoidosis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
idiopathic pulmonary fibrosis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
bronchopulmonary dysplasia
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
retinal disease
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
16/98
2018-06-23 10:56:32
Scleroderma
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
renal ischemia
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
mycocardial infarction
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
cerebral ischemia
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
nephritis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
hepatitis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
glomerulonephritis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
cryptogenic fibrosing aveolitis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
psoriasis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
transplant rejection
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
atopic dermatitis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
vasculitis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
allergy
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Seasonal allergic rhinitis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Crohn's disease
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
inflammatory bowel disease
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
reversible airway obstruction
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
adult respiratory distress syndrome
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
chronic obstructive pulmonary disease
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
bronchitis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
cerebral apoplexy
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
craniocerebral trauma
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
neuropathic pain disorders
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
gastric ulcers
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
atheriosclerosis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
liver cirrhosis
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
17/98
2018-06-23 10:56:32
Acute health problems
Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
melanocortin 3 receptor (MC3-R) agonist; (MC4-R) agonist; α-melanocyte stimulating hormone (α-MSH) activity enhancer; POMC neuron activity promoter; selective serotonin reuptake inhibitor (SSRI); serotonin 2C agonist; serotonin 1B agonist; agouti-related protein (AgRP) inhibitor; neruopeptide Y (NPY) inhibitor; αamino butyric acid (GABA) inhibitor; GABA receptor antagonist; GABA channel antagonist; dopamine agonist; dopamine reuptake inhibitor; norepinephrine agonist
Patent; OREXIGEN THERAPEUTICS, INC.; WO2007/16108; (2007); (A1) English, View in Reaxys
Anti-obesity
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2007/10222; (2007); (A2) English, View in Reaxys; Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2007/39740; (2007); (A2) English, View in Reaxys
weight loss agent
Patent; Schering Corporation; US2007/66644; (2007); (A1) English, View in Reaxys
α-adrenergic receptor agonist, preferably α-3 receptor agonist
Patent; MELIOR DISCOVERY, INC.; WO2007/24863; (2007); (A2) English, View in Reaxys
anti-obesity drug
Patent; MELIOR DISCOVERY, INC.; WO2007/24863; (2007); (A2) English, View in Reaxys
selective serotonin reuptalce inhibitor
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55728; (2007); (A1) English, View in Reaxys
Obesity-related disorder
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55728; (2007); (A1) English, View in Reaxys
Insulin-resistance syndrome
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55728; (2007); (A1) English, View in Reaxys; Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55743; (2007); (A2) English, View in Reaxys
Lipodystrophy
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55728; (2007); (A1) English, View in Reaxys; Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55743; (2007); (A2) English, View in Reaxys
Nonalcoholic steatohepatitis
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55728; (2007); (A1) English, View in Reaxys
Cardiovascular disease
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55728; (2007); (A1) English, View in Reaxys; Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55743; (2007); (A2) English, View in Reaxys
Obesity related disorders
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55743; (2007); (A2) English, View in Reaxys
Nonalcoholic steatohepatitis (NASH)
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55743; (2007); (A2) English, View in Reaxys
Desire to lose body weight
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55743; (2007); (A2) English, View in Reaxys
Metabolic conditions
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55743; (2007); (A2) English, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
18/98
2018-06-23 10:56:32
Type 2 dependent diabetes
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55743; (2007); (A2) English, View in Reaxys
Non-insulin dependent diabetes
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55743; (2007); (A2) English, View in Reaxys
gestational diabetes
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55743; (2007); (A2) English, View in Reaxys
Eating disorders
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55743; (2007); (A2) English, View in Reaxys
Therapeutic agent
Patent; Mallinckrodt Inc.; US2007/129444; (2007); (A1) English, View in Reaxys
Diabetes
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys; Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55728; (2007); (A1) English, View in Reaxys; Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55743; (2007); (A2) English, View in Reaxys
Hypertension
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys; Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Metabolic syndrome
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys; Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55728; (2007); (A1) English, View in Reaxys; Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55743; (2007); (A2) English, View in Reaxys
Polycystic ovary syndrome
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys; Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55728; (2007); (A1) English, View in Reaxys; Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55743; (2007); (A2) English, View in Reaxys
Type 1 diabetes
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys; Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55743; (2007); (A2) English, View in Reaxys
vomiting
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys; Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
Appetite regulating agent
Patent; IRM LLC; WO2007/89557; (2007); (A2) English, View in Reaxys; Patent; IRM LLC; WO2007/89667; (2007); (A1) English, View in Reaxys
bipolar disorders
Patent; OREXIGEN THERAPEUTICS, INC.; WO2006/17504; (2006); (A1) English, View in Reaxys; Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys
appetite suppresant; antiobesity agent
Patent; GELESIS, INC.; WO2007/112436; (2007); (A2) English, View in Reaxys
enhancing gastric retention
Patent; GELESIS, INC.; WO2007/112436; (2007); (A2) English, View in Reaxys
controlled drug delivery
Patent; GELESIS, INC.; WO2007/112436; (2007); (A2) English, View in Reaxys
inducing weight loss
Patent; GELESIS, INC.; WO2007/112436; (2007); (A2) English, View in Reaxys
gastrointestinal disorders
Patent; GELESIS, INC.; WO2007/112436; (2007); (A2) English, View in Reaxys
Obesity
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys; Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys; Patent; LABORATORIOS DEL DR.ESTEVE, S.A; WO2007/9693; (2007); (A1) English, View in Reaxys; Patent; AMYLIN PHARMACEUTICALS, INC.; WO2007/55743; (2007); (A2) English, View in Reaxys; Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2005/95354; (2005); (A1) English, View in Reaxys
anti-obesity compound
Page/Page column 26
Patent; ASTRAZENECA AB; WO2007/18460; (2007); (A1) English, View in Reaxys
Anorectic agent
Page/Page column 13
Patent; KARO BIO AB; WO2007/39125; (2007); (A2) English, View in Reaxys
Anti-obesity drug
Page/Page column 31
Patent; NOVARTIS AG; NOVARTIS PHARMA GmbH; WO2007/67613; (2007); (A1) English, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
19/98
2018-06-23 10:56:32
Anti-obesity agent
Page/Page column 36
Patent; NOVARTIS AG; NOVARTIS PHARMA GmbH; WO2007/67615; (2007); (A2) English, View in Reaxys
Syndrome X
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys; Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Stroke
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys; Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Hyperlipidemia
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys; Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
A component of composition for treatment of obesity or an obesity-related condition
Patent; Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; Koehler-Stec, Ellen-Marie; US2006/58224; (2006); (A1) English, View in Reaxys
reduction in body weight
Patent; Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; Koehler-Stec, Ellen-Marie; US2006/58224; (2006); (A1) English, View in Reaxys
improvement in diabetic parameters
Patent; Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; Koehler-Stec, Ellen-Marie; US2006/58224; (2006); (A1) English, View in Reaxys
liver steatosis
Patent; Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; Koehler-Stec, Ellen-Marie; US2006/58224; (2006); (A1) English, View in Reaxys
fasting glucose and insulin levels
Patent; Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; Koehler-Stec, Ellen-Marie; US2006/58224; (2006); (A1) English, View in Reaxys
oral glucose tolerance, triglycerides and non-esterified free-fatty acids
Patent; Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; Koehler-Stec, Ellen-Marie; US2006/58224; (2006); (A1) English, View in Reaxys
type II diabetes
Patent; Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; Koehler-Stec, Ellen-Marie; US2006/58224; (2006); (A1) English, View in Reaxys
therapeutic agent
Patent; Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; Koehler-Stec, Ellen-Marie; US2006/58224; (2006); (A1) English, View in Reaxys
vasoconstricting agent
Patent; Higuchi, John; Li, S. Kevin; Higuchi, William I.; Hastings, Matthew S.; US2006/88515; (2006); (A1) English, View in Reaxys
sympathomimetic
Patent; Higuchi, John; Li, S. Kevin; Higuchi, William I.; Hastings, Matthew S.; US2006/88515; (2006); (A1) English, View in Reaxys
Anti-obezity agent
Patent; Meng, Wei; Hamann, Lawrence G.; Brigance, Robert; US2006/142576; (2006); (A1) English, View in Reaxys
stimulant
Patent; Kirk, Randal J.; US2006/100136; (2006); (A1) English, View in Reaxys
Anti-diabetic agent
Patent; JOHN I. HASS, INC.; WO2006/55985; (2006); (A1) English, View in Reaxys
sympathomimetic agent of controlledrelease pharmaceutical composition which is capable of delivering therapeutic amounts of active agent to specific region of gastrointestinal tract
Patent; Elan Corporation, plc; US2006/121112; (2006); (A1) English, View in Reaxys
in combination with topiramate
Patent; Elan Corporation, plc; US2006/121112; (2006); (A1) English, View in Reaxys
partial seizures with or without secondarily generalized seizures
Patent; Elan Corporation, plc; US2006/121112; (2006); (A1) English, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
20/98
2018-06-23 10:56:32
primary generalized tonic-clonic seizures
Patent; Elan Corporation, plc; US2006/121112; (2006); (A1) English, View in Reaxys
seizures associated with Lennox Gastaut Syndrome
Patent; Elan Corporation, plc; US2006/121112; (2006); (A1) English, View in Reaxys
migraines
Patent; Elan Corporation, plc; US2006/121112; (2006); (A1) English, View in Reaxys
potassium ATP (KATP) channel opener; inhibition of fasting insulin secretion; inhibition of stimulated insulin secretion; elevation of energy expenditure; elevation of beta oxidation of fat; Reduced glyceraldehyde phosphate dehydrogenase activity of adipocytes; Reduced expression of fatty acid synthase by adipocytes; Enhanced lipolysis by adipocytes; Reduced production of lipoprotein lipase by adipocytes; enhanced expression of α3 Adrenergic Receptor (α3AR)
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Disease involving KATP channels
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Hyperphagia
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Hypoglycemia
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Obesity associated co-morbidities
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
weight loss
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Reducing visceral fat
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Restore normal glucose tolerance
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
weight gain
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Impaired glucose tolerance
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Dyslipidemia associated with the use of the anti-psychotics
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Prader-Willi Syndrome
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Froelich's Syndrome
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Cohen Syndrome
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Summit Syndrome
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Alstrom Syndrome
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
21/98
2018-06-23 10:56:32
Borjeson Syndrome
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Bardet-Biedl Syndrome
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Hyperlipoproteinemia type I
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Hyperlipoproteinemia type II
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Hyperlipoproteinemia type III
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Hyperlipoproteinemia type IV
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Reducing the incidence of adverse effects
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Prediabetes
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Type 2 diabetes
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Osteoarthritis
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Cardiovascular condition
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Metabolic disease
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Hyperinsulemia
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Hyperinsulinism
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Preservation of pancreatic function in type 1 diabetics
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Prevention of the transition from prediabetes to diabetes
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Correction of the defects in insulin secretion contributing to prediabetes
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Correction of the defects in insulin secretion contributing to type II diabetes
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Correction of the defects in insulin sensitivity contributing to prediabetes
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Correction of the defects in insulin sensitivity contributing to type II diabetes
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Ischemic injury
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Reperfusion injury
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Provide beta cell rest
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Beta cell failure
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Improved glycemic control
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Reduction in blood pressure
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Myocardial infarct
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Edema
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Fluid retention
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Reduced rates of excretion of sodium
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Reduced rates of excretion of chloride
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Reduced rates of excretion of uric acid
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
ketoacidosis
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Nausea
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Dyspepsia
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Ileus
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
Headaches
Patent; Essentialis, Inc.; US2006/51418; (2006); (A1) English, View in Reaxys
compositions for affecting weight loss
Patent; OREXIGEN THERAPEUTICS, INC.; WO2006/17504; (2006); (A1) English, View in Reaxys
increasing energy expenditure
Patent; OREXIGEN THERAPEUTICS, INC.; WO2006/17504; (2006); (A1) English, View in Reaxys
increasing satiety
Patent; OREXIGEN THERAPEUTICS, INC.; WO2006/17504; (2006); (A1) English, View in Reaxys
suppressing the appetite of an individual
Patent; OREXIGEN THERAPEUTICS, INC.; WO2006/17504; (2006); (A1) English, View in Reaxys
Composition for the Page/Page column treating, preventing, 53; 96 or ameliorating one or more symptoms of a protein tyrosine phosphatase mediated disease
Patent; CENGENT THERAPEUTICS, INC.; WO2006/28970; (2006); (A1) English, View in Reaxys
Anti-obesity agent
Patent; PFIZER PRODUCTS INC.; WO2006/33001; (2006); (A1) English, View in Reaxys
Page/Page column 30
modulating central norepinephrine and dopamine receptors through the promotion of catecholamine release
Patent; PFIZER PRODUCTS INC.; WO2005/61506; (2005); (A1) English, View in Reaxys; Patent; PFIZER PRODUCTS INC.; WO2005/61507; (2005); (A1) English, View in Reaxys
Adrenergic agent
Patent; PFIZER PRODUCTS INC.; WO2005/61506; (2005); (A1) English, View in Reaxys; Patent; PFIZER PRODUCTS INC.; WO2005/61507; (2005); (A1) English, View in Reaxys
Type 2 diabetes mellitus
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Hypertension including hypertension in the elderly
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Familial dyslipidemic hypertension
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Isolated systolic hypertension(ISH)
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Increased collagen formation
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Fibrosis
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Remodeling following hypertension
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Erectile dysfunction
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Impaired vascular compliance
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Congestive heart failure
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Left ventricular hypertrophy
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Survival post myocardial infarction(MI)
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Coronary artery diseases
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Atherosclerosis
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Angina pectoris
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Thrombosis
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Renal failure
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Chronic renal failure
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Glomerulosclerosis
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Nephropathy
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Hypothyroidism
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Endothelial dysfunction with or without hypertension
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Hyperlipoproteinemia
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Hypertryglyceridemia
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Hypercholesterolemia
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Macular degeneration
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Cataract
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Glaucoma
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Skin and connective tissue disorders
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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2018-06-23 10:56:32
Restenosis after percutaneous transluminal angioplasty
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Restenosis after coronary artery bypass surgery
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Peripheral vascular disease
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Reproductive disorders
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Pulmonary disease
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Gallstones
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Fasting-inducedcholecystitis
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Cancers
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Cutaneous disease
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Cushing's syndrome
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Insulinoma
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Craniopharyngioma
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
Premenstrual syndrome
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/49088; (2005); (A2) English, View in Reaxys
anorectic
Patent; Boehringer Ingelheim International GmbH; US2005/245500; (2005); (A1) English, View in Reaxys
appetite suppressant
Patent; BLM Group, Inc.; US2005/222040; (2005); (A1) English, View in Reaxys
weight loss promotor
Patent; BLM Group, Inc.; US2005/222040; (2005); (A1) English, View in Reaxys
noradrenergic agent
Patent; BLM Group, Inc.; US2005/222040; (2005); (A1) English, View in Reaxys
pharmaceutical composition
Patent; BLM Group, Inc.; US2005/222040; (2005); (A1) English, View in Reaxys
combination therapy
Patent; BLM Group, Inc.; US2005/222040; (2005); (A1) English, View in Reaxys
Appetite-regulating agent
Patent; IRM LLC; WO2005/113506; (2005); (A1) English, View in Reaxys; Patent; IRM LLC; WO2005/113519; (2005); (A1) English, View in Reaxys
Anorectic agent
Patent; MERCK and CO., INC.; WO2003/87037; (2003); (A1) English, View in Reaxys
Isolation from Natural Product (1) Isolation from Nat- References ural Product Rabbit liver
Beckett; Belanger; Journal of Pharmacy and Pharmacology; vol. 27; nb. 12; (1975); p. 928 - 936, View in Reaxys
Medchem (81) 1 of 81
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : Body weight and food intake; effect onTarget : Diet-Induced Obesity; AKR/J mouseBioassay : A study was conducted to determine the effect of the combination of phentermine and Axokine™ on body weight and food intake in a mouse model of obesity. 30 DIO (Diet-Induced
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
25/98
2018-06-23 10:56:32
Obesity; AKR/J mice fed a high fat diet) mice were divided into 5 equal groups (n=6 per group). Four groups were treated Substance RN
970319View in Reaxys
Substance Name
4834
Substance Route of Adm.
intraperitoneal administration
Qualitative Results
After 21 days of treatment, animals receiving test compound lost approximately 15% of their starting body weight, while control animals had a decrease of 2%. Test compound treated mice also had decreased food intake relative to control but the overall
Measurement Parameter
qualitative
Patent; Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; Koehler-Stec, Ellen-Marie; US2006/58224; (2006); (A1) English, View in Reaxys 2 of 81
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : locomotor behaviors; effect onTarget : DAT-KO mouseBioassay : Experimental We report here that the pharmacologic inhibition of the rate-limiting enzyme of DA synthesis, TH, almost immediately depletes brain DA to undetectable levels in DAT-KO mice and induces a transient recapitulation of essentially all PD symptoms for up to 16 h. DA-deficient DAT-KO mice (DDD
Substance RN
970319View in Reaxys
Substance Name
4834
Qualitative Results
Akinesia test: ~10-40 number of steps; at Catalepsy test: ~30-180sec; at Grasping test: ~10-30 seconds time spent on the rod of the title compound administered after 1h of αMT treatment; figure is given
Measurement Parameter
qualitative
Patent; Caron, Marc G.; Sotnikova, Tatyana D.; Gainetdinov, Raul R.; US2007/27208; (2007); (A1) English, View in Reaxys 3 of 81
Target Name
alpha-adrenergic receptor [rat]
Target Synonyms
alpha-adrenergic receptor
Target, Subunit, Species
alpha-adrenergic receptor [rat]
Target Mutant/Chimera Details
alpha-adrenergic receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain
Substance RN
970319View in Reaxys
Substance Name
Phentermine
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Quantitative value
1400
Deviation
100
Measurement pX
5.85
Concomitants: Compound RN
883415; 2804840
Concomitants: Compound name
[3H]-Clonidine; Norepinephrine
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
26/98
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4 of 81
5 of 81
Concomitants: Compound role
RAD; NSB
Target Name
alpha-adrenergic receptor [rat]
Target Synonyms
alpha-adrenergic receptor
Target, Subunit, Species
alpha-adrenergic receptor [rat]
Target Mutant/Chimera Details
alpha-adrenergic receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain
Substance RN
970319View in Reaxys
Substance Name
Phentermine
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Quantitative value
24000
Deviation
3100
Measurement pX
4.62
Concomitants: Compound RN
2804840; 4206776
Concomitants: Compound name
Norepinephrine; [3H]-WB 4101
Concomitants: Compound role
NSB; RAD
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Substance RN
970319View in Reaxys
Substance Name
4834
Qualitative Results
inhibition of rat pancreatic lipase
Measurement Parameter
qualitative
Comai; Sullivan; Journal of Pharmaceutical Sciences; vol. 71; nb. 4; (1982); p. 418 - 421, View in Reaxys 6 of 81
Substance Effect
Antiobesity
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Bioassay : overweight rats were used; TG: total triacylglycerol; TC: total cholesterol; AST and ALT: aspartate and alanine transaminase; HOMA: homeostasis model assessment; untreated control title comp. administered; body weight and food intake recorded; rats were killed; body composition (energy, lipid) determined using bomb calorimeter; serum TG, TC, insulin, glucose, AST, ALT, 3-hydroxybutyrate levels, HOMA score measured
Biological Species/NCBI ID
rat
Substance RN
970319View in Reaxys
Substance Name
4834
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
27/98
2018-06-23 10:56:32
Substance Dose
5 mg/kg
Substance Route of Adm.
oral administration
Qualitative Results
title comp. did not significantly affect body weight and energy, food intake; title comp. did not reduce glucose, 3-hydroxybutyrate, AST but induced increase in ALT levels (diagram, table)
Measurement Parameter
qualitative
Ferrer-Lorente, Raquel; Cabot, Cristina; Fernandez-Lopez, Jose-Antonio; Remesar, Xavier; Alemany, Maria; European Journal of Pharmacology; vol. 513; nb. 3; (2005); p. 243 - 248, View in Reaxys 7 of 81
8 of 81
Target Name
trace amine-associated receptor 1 [human]
Target Synonyms
ta1; taar1; tar-1; tar1; trace amine receptor 1; trace amine-associated receptor 1; trar1
Target Uniprot ID
q96rj0
Target, Subunit, Species
trace amine-associated receptor 1 [human]
Target Mutant/Chimera Details
trace amine-associated receptor 1 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
cAMP production
Cells/Cell Lines
HEK293T cell line
Substance RN
970319View in Reaxys
Substance Name
Phentermine
Substance Dose
1.00000E-10 M
Measurement Parameter
EC50
Unit
M
Quantitative value
1.08E-06
Deviation
4.00000E-08
Measurement pX
5.97
Concomitants: Compound RN
902535
Concomitants: Compound name
Coelenterazine
Concomitants: Compound role
COM
Target Name
trace amine-associated receptor 1 [human]
Target Synonyms
ta1; taar1; tar-1; tar1; trace amine receptor 1; trace amine-associated receptor 1; trar1
Target Uniprot ID
q96rj0
Target, Subunit, Species
trace amine-associated receptor 1 [human]
Target Mutant/Chimera Details
trace amine-associated receptor 1 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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9 of 81
10 of 81
Bioassay Name
cAMP production
Cells/Cell Lines
HEK293T cell line
Substance RN
970319View in Reaxys
Substance Name
Phentermine
Substance Dose
1.00000E-10 M
Measurement Parameter
Emax
Unit
%
Quantitative value
87.7
Deviation
1.10000
Concomitants: Compound RN
902535
Concomitants: Compound name
Coelenterazine
Concomitants: Compound role
COM
Target Name
Potassium channel
Target Synonyms
potassium channel; potassium channel activity
Target, Subunit, Species
Potassium channel
Target Mutant/Chimera Details
Potassium channel:Wild
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Bioassay Details
Effect : potassium channel; inhibition ofBioassay : cells expressing human Kv1.5 voltage-gated potassium channel; further studies on voltage-dependence potassium outward current measured at 23-25 deg C, in whole cell configuration of patch-clamp technique; voltage-clamp protocols applied; amplitude of current assessed at end of 250-ms command pulse voltages applied every 15 s from -70 to +50 mV
Cells/Cell Lines
CHO cell line
Substance RN
970319View in Reaxys
Substance Name
4834
Substance Dose
30 µM
Qualitative Results
title comp. dose-dependently inhibited potassium current, at 300 μmol/l 21 percent of current blocked
Measurement Parameter
qualitative
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : incorporation into hairTarget : Dark-Agouti ratsBioassay : rats of 95-105 g, 5 wks old; back hair of rats shaved; hair collected; blood collected 5, 15, 30, 60, 120, 360 min after dosing; plasma prepared; areas under conc. vs. time curve (AUCs) calculated; incorporated rates (ICRs) determination
Substance RN
970319View in Reaxys
Substance Name
4834
Substance Dose
5 mg/kg
Substance Route of Adm.
intraperitoneal administration
Qualitative Results
AUC, 211.4 μg*min/ml; 35.55 ng/mg conc. in hair; ICR, 0.17
Measurement Parameter
qualitative
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
29/98
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Nakahara, Yuji; Kikura, Ruri; Archives of Toxicology; vol. 70; nb. 12; (1996); p. 841 - 849, View in Reaxys 11 of 81
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |transmitter releasing Target : rat caudate putamen crude vesicular fractionBioassay : EC50 for title comp. inhibition of <3H>dopamine release vesicular fraction preloaded with 60 nmol/l <3H>dopamine for 20 min at 25 deg C, incubated with title comp. for 10 min at 25 deg C; rapid filtration; liquid scintillation counting; <3H>dopamine release evaluated
Substance RN
970319View in Reaxys
Substance Name
4834
Measurement Parameter
EC50
Unit
µM
Quantitative value
100
Measurement pX
4
Partilla, John S.; Dempsey, Allison G.; Nagpal, Ameet S.; Blough, Bruce E.; Baumann, Michael H.; Rothman, Richard B.; Journal of Pharmacology and Experimental Therapeutics; vol. 319; nb. 1; (2006); p. 237 - 246, View in Reaxys 12 of 81
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |transmitter releasing Target : rat caudate putamen crude vesicular fractionBioassay : EC50 for title comp. inhibition of <3H>tyramine release vesicular fraction preloaded with 60 nmol/l <3H>tyramine for 20 min at 25 deg C, incubated with title comp. for 2 min at 25 deg C; rapid filtration; liquid scintillation counting; <3H>tyramine release evaluated
Substance RN
970319View in Reaxys
Substance Name
4834
Measurement Parameter
EC50
Unit
µM
Quantitative value
100
Measurement pX
4
Partilla, John S.; Dempsey, Allison G.; Nagpal, Ameet S.; Blough, Bruce E.; Baumann, Michael H.; Rothman, Richard B.; Journal of Pharmacology and Experimental Therapeutics; vol. 319; nb. 1; (2006); p. 237 - 246, View in Reaxys 13 of 81
Target Name
Synaptic vesicular amine transporter
Target Synonyms
monoamine transporter; slc18a2; solute carrier family 18 member 2; svat; svmt; synaptic vesicular amine transporter; vat2; vesicular amine transporter 2; vmat2
Target, Subunit, Species
Synaptic vesicular amine transporter
Target Mutant/Chimera Details
Synaptic vesicular amine transporter:Wild
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : monoamine transporter; interaction withBioassay : DHTBZ: dihydrotetrabenazine; VMAT2: vesicular monoamine transporter type 2; IC50 for title comp. inhibition of <3H>DHTBZ binding vesicular fraction incubated with title comp. and 2 nmol/l <3H>DHTBZ for 4 h at 25 deg C; rapid filtration; liquid scintillation counting
Substance RN
970319View in Reaxys
Substance Name
4834
Measurement Parameter
IC50
Unit
µM
Quantitative value
100
Measurement pX
4
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Partilla, John S.; Dempsey, Allison G.; Nagpal, Ameet S.; Blough, Bruce E.; Baumann, Michael H.; Rothman, Richard B.; Journal of Pharmacology and Experimental Therapeutics; vol. 319; nb. 1; (2006); p. 237 - 246, View in Reaxys 14 of 81
Target Name
Synaptic vesicular amine transporter
Target Synonyms
monoamine transporter; slc18a2; solute carrier family 18 member 2; svat; svmt; synaptic vesicular amine transporter; vat2; vesicular amine transporter 2; vmat2
Target, Subunit, Species
Synaptic vesicular amine transporter
Target Mutant/Chimera Details
Synaptic vesicular amine transporter:Wild
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : monoamine transporter; interaction withBioassay : DHTBZ: dihydrotetrabenazine; VMAT2: vesicular monoamine transporter type 2; IC50 for title comp. inhibition of <3H>dopamine uptake vesicular fraction incubated with title comp. and 60 nmol/l <3H>dopamine for 5 min at 25 deg C; rapid filtration; liquid scintillation counting
Substance RN
970319View in Reaxys
Substance Name
4834
Measurement Parameter
IC50
Unit
µM
Quantitative value
100
Measurement pX
4
Partilla, John S.; Dempsey, Allison G.; Nagpal, Ameet S.; Blough, Bruce E.; Baumann, Michael H.; Rothman, Richard B.; Journal of Pharmacology and Experimental Therapeutics; vol. 319; nb. 1; (2006); p. 237 - 246, View in Reaxys 15 of 81
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : fat mass; effect onTarget : DIO (Levin) ratBioassay : EXAMPLE 4[00268] To demonstrate effects of the combination of amylin and a serotonergic/noradrenergic reuptake inhibitor on changes in body weight and body composition, DIO male rats were fattened and divided into four treatment groups, as described in Example 2. Rat amylin was dissolved in 50% DMSO
Substance RN
970319View in Reaxys
Substance Name
4834
Substance Route of Adm.
oral administration
Qualitative Results
title compound at 10 mg/kg/day produced the fat mass loss to be ~-5 grams at ~0-2w treatment; synergistic effect at ~-40 grams was observed when the compound was administered with amylin; figure is given
Measurement Parameter
qualitative
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2006/105527; (2006); (A3) English, View in Reaxys 16 of 81
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : lean (protein) mass; effect onTarget : DIO (Levin) ratBioassay : EXAMPLE 4[00268] To demonstrate effects of the combination of amylin and a serotonergic/noradrenergic reuptake inhibitor on changes in body weight and body composition, DIO male rats were fattened and divided into four treatment groups, as described in Example 2. Rat amylin was dissolved in 50% DMSO
Substance RN
970319View in Reaxys
Substance Name
4834
Substance Route of Adm.
oral administration
Qualitative Results
title compound at 10mg/kg/day did not change the lean (protein) mass at ~0-2w treatment; title compound administered with amylin tended to have the greatest increase in the lean (protein) mass at ~6 grams; figure is given
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Measurement Parameter
qualitative
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2006/105527; (2006); (A3) English, View in Reaxys 17 of 81
Substance Effect
Body Weight
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : DIO (Levin) ratBioassay : EXAMPLE 4[00268] To demonstrate effects of the combination of amylin and a serotonergic/noradrenergic reuptake inhibitor on changes in body weight and body composition, DIO male rats were fattened and divided into four treatment groups, as described in Example 2. Rat amylin was dissolved in 50% DMSO
Substance RN
970319View in Reaxys
Substance Name
4834
Substance Route of Adm.
oral administration
Qualitative Results
title compound at 10 mg/kg/day produced ~5% decrease in body weight at ~0-2w treatment; administration with amylin produced ~12% decrease in body weight; figure is given
Measurement Parameter
qualitative
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2006/105527; (2006); (A3) English, View in Reaxys 18 of 81
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : body fat; effect onTarget : Diet-induced obesity (DIO) ratBioassay : EXAMPLE 4[00270] To demonstrate effects of the combination of amylin and a serotonergic/noradrenergic reuptake inhibitor on changes in body weight and body composition, DIO male rats were fattened and divided into four treatment groups, as described in Example 2. Rat amylin was dissolved in 50% DMSO
Substance RN
970319View in Reaxys
Substance Name
4834
Qualitative Results
modest amount of fat loss was evident with title compound treatment; figure is given
Measurement Parameter
qualitative
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2006/105527; (2006); (A3) English, View in Reaxys 19 of 81
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : body protein; effect onTarget : Diet-induced obesity (DIO) ratBioassay : EXAMPLE 4[00270] To demonstrate effects of the combination of amylin and a serotonergic/noradrenergic reuptake inhibitor on changes in body weight and body composition, DIO male rats were fattened and divided into four treatment groups, as described in Example 2. Rat amylin was dissolved in 50% DMSO
Substance RN
970319View in Reaxys
Substance Name
4834
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2006/105527; (2006); (A3) English, View in Reaxys 20 of 81
Substance Effect
Body Weight
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Target : Diet-induced obesity (DIO) ratBioassay : EXAMPLE 4[00270] To demonstrate effects of the combination of amylin and a serotonergic/noradrenergic reuptake inhibitor on changes in body weight and body composition, DIO male rats were fattened and divided into four treatment groups, as described in Example 2. Rat amylin was dissolved in 50% DMSO
Substance RN
970319View in Reaxys
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Substance Name
4834
Qualitative Results
title compound resulted in about a 5% decrease in body weight; figure is given
Measurement Parameter
qualitative
Patent; AMYLIN PHARMACEUTICALS, INC.; WO2006/105527; (2006); (A3) English, View in Reaxys 21 of 81
Substance Effect
Neuroregulatoric
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Bioassay : rats perfused, title comp. added, samples collected from striatal dialysis, dopamine (DA) and serotonin (5-HT) measured with HPLC
Biological Species/NCBI ID
rat
Substance RN
970319View in Reaxys
Substance Name
4834
Substance Dose
20 mg/kg
Substance Route of Adm.
intraperitoneal administration
Qualitative Results
title comp. increased striatal DA concentrations (148 +/- 17 percent) without affecting those of 5HT
Measurement Parameter
qualitative
Balcioglu, Aygul; Wurtman, Richard J.; Journal of Pharmacology and Experimental Therapeutics; vol. 284; nb. 3; (1998); p. 991 - 997, View in Reaxys 22 of 81
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : modulation of discriminative effect of cocaineBioassay : lever-responding drug discrimination test; rats trained to discriminate i.p. injected 10.0 mg/kg cocaine from saline; substitution test of title comp. at 20 min pre-session; percentage of rats making cocaine-lever selections counted
Biological Species/NCBI ID
rat
Substance RN
970319View in Reaxys
Substance Name
4834
Substance Dose
1.25000 mg/kg
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
ED50
Unit
mg/kg
Quantitative value
2.356
Schechter, Martin D.; McBurney, Denise; Life Sciences; vol. 59; nb. 20; (1996); p. PL303-PL308, View in Reaxys 23 of 81
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : modulation of discriminative effect of cocaineBioassay : fenfluramine coadministered at 2 mg/kg lever-responding drug discrimination test; rats trained to discriminate 10.0 mg/kg cocaine from saline; substitution test of title comp. in combination with fenfluramine at 20 min pre-session; percentage of rats making cocaine-lever selections counted
Biological Species/NCBI ID
rat
Substance RN
970319View in Reaxys
Substance Name
4834
Substance Dose
1.25000 mg/kg
Substance Route of Adm.
intraperitoneal administration
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Measurement Parameter
ED50
Unit
mg/kg
Quantitative value
2.356
Schechter, Martin D.; McBurney, Denise; Life Sciences; vol. 59; nb. 20; (1996); p. PL303-PL308, View in Reaxys 24 of 81
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |antagonist Target : adult rhesus monkeys (Macaca mulatta)Bioassay : acute treatment (0.3-10 mg/kg) with 10-100 μg/kg cocaine; subacute treatment (3 or 5.6 mg/kg); assessement with GBR 12909-maiintained responding (30 μg/kg) monkeys trained to sit in a chair, examined in an operant chamber; i.v. jugular catheter and vascular-access port inplanted; various light effects connected with various actions; effect of title comp. on cocaine abuse examined
Substance RN
970319View in Reaxys
Substance Name
4834
Substance Dose
0.100000 mg/kg
Substance Route of Adm.
intravenous administration
Qualitative Results
acute treatment with title comp. decreased cocaine maintained responding; subacute treatment also decreased cocaine-maintained responding more than food.maintained responding; decreased responding mainitained by GBR 12909 (30 μg/kg)
Measurement Parameter
qualitative
Wojnicki, Francis H. E.; Rothman, Richard B.; Rice, Kenner C.; Glowa, John R.; Journal of Pharmacology and Experimental Therapeutics; vol. 288; nb. 2; (1999); p. 550 - 560, View in Reaxys 25 of 81
Target Name
Cytochrome P450 1A2 [human]
Target Synonyms
cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3
Target Uniprot ID
p05177
Target PDB ID
2hi4
Target, Subunit, Species
Cytochrome P450 1A2 [human]
Target Mutant/Chimera Details
Cytochrome P450 1A2 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Non Transfected
Bioassay Category
Metabolism/Transport
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
human
Organs/Tissues
liver
Cell Fraction
Microsome
Substance RN
970319View in Reaxys
Substance Name
phentermine
Substance Dose
0 µM
Measurement Parameter
IC50
Unit
µM
Qualitative value
>
Quantitative value
250
Measurement pX
1
Metabolite RN
2208089
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Metabolite name
acetaminophen
Concomitants: Compound RN
1727945; 1869238; 3885115
Concomitants: Compound name
(+/-)-Isocitric acid; Phenacetin; NADP
Concomitants: Compound role
COM; SUB; COE
Target Name
Cytochrome P450 2C9 [human]
Target Synonyms
(r)-limonene 6-monooxygenase; (s)-limonene 6-monooxygenase; (s)-limonene 7-monooxygenase; cholesterol 25-hydroxylase; cyp2c10; cyp2c9; cypiic9; cytochrome p-450mp; cytochrome p450 2c9; cytochrome p450 mp-4; cytochrome p450 mp-8; cytochrome p450 pb-1; s-mephenytoin 4-hydroxylase
Target Uniprot ID
p11712
Target PDB ID
1og2; 1og5; 1r9o; 4nz2; 5a5i; 5a5j
Target, Subunit, Species
Cytochrome P450 2C9 [human]
Target Mutant/Chimera Details
Cytochrome P450 2C9 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Non Transfected
Bioassay Category
Metabolism/Transport
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
human
Organs/Tissues
liver
Cell Fraction
Microsome
Substance RN
970319View in Reaxys
Substance Name
phentermine
Substance Dose
0 µM
Measurement Parameter
IC50
Unit
µM
Qualitative value
>
Quantitative value
250
Measurement pX
1
Metabolite RN
2867981
Metabolite name
OH-tolbutamide
Concomitants: Compound RN
1984428; 1727945; 3885115
Concomitants: Compound name
Tolbutamide; (+/-)-Isocitric acid; NADP
Concomitants: Compound role
SUB; COM; COE
Target Name
Cytochrome P450 2D6 [human]
Target Synonyms
cholesterol 25-hydroxylase; cyp2d6; cyp2dl1; cypiid6; cytochrome p450 2d6; cytochrome p450db1; debrisoquine 4-hydroxylase
Target Uniprot ID
p10635
Target PDB ID
2f9q; 3qm4; 3tbg; 3tda; 4wnt; 4wnu; 4wnv; 4wnw; 4xry; 4xrz; 5tft; 5tfu
Target, Subunit, Species
Cytochrome P450 2D6 [human]
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Target Mutant/Chimera Details
Cytochrome P450 2D6 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Non Transfected
Bioassay Category
Metabolism/Transport
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
human
Organs/Tissues
liver
Cell Fraction
Microsome
Substance RN
970319View in Reaxys
Substance Name
phentermine
Substance Dose
0 µM
Measurement Parameter
IC50
Unit
µM
Qualitative value
>
Quantitative value
250
Measurement pX
1
Metabolite RN
88093
Metabolite name
dextrorphan
Concomitants: Compound RN
88549; 1727945; 3885115
Concomitants: Compound name
Dextromethorphan; (+/-)-Isocitric acid; NADP
Concomitants: Compound role
SUB; COM; COE
Target Name
Cytochrome P450 2E1 [human]
Target Synonyms
4-nitrophenol 2-hydroxylase; cyp2e; cyp2e1; cypiie1; cytochrome p450 2e1; cytochrome p450-j
Target Uniprot ID
p05181
Target PDB ID
3e4e; 3e6i; 3gph; 3koh; 3lc4; 3t3z
Target, Subunit, Species
Cytochrome P450 2E1 [human]
Target Mutant/Chimera Details
Cytochrome P450 2E1 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Non Transfected
Bioassay Category
Metabolism/Transport
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
human
Organs/Tissues
liver
Cell Fraction
Microsome
Substance RN
970319View in Reaxys
Substance Name
phentermine
Substance Dose
0 µM
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Measurement Parameter
IC50
Unit
µM
Qualitative value
>
Quantitative value
250
Measurement pX
1
Metabolite RN
8407512
Metabolite name
6-OH-chlorzoxazone
Concomitants: Compound RN
1727945; 638882; 3885115
Concomitants: Compound name
(+/-)-Isocitric acid; Chlorzoxazone; NADP
Concomitants: Compound role
COM; SUB; COE
Target Name
Cytochrome P450 3A [human]
Target Synonyms
cytochrome p450 3a
Target, Subunit, Species
Cytochrome P450 3A [human]
Target Mutant/Chimera Details
Cytochrome P450 3A [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Non Transfected
Bioassay Category
Metabolism/Transport
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
human
Organs/Tissues
liver
Cell Fraction
Microsome
Substance RN
970319View in Reaxys
Substance Name
phentermine
Substance Dose
0 µM
Measurement Parameter
IC50
Unit
µM
Qualitative value
>
Quantitative value
250
Measurement pX
1
Metabolite RN
899031
Metabolite name
alpha-OH-midazolam
Concomitants: Compound RN
625572; 1727945; 3885115
Concomitants: Compound name
Midazolam; (+/-)-Isocitric acid; NADP
Concomitants: Compound role
SUB; COM; COE
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
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Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
telencephalon
Substance RN
970319View in Reaxys
Substance Name
Phentermine
Measurement Parameter
IC50
Unit
µM
Quantitative value
158
Deviation
2
Measurement pX
3.8
Concomitants: Compound RN
2205872
Concomitants: Compound name
[3H]-d-Amphetamine
Concomitants: Compound role
RAD
Zaczek; Culp; Goldberg; Mccann; De Souza; The Journal of pharmacology and experimental therapeutics; vol. 257; nb. 2; (1991); p. 820 - 829, View in Reaxys 31 of 81
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |transmitter releasing Bioassay : title comp. administered with 5-HT1A receptor agonist, 8OH-DPAT (0.1 mg/kg, s.c.), fluoxetine (10 mg/kg), or D-fenfluramine (1 mg/kg); title comp. administered locally into hypothalamus followed by systemic title comp. injection; 5-HT: serotonin title comp. administered; microdialysis of hypothalamus performed; dialysate samples collected every 30 min and analyzed for 5-HT by high-performance liquid chromatography
Biological Species/NCBI ID
rat
Substance RN
970319View in Reaxys
Substance Name
4834
Substance Dose
1 mg/kg
Substance Route of Adm.
intraperitoneal administration
Qualitative Results
title comp. produced dose-dependent increases in extracellular 5-HT in hypothalamus; fluoxetine attenuated increase in 5-HT induced by title comp.; effect of title comp. increased in presence of Dfenfluramine
Measurement Parameter
qualitative
Tao, Rui; Fray, Anne; Aspley, Sue; Brammer, Richard; Heal, David; Auerbach, Sidney; European Journal of Pharmacology; vol. 445; nb. 1-2; (2002); p. 69 - 81, View in Reaxys 32 of 81
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Percent reduction in expression of dopamine transporter in mouse by compound was determined
Biological Species/NCBI ID
mouse
Substance RN
970319View in Reaxys
Measurement Parameter
percentage
Unit
%
Measurement Object
Reduction activity
Qualitative value
<
Quantitative value
10
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Sotnikova, Tatyana D; Beaulieu, Jean-Martin; Gainetdinov, Raul R; Caron, Marc G; CNS and neurological disorders drug targets; vol. 5; nb. 1; (2006); p. 45 - 56, View in Reaxys 33 of 81
Bioassay Category
In Vivo (Animal models)
Bioassay Details
Oral dose of the compound suppressing food consumption by 50 in rat after 1hr
Biological Species/NCBI ID
rat
Substance RN
970319View in Reaxys
Substance Route of Adm.
oral administration
Measurement Parameter
ED50
Unit
mg/kg
Qualitative value
=
Quantitative value
1.76
Aeberli; Eden; Gogerty; Houlihan; Penberthy; Journal of Medicinal Chemistry; vol. 18; nb. 2; (1975); p. 177 - 182, View in Reaxys 34 of 81
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Oral dose of the compound suppressing food consumption by 50 in rat after 4hr
Biological Species/NCBI ID
rat
Substance RN
970319View in Reaxys
Substance Route of Adm.
oral administration
Measurement Parameter
ED50
Unit
mg/kg
Qualitative value
=
Quantitative value
5.26
Aeberli; Eden; Gogerty; Houlihan; Penberthy; Journal of Medicinal Chemistry; vol. 18; nb. 2; (1975); p. 177 - 182, View in Reaxys 35 of 81
Bioassay Category
In Vivo (Animal models)
Bioassay Details
Oral dose of the compound suppressing food consumption by 50 in monkey after 90min
Biological Species/NCBI ID
Cercopithecidae
Substance RN
970319View in Reaxys
Substance Route of Adm.
oral administration
Measurement Parameter
ED50
Unit
mg/kg
Measurement Object
suppressing food consumption by 50% in monkey after 90min
Qualitative value
=
Quantitative value
0.29
Aeberli; Eden; Gogerty; Houlihan; Penberthy; Journal of Medicinal Chemistry; vol. 18; nb. 2; (1975); p. 177 - 182, View in Reaxys 36 of 81
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Concentration of compound required to inhibit binding of amphetamine-3H by Anti-methamphetamine serum upon incubation at 37 degree C for 1 h
Substance RN
970319View in Reaxys
Measurement Parameter
IC50
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Unit
ng
Qualitative value
=
Quantitative value
95
Concomitants: Compound name
[3H]Amphetamine
Concomitants: Compound role
RAD
Faraj; Israili; Kight; Smissman; Pazdernik; Journal of medicinal chemistry; vol. 19; nb. 1; (1976); p. 20 - 25, View in Reaxys 37 of 81
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vivo effect of compound on 30 min light-induced acute retinal degeneration in Abca4-/- Rdh8-/mouse after oral administration of 14 mg/kg dose was determined by measuring the rhodopsin level after light expose; n = 3
Biological Species/NCBI ID
mouse
Cells/Cell Lines
retina cell
Substance RN
970319View in Reaxys
Substance Route of Adm.
oral administration
Qualitative Results
RHODOPSIN LEVELS not calculated
Measurement Parameter
qualitative
Measurement Object
RHODOPSIN LEVELS
Maeda, Akiko; Golczak, Marcin; Chen, Yu; Okano, Kiichiro; Kohno, Hideo; Shiose, Satomi; Ishikawa, Kaede; Harte, William; Palczewska, Grazyna; Maeda, Tadao; Palczewski, Krzysztof; Nature Chemical Biology; vol. 8; nb. 2; (2012); p. 170 - 178, View in Reaxys 38 of 81
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Lethal dose of the compound in Abca4-/- Rdh8-/- mouse after oral administration was determined
Biological Species/NCBI ID
mouse
Substance RN
970319View in Reaxys
Substance Route of Adm.
oral administration
Qualitative Results
Unknown or not determined
Measurement Parameter
qualitative
Measurement Object
LD50
Maeda, Akiko; Golczak, Marcin; Chen, Yu; Okano, Kiichiro; Kohno, Hideo; Shiose, Satomi; Ishikawa, Kaede; Harte, William; Palczewska, Grazyna; Maeda, Tadao; Palczewski, Krzysztof; Nature Chemical Biology; vol. 8; nb. 2; (2012); p. 170 - 178, View in Reaxys 39 of 81
Bioassay Category
In Vivo (Animal models)
Bioassay Details
In vivo effect of compound on 30 min light-induced acute retinal degeneration in Abca4-/- Rdh8-/mouse after oral administration of 14 mg/kg dose was determined by measuring the optical coherence tomography score; n = 3
Biological Species/NCBI ID
mouse
Cells/Cell Lines
retina cell
Substance RN
970319View in Reaxys
Substance Route of Adm.
oral administration
Measurement Parameter
number
Measurement Object
OPTICAL COHERENCE TOMOGRAPHY SCORE
Quantitative value
1
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Maeda, Akiko; Golczak, Marcin; Chen, Yu; Okano, Kiichiro; Kohno, Hideo; Shiose, Satomi; Ishikawa, Kaede; Harte, William; Palczewska, Grazyna; Maeda, Tadao; Palczewski, Krzysztof; Nature Chemical Biology; vol. 8; nb. 2; (2012); p. 170 - 178, View in Reaxys 40 of 81
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Target Name
Sodium-dependent noradrenaline transporter [rat]
Target Synonyms
sodium-dependent noradrenaline transporter
Target, Subunit, Species
Sodium-dependent noradrenaline transporter [rat]
Target Mutant/Chimera Details
Sodium-dependent noradrenaline transporter [rat]:Wild
Target Species (Bioactivity)
rat
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective concentration of the compound required for release of Norepinephrine transporter from rat brain synaptosomes using [3H]MPP+ as radioligand
Biological Species/NCBI ID
rat
Substance RN
970319View in Reaxys
Measurement Parameter
EC50
Unit
nM
Measurement Object
Release of Norepinephrine transporter from rat brain synaptosomes
Qualitative value
=
Quantitative value
39.4
Deviation
6.6
Measurement pX
7.4
Concomitants: Compound name
[3H]MPP
Concomitants: Compound role
RAD
Target Name
5-hydroxytryptamine receptor 2b [human]
Target Synonyms
5-ht-2b; 5-ht2b; 5-hydroxytryptamine receptor 2b; htr2b; serotonin receptor 2b
Target Uniprot ID
p41595
Target PDB ID
4ib4; 4nc3; 5tvn
Target, Subunit, Species
5-hydroxytryptamine receptor 2b [human]
Target Mutant/Chimera Details
5-hydroxytryptamine receptor 2b [human]:Wild
Target Species (Bioactivity)
human
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective concentration of the compound towards human 5-hydroxytryptamine 2B receptor mediated Ca2+ mobilization; Inactive
Biological Species/NCBI ID
human
Substance RN
970319View in Reaxys
Qualitative Results
Inactive
Measurement Parameter
EC50
Qualitative value
NA
Measurement pX
1
Target Name
Sodium-dependent serotonin transporter [rat]
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44 of 81
Target Synonyms
5ht transporter; 5htt; sert; slc6a4; sodium-dependent serotonin transporter; solute carrier family 6 member 4
Target Uniprot ID
p31652
Target, Subunit, Species
Sodium-dependent serotonin transporter [rat]
Target Mutant/Chimera Details
Sodium-dependent serotonin transporter [rat]:Wild
Target Species (Bioactivity)
rat
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective concentration of the compound required for release of Serotonin transporter from rat brain synaptosomes
Biological Species/NCBI ID
rat
Substance RN
970319View in Reaxys
Measurement Parameter
EC50
Unit
nM
Qualitative value
=
Quantitative value
3511
Deviation
253
Measurement pX
5.45
Target Name
Sodium-dependent dopamine transporter [rat]
Target Synonyms
da transporter; dat; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3
Target Uniprot ID
p23977
Target, Subunit, Species
Sodium-dependent dopamine transporter [rat]
Target Mutant/Chimera Details
Sodium-dependent dopamine transporter [rat]:Wild
Target Species (Bioactivity)
rat
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective concentration of the compound required for release of Dopamine transporter from rat brain synaptosomes using [3H]MPP+ as radioligand
Biological Species/NCBI ID
rat
Substance RN
970319View in Reaxys
Measurement Parameter
EC50
Unit
nM
Measurement Object
Eelease of Dopamine transporter from rat brain synaptosomes
Qualitative value
=
Quantitative value
262
Deviation
21
Measurement pX
6.58
Concomitants: Compound name
[3H]MPP
Concomitants: Compound role
RAD
Target Name
5-hydroxytryptamine receptor 2a [human]
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46 of 81
Target Synonyms
5-ht-2; 5-ht-2a; 5-hydroxytryptamine receptor 2a; htr2; htr2a; serotonin receptor 2a
Target Uniprot ID
p28223
Target, Subunit, Species
5-hydroxytryptamine receptor 2a [human]
Target Mutant/Chimera Details
5-hydroxytryptamine receptor 2a [human]:Wild
Target Species (Bioactivity)
human
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective concentration of the compound towards human 5-hydroxytryptamine 2A receptor mediated Ca2+ mobilization; Inactive
Biological Species/NCBI ID
human
Substance RN
970319View in Reaxys
Qualitative Results
Inactive
Measurement Parameter
EC50
Measurement Object
Ca2+ mobilization
Qualitative value
NA
Measurement pX
1
Target Name
5-hydroxytryptamine receptor 2c [human]
Target Synonyms
5-ht-1c; 5-ht-2c; 5-ht1c; 5-ht2c; 5-htr2c; 5-hydroxytryptamine receptor 1c; 5-hydroxytryptamine receptor 2c; htr1c; htr2c; serotonin receptor 2c
Target Uniprot ID
p28335
Target, Subunit, Species
5-hydroxytryptamine receptor 2c [human]
Target Mutant/Chimera Details
5-hydroxytryptamine receptor 2c [human]:Wild
Target Species (Bioactivity)
human
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective concentration of the compound towards human 5-hydroxytryptamine 2C receptor mediated Ca2+ mobilization; Inactive
Biological Species/NCBI ID
human
Substance RN
970319View in Reaxys
Qualitative Results
Inactive
Measurement Parameter
EC50
Measurement Object
Ca2+ mobilization
Qualitative value
NA
Measurement pX
1
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Intravenous lethal dose
Biological Species/NCBI ID
mouse
Substance RN
970319View in Reaxys
Substance Route of Adm.
intravenous administration
Measurement Parameter
LD50
Unit
mg/kg
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Qualitative value
=
Quantitative value
14
Mori; Uemura; Kobayashi; Miyahara; Kozuka; Xenobiotica; vol. 23; nb. 6; (1993); p. 709 - 716, View in Reaxys 47 of 81
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Oral lethal dose
Biological Species/NCBI ID
mouse
Substance RN
970319View in Reaxys
Measurement Parameter
LD50
Unit
mg/kg
Qualitative value
=
Quantitative value
105
Mori; Uemura; Kobayashi; Miyahara; Kozuka; Xenobiotica; vol. 23; nb. 6; (1993); p. 709 - 716, View in Reaxys 48 of 81
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Lowest published toxic dose
Biological Species/NCBI ID
human
Substance RN
970319View in Reaxys
Measurement Parameter
TDLo
Unit
mg/kg
Measurement Object
Lowest published toxic dose
Qualitative value
=
Quantitative value
1.429
Yelnosky; Panasevich; Borrelli; Lawlor; Archives internationales de pharmacodynamie et de thérapie; vol. 178; nb. 1; (1969); p. 62 - 76, View in Reaxys 49 of 81
Target Name
trace amine-associated receptor 1 [human]
Target Synonyms
ta1; taar1; tar-1; tar1; trace amine receptor 1; trace amine-associated receptor 1; trar1
Target Uniprot ID
q96rj0
Target, Subunit, Species
trace amine-associated receptor 1 [human]
Target Mutant/Chimera Details
trace amine-associated receptor 1 [human]:Wild
Target Species (Bioactivity)
human
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective concentration of the compound for activation of human Trace amine-associated receptor 1 in CHO cells expressing Galpha 16 (RDHGA16 cells) measured by calcium flux
Biological Species/NCBI ID
human
Cells/Cell Lines
CHO cell line
Substance RN
970319View in Reaxys
Measurement Parameter
EC50
Unit
nM
Measurement Object
Calcium flux
Qualitative value
=
Quantitative value
5470
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Deviation
1900
Measurement pX
5.26
Lewin, Anita H.; Navarro, Hernan A.; Wayne Mascarella; Bioorganic and Medicinal Chemistry; vol. 16; nb. 15; (2008); p. 7415 - 7423, View in Reaxys 50 of 81
51 of 81
Target Name
Dopamine receptor family
Target Synonyms
dopamine receptor family
Target, Subunit, Species
Dopamine receptor family
Target Mutant/Chimera Details
Dopamine receptor family:Wild
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective concentration of the compound against dopamine receptor mediated release of [3H]-dopamine
Substance RN
970319View in Reaxys
Measurement Parameter
EC50
Unit
nM
Measurement Object
Effective concentration
Qualitative value
=
Quantitative value
262
Deviation
21
Measurement pX
6.58
Target Name
trace amine-associated receptor 1 [human]
Target Synonyms
ta1; taar1; tar-1; tar1; trace amine receptor 1; trace amine-associated receptor 1; trar1
Target Uniprot ID
q96rj0
Target, Subunit, Species
trace amine-associated receptor 1 [human]
Target Mutant/Chimera Details
trace amine-associated receptor 1 [human]:Wild
Target Species (Bioactivity)
human
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Maximum efficacy of the compound for activation of human Trace amine-associated receptor 1 in CHO cells expressing Galpha 16 (RDHGA16 cells) measured by calcium flux at 37 degree C for 1 hour
Biological Species/NCBI ID
human
Cells/Cell Lines
CHO cell line
Substance RN
970319View in Reaxys
Measurement Parameter
Emax
Unit
%
Measurement Object
Calcium flux
Qualitative value
=
Quantitative value
68
Deviation
4
Lewin, Anita H.; Navarro, Hernan A.; Wayne Mascarella; Bioorganic and Medicinal Chemistry; vol. 16; nb. 15; (2008); p. 7415 - 7423, View in Reaxys 52 of 81
Target Name
5-hydroxytryptamine receptor
Target Synonyms
5-ht receptor; 5-hydroxytryptamine receptor; serotonin receptor
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Target, Subunit, Species
5-hydroxytryptamine receptor
Target Mutant/Chimera Details
5-hydroxytryptamine receptor:Wild
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective concentration of the compound against 5-hydroxytryptamine receptor mediated release of [3H]-5-hydroxytryptamine
Substance RN
970319View in Reaxys
Measurement Parameter
EC50
Unit
nM
Measurement Object
[3H]-5-hydroxytryptamine release
Qualitative value
=
Quantitative value
3511
Deviation
253
Measurement pX
5.45
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Tested for its ability to elevate blood pressure in rat when administered for 5 days; Produced marked elevation
Biological Species/NCBI ID
rat
Substance RN
970319View in Reaxys
Measurement Parameter
Activity
Qualitative value
ND
John Krapcho; Annual reports in medicinal chemistry; vol. 5; (1969); p. 13 - 22, View in Reaxys 54 of 81
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Anorectic activity of the compound was determined; Active
Substance RN
970319View in Reaxys
Qualitative Results
Acitve
Measurement Parameter
Activity
Qualitative value
@
George I. Poos; Annual reports in medicinal chemistry; vol. 1; (1965); p. 51 - 58, View in Reaxys 55 of 81
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Compound was tested for reduction in weight in a double blind study; significant weight loss observed
Substance RN
970319View in Reaxys
Measurement Parameter
Activity
Measurement Object
Reduction in weight
Qualitative value
ND
Ann C. Sullivan; Lorraine Cheng; James G. Hamilton; Annual reports in medicinal chemistry; vol. 11; (1976); p. 200 - 209, View in Reaxys 56 of 81
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Compound was tested for anorectic activity in humans; active
Biological Species/NCBI ID
human
Substance RN
970319View in Reaxys
Measurement Parameter
Activity
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Qualitative value
ND
Ann C. Sullivan; Lorraine Cheng; James G. Hamilton; Annual reports in medicinal chemistry; vol. 11; (1976); p. 200 - 209, View in Reaxys 57 of 81
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Tested for its ability to increase blood pressure in dog; Effective
Biological Species/NCBI ID
dog
Substance RN
970319View in Reaxys
Qualitative Results
Effective
Measurement Parameter
Activity
Measurement Object
Increase blood pressure
Qualitative value
@
John Krapcho; Annual reports in medicinal chemistry; vol. 5; (1969); p. 13 - 22, View in Reaxys 58 of 81
Bioassay Category
Metabolism/Transport
Bioassay Details
Amount of the compound in urine after administration to rats was determined
Biological Species/NCBI ID
rat
Substance RN
970319View in Reaxys
Measurement Parameter
amount
Unit
%
Qualitative value
=
Quantitative value
4
George I. Poos; Annual reports in medicinal chemistry; vol. 2; (1966); p. 44 - 47, View in Reaxys 59 of 81
Target Name
Indoleamine 2,3-dioxygenase 1 [human]
Target Synonyms
ido; ido-1; ido1; indo; indoleamine 2,3-dioxygenase 1; indoleamine-pyrrole 2,3-dioxygenase
Target Uniprot ID
p14902
Target PDB ID
2d0t; 2d0u; 4pk5; 4pk6; 4u72; 4u74; 5ek2; 5ek3; 5ek4; 5etw; 5xe1
Target, Subunit, Species
Indoleamine 2,3-dioxygenase 1 [human]
Target Mutant/Chimera Details
Indoleamine 2,3-dioxygenase 1 [human]:Wild
Target Species (Bioactivity)
human
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Enzymology inhibition
Substance RN
970319View in Reaxys
Substance Name
page S6, Name Phentermine
Substance Dose
1000 µM
Measurement Parameter
% Inhibition
Unit
%
Quantitative value
0
Measurement pX
1
Concomitants: Compound RN
86197; 2114647; 506008; 3599847; 84272
Concomitants: Compound name
L-Tryptophan; Triton X100; DMSO; Methylene blue; L-(+)-Ascorbic acid
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Concomitants: Compound role
SUB; COM; SLV; COM; COM
Substance Effect
Anorectic
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
rat
Substance RN
970319View in Reaxys
Substance Name
phentermine
Substance Dose
1 mg
Substance Route of Adm.
oral administration
Measurement Parameter
% Inhibition
Qualitative value
Not active
Measurement pX
1
Patent; PROXIMAGEN LIMITED; RICHARDSON, Peter; CAMPBELL, Bruce; WO2015/1359; (2015); (A1) English, View in Reaxys 61 of 81
Target Name
Muscarinic acetylcholine receptor M1
Target Synonyms
chrm-1; chrm1; muscarinic acetylcholine receptor m1
Target, Subunit, Species
Muscarinic acetylcholine receptor M1
Target Mutant/Chimera Details
Muscarinic acetylcholine receptor M1:Wild
Substance Action on Target
Antagonist
Substance Effect
antagonistic activity
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Antagonistic activity of the compound against Muscarinic acetylcholine receptor M1
Substance RN
970319View in Reaxys
Qualitative Results
Not Published
Measurement Parameter
qualitative
Qualitative value
Not Published
Patent; Brain Seed; Jordan Mechanic; US2007/293481; (A1); (2007), View in Reaxys 62 of 81
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Percent reduction in weight gain of rat upon subcutaneous administration of the compound at a dose of 4 mg/kg along with Telenzepine (0.3 mg/kg)
Biological Species/NCBI ID
rat
Substance RN
970319View in Reaxys
Measurement Parameter
percentage
Unit
%
Measurement Object
Reduction activity
Qualitative value
=
Quantitative value
-3
Patent; Brain Seed; Jordan Mechanic; US2007/293481; (A1); (2007), View in Reaxys 63 of 81
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Percent reduction in weight gain of rat upon subcutaneous administration of the compound at a dose of 4 mg/kg
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Biological Species/NCBI ID
rat
Substance RN
970319View in Reaxys
Measurement Parameter
percentage
Unit
%
Measurement Object
Reduction activity
Qualitative value
=
Quantitative value
-1.1
Patent; Brain Seed; Jordan Mechanic; US2007/293481; (A1); (2007), View in Reaxys 64 of 81
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
obesity
Substance RN
970319View in Reaxys
Substance Name
phentermine
Substance Dose
15 mg
Substance Dosing Regimen
Repeated
Measurement Parameter
AUC (0-tau)
Unit
ng*h/ml
Measurement Object
0 - tau
Quantitative value
2250
Concomitants: Compound RN
5988957
Concomitants: Compound name
2,3:4,5-bis-O-(1-methylethylidene)-α-D-fructopyranose sulfamate
Concomitants: Compound role
ICP
Patent; Vivus, Inc.; Najarian, Thomas; Tam, Peter Y.; Wilson, Leland F.; (16 pag.); US2016/22630; (2016); (A1) English, View in Reaxys 65 of 81
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
obesity
Substance RN
970319View in Reaxys
Substance Name
phentermine
Substance Dose
15 mg
Substance Dosing Regimen
Repeated
Measurement Parameter
AUC (0-96 h)
Unit
ng*h/ml
Measurement Object
0 - tau
Quantitative value
4640
Concomitants: Compound RN
5988957
Concomitants: Compound name
2,3:4,5-bis-O-(1-methylethylidene)-α-D-fructopyranose sulfamate
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Concomitants: Compound role
ICP
Patent; Vivus, Inc.; Najarian, Thomas; Tam, Peter Y.; Wilson, Leland F.; (16 pag.); US2016/22630; (2016); (A1) English, View in Reaxys 66 of 81
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
obesity
Substance RN
970319View in Reaxys
Substance Name
phentermine
Substance Dose
15 mg
Substance Dosing Regimen
Repeated
Measurement Parameter
AUC (0-96 h)
Unit
ng*h/ml
Measurement Object
0-t
Quantitative value
4640
Concomitants: Compound RN
5988957
Concomitants: Compound name
2,3:4,5-bis-O-(1-methylethylidene)-α-D-fructopyranose sulfamate
Concomitants: Compound role
ICP
Patent; Vivus, Inc.; Najarian, Thomas; Tam, Peter Y.; Wilson, Leland F.; (16 pag.); US2016/22630; (2016); (A1) English, View in Reaxys 67 of 81
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
obesity
Substance RN
970319View in Reaxys
Substance Name
phentermine
Substance Dose
15 mg
Substance Dosing Regimen
Repeated
Measurement Parameter
tmax
Unit
h
Quantitative value
4.01
Concomitants: Compound RN
5988957
Concomitants: Compound name
2,3:4,5-bis-O-(1-methylethylidene)-α-D-fructopyranose sulfamate
Concomitants: Compound role
ICP
Patent; Vivus, Inc.; Najarian, Thomas; Tam, Peter Y.; Wilson, Leland F.; (16 pag.); US2016/22630; (2016); (A1) English, View in Reaxys 68 of 81
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
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Population State
obesity
Substance RN
970319View in Reaxys
Substance Name
phentermine
Substance Dose
15 mg
Substance Dosing Regimen
Repeated
Measurement Parameter
t1/2
Unit
h
Quantitative value
23.3
Concomitants: Compound RN
5988957
Concomitants: Compound name
2,3:4,5-bis-O-(1-methylethylidene)-α-D-fructopyranose sulfamate
Concomitants: Compound role
ICP
Patent; Vivus, Inc.; Najarian, Thomas; Tam, Peter Y.; Wilson, Leland F.; (16 pag.); US2016/22630; (2016); (A1) English, View in Reaxys 69 of 81
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
obesity
Substance RN
970319View in Reaxys
Substance Name
phentermine
Substance Dose
15 mg
Substance Dosing Regimen
Repeated
Measurement Parameter
Cl ss/F
Unit
l/h
Quantitative value
7.1
Concomitants: Compound RN
5988957
Concomitants: Compound name
2,3:4,5-bis-O-(1-methylethylidene)-α-D-fructopyranose sulfamate
Concomitants: Compound role
ICP
Patent; Vivus, Inc.; Najarian, Thomas; Tam, Peter Y.; Wilson, Leland F.; (16 pag.); US2016/22630; (2016); (A1) English, View in Reaxys 70 of 81
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
obesity
Substance RN
970319View in Reaxys
Substance Name
phentermine
Substance Dose
15 mg
Substance Dosing Regimen
Repeated
Measurement Parameter
V2/F
Unit
l/h
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Quantitative value
229
Concomitants: Compound RN
5988957
Concomitants: Compound name
2,3:4,5-bis-O-(1-methylethylidene)-α-D-fructopyranose sulfamate
Concomitants: Compound role
ICP
Patent; Vivus, Inc.; Najarian, Thomas; Tam, Peter Y.; Wilson, Leland F.; (16 pag.); US2016/22630; (2016); (A1) English, View in Reaxys 71 of 81
Target Name
Carbonic anhydrase 2 [human]
Target Synonyms
ca-ii; ca2; cac; carbonate dehydratase ii; carbonic anhydrase 2; carbonic anhydrase c; carbonic anhydrase ii
Target Uniprot ID
p00918
Target PDB ID
12ca; 1a42; 1am6; 1avn; 1bn4; 1bnm; 1bnn; 1bnq; 1bnt; 1bnu; 1bnv; 1cah; 1cai; 1caj; 1cak; 1cal; 1cam; 1ccs; 1cct; 1ccu; 1cil; 1cim; 1cin; 1cnb; 1cnj; 1cnk; 1cnw; 1cnx; 1cny; 1cra; 1cva; 1cvf; 1cvh; 1dca; 1dcb; 1eou; 1f2w; 1fr4; 1fr7; 1fsn; 1fsq; 1fsr; 1g0e; 1g0f; 1g48; 1g4j; 1g4o; 1g52; 1g53; 1g54; 1h4n; 1heb; 1hec; 1hed; 1hva; 1i8z; 1i90; 1i9o; 1i9p; 1i9q; 1if4; 1if5; 1if6; 1if7; 1lg5; 1lg6; 1lgd; 1lug; 1lzv; 1moo; 1mua; 1ray; 1raz; 1rza; 1rzb; 1rzc; 1rzd; 1te3; 1teq; 1teu; 1tg3; 1tg9; 1th9; 1thk; 1ugd; 1uge; 1ugf; 1ugg; 1xeg; 1xev; 1xpz; 1ydd; 1yo0; 1yo1; 1yo2; 1z9y; 1ze8; 1zh9; 1zsa; 1zsb; 1zsc; 2abe; 2aw1; 2ax2; 2cbd; 2cbe; 2eu2; 2eu3; 2ez7; 2f14; 2fmg; 2foq; 2fos; 2fou; 2fov; 2gd8; 2geh; 2hl4; 2hnc; 2hoc; 2ili; 2nng; 2nno; 2nns; 2nwz; 2nxr; 2nxs; 2nxt; 2o4z; 2osf; 2osm; 2q1q; 2q38; 2qo8; 2qoa; 2qp6; 2vva; 2weh; 2wej; 2weo; 2x7s; 2x7t; 2x7u; 3b4f; 3ca2; 3caj; 3cyu; 3d8w; 3d92; 3d93; 3d9z; 3dcc; 3dcs; 3dcw; 3dd0; 3dd8; 3dv7; 3eft; 3f4x; 3f8e; 3ffp; 3gz0; 3hfp; 3hkn; 3hs4; 3ibi; 3ibl; 3ibn; 3ibu; 3ieo; 3igp; 3kkx; 3kne; 3koi; 3kok; 3kon; 3ks3; 3m1j; 3m1k; 3m1q; 3m1w; 3m2n; 3m2x; 3m2y; 3m5s; 3m5t; 3m67; 3m96; 3m98; 3mhc; 3mhi; 3mmf; 3mna; 3mnh; 3mni; 3mnj; 3mnk; 3n0n; 3n2p; 3n3j; 3n4b; 3nb5; 3ni5; 3nj9; 3okv; 3oy0; 3oyq; 3oys; 3p3h; 3p3j; 3p44; 3p5l; 3pjj; 3po6; 3pyk; 3qyk; 3r16; 3rj7; 3rld; 3ryj; 3ryv; 3ryx; 3ryy; 3ryz; 3rz8; 3s71; 3s72; 3s73; 3s74; 3s75; 3s76; 3sap; 3sax; 3sbh; 3sbi; 3t5u; 3t5z; 3tmj; 3tvn; 3tvo; 3u3a; 3u45; 3u47; 3u7c; 3v3h; 3v3i; 3v3j; 3v5g; 3v7x; 3vbd; 3zp9; 4cac; 4cq0; 4dz7; 4dz9; 4e3d; 4e3f; 4e5q; 4fik; 4fl7; 4fpt; 4frc; 4fu5; 4fvn; 4hew; 4hey; 4hez; 4hf3; 4ht0; 4idr; 4ilx; 4jsa; 4jss; 4jsw; 4jsz; 4k0s; 4k0t; 4kni; 4knj; 4kuv; 4kuw; 4kuy; 4kv0; 4l5u; 4m2r; 4m2u; 4m2v; 4m2w; 4mdg; 4mdl; 4mdm; 4n0x; 4n16; 4pq7; 4pxx; 4pyx; 4pyy; 4q09; 4q49; 4q6d; 4q6e; 4q78; 4q7p; 4q7s; 4q87; 4q8x; 4q8y; 4q8z; 4q90; 4q99; 4q9y; 4qk2; 4qk3; 4qsa; 4qsb; 4qsi; 4qtl; 4rfc; 4rfd; 4rh2; 4riu; 4riv; 4rn4; 4rux; 4xe1; 4y0j; 4ygj; 4ygk; 4ygl; 4ygn; 4yxu; 4yyt; 4z0q; 4z1e; 4z1j; 4z1k; 4zwy; 4zwz; 4zx0; 4zx1; 5a6h; 5amd; 5amg; 5brw; 5byi; 5c8i; 5ca2; 5cac; 5cjl; 5dsj; 5dsk; 5dsl; 5dsm; 5dsn; 5dso; 5e2k; 5e2r; 5e2s; 5eh5; 5eh7; 5eh8; 5ehe; 5ekj; 5ekm; 5eoi; 5fdc; 5fdi; 5flo; 5fng; 5fnh; 5fni; 5fnj; 5fnk; 5fnl; 5g0c; 5j8z; 5jdv; 5je7; 5jeg; 5jeh; 5jep; 5jgt; 5jmz; 5jn1; 5jn3; 5jn7; 5jq0; 5n0d; 5n0e; 5sz0; 5sz1; 5sz2; 5sz3; 5th4; 5thi; 5thj; 5thn; 5ti0; 6ca2; 7ca2
Target, Subunit, Species
Carbonic anhydrase 2 [human]
Target Mutant/Chimera Details
Carbonic anhydrase 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Activator
Bioassay Category
In Vitro (Efficacy)
Cells/Cell Lines
cell line
Substance RN
970319View in Reaxys
Substance Name
phentermine
Measurement Parameter
Ka
Unit
μM
Qualitative value
>
Quantitative value
150
Measurement pX
1
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Angeli, Andrea; Vaiano, Fabio; Mari, Francesco; Bertol, Elisabetta; Supuran, Claudiu T.; Journal of Enzyme Inhibition and Medicinal Chemistry; vol. 32; nb. 1; (2017); p. 1253 - 1259, View in Reaxys 72 of 81
Target Name
Carbonic anhydrase 1 [human]
Target Synonyms
ca-i; ca1; cab; carbonate dehydratase i; carbonic anhydrase 1; carbonic anhydrase b; carbonic anhydrase i
Target Uniprot ID
p00915
Target PDB ID
1azm; 1bzm; 1crm; 1czm; 1hcb; 1hug; 1huh; 1j9w; 1jv0; 2cab; 2foy; 2fw4; 2it4; 2nmx; 2nn1; 2nn7; 3lxe; 3w6h; 3w6i; 4wr7; 4wup; 4wuq; 5e2m
Target, Subunit, Species
Carbonic anhydrase 1 [human]
Target Mutant/Chimera Details
Carbonic anhydrase 1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Activator
Bioassay Category
In Vitro (Efficacy)
Cells/Cell Lines
cell line
Substance RN
970319View in Reaxys
Substance Name
phentermine
Measurement Parameter
Ka
Unit
μM
Qualitative value
>
Quantitative value
150
Measurement pX
1
Angeli, Andrea; Vaiano, Fabio; Mari, Francesco; Bertol, Elisabetta; Supuran, Claudiu T.; Journal of Enzyme Inhibition and Medicinal Chemistry; vol. 32; nb. 1; (2017); p. 1253 - 1259, View in Reaxys 73 of 81
Target Name
Carbonic anhydrase 4 [human]
Target Synonyms
ca-iv; ca4; carbonate dehydratase iv; carbonic anhydrase 4; carbonic anhydrase iv
Target Uniprot ID
p22748
Target PDB ID
1znc; 3f7b; 3f7u; 3fw3; 5ipz; 5jn8; 5jn9; 5jna; 5jnc
Target, Subunit, Species
Carbonic anhydrase 4 [human]
Target Mutant/Chimera Details
Carbonic anhydrase 4 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Activator
Bioassay Category
In Vitro (Efficacy)
Cells/Cell Lines
cell line
Substance RN
970319View in Reaxys
Substance Name
phentermine
Measurement Parameter
Ka
Unit
μM
Quantitative value
0.074
Measurement pX
7.13
Angeli, Andrea; Vaiano, Fabio; Mari, Francesco; Bertol, Elisabetta; Supuran, Claudiu T.; Journal of Enzyme Inhibition and Medicinal Chemistry; vol. 32; nb. 1; (2017); p. 1253 - 1259, View in Reaxys
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74 of 81
Target Name
Carbonic anhydrase 7 [human]
Target Synonyms
ca-vii; ca7; carbonate dehydratase vii; carbonic anhydrase 7; carbonic anhydrase vii
Target Uniprot ID
p43166
Target PDB ID
3mdz; 3ml5
Target, Subunit, Species
Carbonic anhydrase 7 [human]
Target Mutant/Chimera Details
Carbonic anhydrase 7 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Activator
Bioassay Category
In Vitro (Efficacy)
Cells/Cell Lines
cell line
Substance RN
970319View in Reaxys
Substance Name
phentermine
Measurement Parameter
Ka
Unit
μM
Quantitative value
0.89
Measurement pX
6.05
Angeli, Andrea; Vaiano, Fabio; Mari, Francesco; Bertol, Elisabetta; Supuran, Claudiu T.; Journal of Enzyme Inhibition and Medicinal Chemistry; vol. 32; nb. 1; (2017); p. 1253 - 1259, View in Reaxys 75 of 81
Target Name
Carbonic anhydrase 13 [human]
Target Synonyms
ca-xiii; ca13; carbonate dehydratase xiii; carbonic anhydrase 13; carbonic anhydrase xiii
Target Uniprot ID
q8n1q1
Target PDB ID
3czv; 3d0n; 3da2; 4hu1; 4knm; 4knn; 4qiz; 4qjp; 4qjx; 4qsj; 5e2n
Target, Subunit, Species
Carbonic anhydrase 13 [human]
Target Mutant/Chimera Details
Carbonic anhydrase 13 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Activator
Bioassay Category
In Vitro (Efficacy)
Cells/Cell Lines
cell line
Substance RN
970319View in Reaxys
Substance Name
phentermine
Measurement Parameter
Ka
Unit
μM
Quantitative value
54.2
Measurement pX
4.27
Angeli, Andrea; Vaiano, Fabio; Mari, Francesco; Bertol, Elisabetta; Supuran, Claudiu T.; Journal of Enzyme Inhibition and Medicinal Chemistry; vol. 32; nb. 1; (2017); p. 1253 - 1259, View in Reaxys 76 of 81
Target Name
Carbonic anhydrase 12 [human]
Target Synonyms
ca-xii; ca12; carbonate dehydratase xii; carbonic anhydrase 12; carbonic anhydrase xii; tumor antigen hom-rcc-3.1.3
Target Uniprot ID
o43570
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Target PDB ID
1jcz; 1jd0; 4ht2; 4kp5; 4kp8; 4q0l; 4qj0; 4qjo; 4qjw; 4ww8
Target, Subunit, Species
Carbonic anhydrase 12 [human]
Target Mutant/Chimera Details
Carbonic anhydrase 12 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Activator
Bioassay Category
In Vitro (Efficacy)
Cells/Cell Lines
cell line
Substance RN
970319View in Reaxys
Substance Name
phentermine
Measurement Parameter
Ka
Unit
μM
Quantitative value
12.7
Measurement pX
4.9
Angeli, Andrea; Vaiano, Fabio; Mari, Francesco; Bertol, Elisabetta; Supuran, Claudiu T.; Journal of Enzyme Inhibition and Medicinal Chemistry; vol. 32; nb. 1; (2017); p. 1253 - 1259, View in Reaxys 77 of 81
Target Name
Carbonic anhydrase 14 [human]
Target Synonyms
ca-xiv; ca14; carbonate dehydratase xiv; carbonic anhydrase 14; carbonic anhydrase xiv
Target Uniprot ID
q9ulx7
Target PDB ID
4lu3; 5cjf
Target, Subunit, Species
Carbonic anhydrase 14 [human]
Target Mutant/Chimera Details
Carbonic anhydrase 14 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Activator
Bioassay Category
In Vitro (Efficacy)
Cells/Cell Lines
cell line
Substance RN
970319View in Reaxys
Substance Name
phentermine
Measurement Parameter
Ka
Unit
μM
Quantitative value
12.7
Measurement pX
4.9
Angeli, Andrea; Vaiano, Fabio; Mari, Francesco; Bertol, Elisabetta; Supuran, Claudiu T.; Journal of Enzyme Inhibition and Medicinal Chemistry; vol. 32; nb. 1; (2017); p. 1253 - 1259, View in Reaxys 78 of 81
Target Name
Carbonic anhydrase 5A, mitochondrial [human]
Target Synonyms
ca-va; ca5; ca5a; carbonate dehydratase va; carbonic anhydrase 5a, mitochondrial; carbonic anhydrase va
Target Uniprot ID
p35218
Target, Subunit, Species
Carbonic anhydrase 5A, mitochondrial [human]
Target Mutant/Chimera Details
Carbonic anhydrase 5A, mitochondrial [human]:Wild
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Target Species (Bioactivity)
human
Substance Action on Target
Activator
Bioassay Category
In Vitro (Efficacy)
Cells/Cell Lines
cell line
Substance RN
970319View in Reaxys
Substance Name
phentermine
Measurement Parameter
Ka
Unit
μM
Quantitative value
0.53
Measurement pX
6.28
Angeli, Andrea; Vaiano, Fabio; Mari, Francesco; Bertol, Elisabetta; Supuran, Claudiu T.; Journal of Enzyme Inhibition and Medicinal Chemistry; vol. 32; nb. 1; (2017); p. 1253 - 1259, View in Reaxys 79 of 81
Target Name
Carbonic anhydrase 5B, mitochondrial [human]
Target Synonyms
ca-vb; ca5b; carbonate dehydratase vb; carbonic anhydrase 5b, mitochondrial; carbonic anhydrase vb
Target Uniprot ID
q9y2d0
Target, Subunit, Species
Carbonic anhydrase 5B, mitochondrial [human]
Target Mutant/Chimera Details
Carbonic anhydrase 5B, mitochondrial [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Activator
Bioassay Category
In Vitro (Efficacy)
Cells/Cell Lines
cell line
Substance RN
970319View in Reaxys
Substance Name
phentermine
Measurement Parameter
Ka
Unit
μM
Quantitative value
0.62
Measurement pX
6.21
Angeli, Andrea; Vaiano, Fabio; Mari, Francesco; Bertol, Elisabetta; Supuran, Claudiu T.; Journal of Enzyme Inhibition and Medicinal Chemistry; vol. 32; nb. 1; (2017); p. 1253 - 1259, View in Reaxys 80 of 81
Target Name
Carbonic anhydrase 6 [human]
Target Synonyms
ca-vi; ca6; carbonate dehydratase vi; carbonic anhydrase 6; carbonic anhydrase vi; salivary carbonic anhydrase; secreted carbonic anhydrase
Target Uniprot ID
p23280
Target PDB ID
3fe4
Target, Subunit, Species
Carbonic anhydrase 6 [human]
Target Mutant/Chimera Details
Carbonic anhydrase 6 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Activator
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Bioassay Category
In Vitro (Efficacy)
Cells/Cell Lines
cell line
Substance RN
970319View in Reaxys
Substance Name
phentermine
Measurement Parameter
Ka
Unit
μM
Qualitative value
>
Quantitative value
150
Measurement pX
1
Angeli, Andrea; Vaiano, Fabio; Mari, Francesco; Bertol, Elisabetta; Supuran, Claudiu T.; Journal of Enzyme Inhibition and Medicinal Chemistry; vol. 32; nb. 1; (2017); p. 1253 - 1259, View in Reaxys 81 of 81
Target Name
Carbonic anhydrase 9 [human]
Target Synonyms
ca-ix; ca9; caix; carbonate dehydratase ix; carbonic anhydrase 9; carbonic anhydrase ix; g250; membrane antigen mn; mn; p54/58n; pmw1; rcc-associated antigen g250; renal cell carcinoma-associated antigen g250
Target Uniprot ID
q16790
Target PDB ID
2hkf; 3iai; 5dvx; 5fl4; 5fl5; 5fl6
Target, Subunit, Species
Carbonic anhydrase 9 [human]
Target Mutant/Chimera Details
Carbonic anhydrase 9 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Activator
Bioassay Category
In Vitro (Efficacy)
Cells/Cell Lines
cell line
Substance RN
970319View in Reaxys
Substance Name
phentermine
Measurement Parameter
Ka
Unit
μM
Quantitative value
34.6
Measurement pX
4.46
Angeli, Andrea; Vaiano, Fabio; Mari, Francesco; Bertol, Elisabetta; Supuran, Claudiu T.; Journal of Enzyme Inhibition and Medicinal Chemistry; vol. 32; nb. 1; (2017); p. 1253 - 1259, View in Reaxys
Reaxys ID 3912379 View in Reaxys
2/6 CAS Registry Number: 1197-21-3 Chemical Name: phentermine hydrochloride; α,α-dimethylphenethylamine hydrochloride; Phentermine hydrochloride; 1,1-dimethyl-2-phenyl-ethylamine hydrochloride; 1,1-Dimethyl-2-phenylethylamine hydrochloride; 1,1-dimethyl-2-phenylethylamine HCl; phentermine HCl Linear Structure Formula: C6H5CH2C(CH3)2NH3 (1+)*Cl(1-)=C H CH C(CH )2NH Cl 6 5 2 3 3 Molecular Formula: C10H16N*Cl Molecular Weight: 185.697 Type of Substance: isocyclic InChI Key: NCAIGTHBQTXTLR-UHFFFAOYSA-N
H 2N Cl
H
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Note: Substance Label (7) Label References Intermediate 75
Patent; GLAXOSMITHKLINE LLC; AXTEN, Jeffrey, Michael; BLACKLEDGE, Charles, William; BRADY, Gerald, Patrick; FENG, Yanhoug, G.; GRANT, Seth, W.; MEDINA, Jesus, Rahul; MILLER, William, H.; ROMERIL, Stuart, P.; WO2010/59658; (2010); (A1) English, View in Reaxys
Phent
Li, Su-Min; Campbell, Bettye L.; Katz, Jonathan L.; Journal of Pharmacology and Experimental Therapeutics; vol. 317; nb. 3; (2006); p. 1088 - 1096, View in Reaxys
14
Shao, Ning; Wang, Cheng; Huang, Xianhai; Xiao, Dong; Palani, Anandan; Aslanian, Robert; Shih, Neng-Yang; Tetrahedron Letters; vol. 47; nb. 38; (2006); p. 6743 - 6746, View in Reaxys
phen
Zolkowska, Dorota; Rothman, Richard B.; Baumann, Michael H.; Journal of Pharmacology and Experimental Therapeutics; vol. 318; nb. 2; (2006); p. 604 - 610, View in Reaxys
13
Katritzky, Alan R.; Cui, Xilin; Long, Qiuhe; Yang, Baozhen; Wilcox, Allan L.; Zhang, Yong-Kang; Organic Preparations and Procedures International; vol. 32; nb. 2; (2000); p. 175 - 183, View in Reaxys
3d
Jirgensons; Kauss; Kalvinsh; Gold; Synthesis; nb. 12; (2000); p. 1709 - 1712, View in Reaxys
2e
Gajda; Koziara; Napieraj; Sikora; Zwierzak; Polish Journal of Chemistry; vol. 74; nb. 10; (2000); p. 1385 - 1387, View in Reaxys
Patent-Specific Data (3) Location in Patent References Page/Page column
Patent; King, Clifford Riley; Bristol, David W.; English, Michael L.; US2014/178480; (2014); (A1) English, View in Reaxys
Claim
Patent; Louisiana State University Medical Center Foundation; US5795880; (1998); (A) English, View in Reaxys; Patent; General Mills, Inc.; US2002/44968; (2002); (A1) English, View in Reaxys; Patent; The Procter and Gamble Company; US5614178; (1997); (A) English, View in Reaxys Patent; G.D. Searle and Co.; US6337398; (2002); (B1) English, View in Reaxys
Druglikeness (1) 1 of 1
LogP
2.691
H Bond Donors
1
H Bond Acceptors
1
Rotatable Bonds
2
TPSA
26.02
Lipinski Number
4
Veber Number
2
Highest Clinical Phase (1) Highest Clinical Phase Withdrawn Melting Point (5) 1 of 5
Melting Point [°C]
196 - 200
Jirgensons; Kauss; Kalvinsh; Gold; Synthesis; nb. 12; (2000); p. 1709 - 1712, View in Reaxys 2 of 5
Melting Point [°C]
200 - 202
Dube, Michael F.; Timberlake, Jack W.; Tetrahedron; vol. 36; (1980); p. 1753 - 1756, View in Reaxys 3 of 5
Melting Point [°C]
203
Comment (Melting Point)
Decomposition.
Girault-Vexlearschi; Bulletin de la Societe Chimique de France; (1956); p. 589,596, View in Reaxys 4 of 5
Melting Point [°C]
199 - 200
Solvent (Melting Point)
propan-2-ol; diisopropyl ether
Zenitz; Macks; Moore; Journal of the American Chemical Society; vol. 70; (1948); p. 955, View in Reaxys 5 of 5
Melting Point [°C]
198 - 198.5
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Ritter; Kalish; Journal of the American Chemical Society; vol. 70; (1948); p. 4048; Organic Syntheses; vol. 44; (1964); p. 44,45, View in Reaxys Crystal Phase (1) Description (Crystal Phase)
References
Crystal habit
Jordan; Journal of Pharmaceutical Sciences; vol. 82; nb. 12; (1993); p. 1269 - 1271, View in Reaxys
Crystal Property Description (3) Colour & Other Location Properties
References
white
Page/Page column 158
Patent; GLAXOSMITHKLINE LLC; AXTEN, Jeffrey, Michael; BLACKLEDGE, Charles, William; BRADY, Gerald, Patrick; FENG, Yanhoug, G.; GRANT, Seth, W.; MEDINA, Jesus, Rahul; MILLER, William, H.; ROMERIL, Stuart, P.; WO2010/59658; (2010); (A1) English, View in Reaxys
white
Page/Page column 115
Patent; GLAXOSMITHKLINE LLC; AXTEN, Jeffrey, Michael; BRADY, Gerald, Patrick, Jr.; GALLAGHER, Timothy, Francis; HEERDING, Dirk, A.; MEDINA, Jesus, Raul; ROMERIL, Stuart, Paul; WO2010/120854; (2010); (A1) English, View in Reaxys
white
Page/Page column 16
Patent; Andersen, Denise Lyn; Chang, Catherine H.; Falsey, James R.; Frohn, Michael J.; Hong, Fang-Tsao; Liao, Hongyu; Liu, Longbin; Lopez, Patricia; Retz, Daniel Martin; Rishton, Gilbert M.; Rzasa, Robert M.; Siegmund, Aaron; Tadesse, Seifu; Tamayo, Nuria; Tegley, Christopher M.; US2006/69110; (2006); (A1) English, View in Reaxys
Optics (2) Description (Optics)
References
Crystal refractive indices
Jordan; Journal of Pharmaceutical Sciences; vol. 82; nb. 12; (1993); p. 1269 - 1271, View in Reaxys
Natural birefringence
Jordan; Journal of Pharmaceutical Sciences; vol. 82; nb. 12; (1993); p. 1269 - 1271, View in Reaxys
Solubility (MCS) (1) 1 of 1
Location
Paragraph 0212-0218
Comment (Solubility (MCS))
phentermine hydrochloride was completely soluble at pH 4.5 and pH 7.0
Patent; King, Clifford Riley; Bristol, David W.; English, Michael L.; US2014/178480; (2014); (A1) English, View in Reaxys NMR Spectroscopy (4) 1 of 4
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectroscopy)
CDCl3
Frequency (NMR Spectro- 200 scopy) [MHz] Jirgensons; Kauss; Kalvinsh; Gold; Synthesis; nb. 12; (2000); p. 1709 - 1712, View in Reaxys 2 of 4
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
13C
Solvents (NMR Spectroscopy)
CDCl3
Frequency (NMR Spectro- 50 scopy) [MHz] Jirgensons; Kauss; Kalvinsh; Gold; Synthesis; nb. 12; (2000); p. 1709 - 1712, View in Reaxys 3 of 4
Description (NMR Spectroscopy)
Chemical shifts
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Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectroscopy)
D2O
Frequency (NMR Spectro- 250 scopy) [MHz] Gajda; Koziara; Napieraj; Sikora; Zwierzak; Polish Journal of Chemistry; vol. 74; nb. 10; (2000); p. 1385 - 1387, View in Reaxys 4 of 4
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectroscopy)
D2O
Koziara, Anna; Osowska-Pacewicka, Krystyna; Zawadzki, Stefan; Zwierzak, Andrzej; Synthesis; nb. 5; (1987); p. 487 489, View in Reaxys IR Spectroscopy (2) 1 of 2
Description (IR Spectroscopy)
Bands
Solvent (IR Spectroscopy)
KBr
Gajda; Koziara; Napieraj; Sikora; Zwierzak; Polish Journal of Chemistry; vol. 74; nb. 10; (2000); p. 1385 - 1387, View in Reaxys 2 of 2
Description (IR Spectroscopy)
Bands
Solvent (IR Spectroscopy)
KBr
Comment (IR Spectroscopy)
2960 - 990 cm**(-1)
Koziara, Anna; Osowska-Pacewicka, Krystyna; Zawadzki, Stefan; Zwierzak, Andrzej; Synthesis; nb. 5; (1987); p. 487 489, View in Reaxys Mass Spectrometry (2) Description (Mass Location Spectrometry)
References
LCMS (Liquid chromatography mass spectrometry); ESI (Electrospray ionisation)
Page/Page column 158
Patent; GLAXOSMITHKLINE LLC; AXTEN, Jeffrey, Michael; BLACKLEDGE, Charles, William; BRADY, Gerald, Patrick; FENG, Yanhoug, G.; GRANT, Seth, W.; MEDINA, Jesus, Rahul; MILLER, William, H.; ROMERIL, Stuart, P.; WO2010/59658; (2010); (A1) English, View in Reaxys
LCMS (Liquid chromatography mass spectrometry); ESI (Electrospray ionisation)
Page/Page column 115
Patent; GLAXOSMITHKLINE LLC; AXTEN, Jeffrey, Michael; BRADY, Gerald, Patrick, Jr.; GALLAGHER, Timothy, Francis; HEERDING, Dirk, A.; MEDINA, Jesus, Raul; ROMERIL, Stuart, Paul; WO2010/120854; (2010); (A1) English, View in Reaxys
Use (1) Use Pattern
References
weight-control
Patent; ALPEX PHARMA S.A.; US2008/206327; (2008); (A1) English, View in Reaxys
Medchem (83) 1 of 83
Target Name
Amine oxidase [flavin-containing] A [rat]
Target Synonyms
amine oxidase; mao-a; maoa; monoamine oxidase type a
Target Uniprot ID
p21396
Target, Subunit, Species
Amine oxidase [flavin-containing] A [rat]
Target Mutant/Chimera Details
Amine oxidase [flavin-containing] A [rat]:Wild
Target Species (Bioactivity)
rat
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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2 of 83
Target Transfection
Non Transfected
Bioassay Category
Metabolism/Transport
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
lung
Cell Fraction
Homogenate
Substance RN
3912379View in Reaxys
Substance Name
Phentermine HCl
Measurement Parameter
Ki (inhibition constant)
Unit
µM
Quantitative value
85
Deviation
10
Measurement pX
4.07
Metabolite RN
1453495
Metabolite name
5-hydroxyindole-3-acetaldehyde
Concomitants: Compound RN
3886526
Concomitants: Compound name
[14C]-5-HT creatinine sulfate
Concomitants: Compound role
SUB
Target Name
Amine oxidase [flavin-containing] A [rat]
Target Synonyms
amine oxidase; mao-a; maoa; monoamine oxidase type a
Target Uniprot ID
p21396
Target, Subunit, Species
Amine oxidase [flavin-containing] A [rat]
Target Mutant/Chimera Details
Amine oxidase [flavin-containing] A [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
Metabolism/Transport
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
liver
Cell Fraction
Homogenate
Substance RN
3912379View in Reaxys
Substance Name
Phentermine HCl
Measurement Parameter
Ki (inhibition constant)
Unit
µM
Quantitative value
85
Deviation
4
Measurement pX
4.07
Metabolite RN
1453495
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
61/98
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3 of 83
4 of 83
Metabolite name
5-hydroxyindole-3-acetaldehyde
Concomitants: Compound RN
3886526
Concomitants: Compound name
[14C]-5-HT creatinine sulfate
Concomitants: Compound role
SUB
Target Name
Amine oxidase [flavin-containing] A [rat]
Target Synonyms
amine oxidase; mao-a; maoa; monoamine oxidase type a
Target Uniprot ID
p21396
Target, Subunit, Species
Amine oxidase [flavin-containing] A [rat]
Target Mutant/Chimera Details
Amine oxidase [flavin-containing] A [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
Metabolism/Transport
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain
Cell Fraction
Homogenate
Substance RN
3912379View in Reaxys
Substance Name
Phentermine HCl
Measurement Parameter
Ki (inhibition constant)
Unit
µM
Quantitative value
88
Deviation
9
Measurement pX
4.06
Metabolite RN
1453495
Metabolite name
5-hydroxyindole-3-acetaldehyde
Concomitants: Compound RN
3886526
Concomitants: Compound name
[14C]-5-HT creatinine sulfate
Concomitants: Compound role
SUB
Target Name
Amine oxidase [flavin-containing] A [rat]
Target Synonyms
amine oxidase; mao-a; maoa; monoamine oxidase type a
Target Uniprot ID
p21396
Target, Subunit, Species
Amine oxidase [flavin-containing] A [rat]
Target Mutant/Chimera Details
Amine oxidase [flavin-containing] A [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
Metabolism/Transport
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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5 of 83
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
lung
Cell Fraction
Homogenate
Substance RN
3912379View in Reaxys
Substance Name
Phentermine HCl
Measurement Parameter
Ki (inhibition constant)
Unit
µM
Quantitative value
326
Deviation
43
Measurement pX
3.49
Metabolite RN
505944
Metabolite name
Ethanolamine
Concomitants: Compound RN
3624163
Concomitants: Compound name
[14C]-beta-Phenylethylamine hydrochloride
Concomitants: Compound role
SUB
Target Name
Amine oxidase [flavin-containing] A [rat]
Target Synonyms
amine oxidase; mao-a; maoa; monoamine oxidase type a
Target Uniprot ID
p21396
Target, Subunit, Species
Amine oxidase [flavin-containing] A [rat]
Target Mutant/Chimera Details
Amine oxidase [flavin-containing] A [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
Metabolism/Transport
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
liver
Cell Fraction
Homogenate
Substance RN
3912379View in Reaxys
Substance Name
Phentermine HCl
Measurement Parameter
Ki (inhibition constant)
Unit
µM
Quantitative value
416
Deviation
57
Measurement pX
3.38
Metabolite RN
505944
Metabolite name
Ethanolamine
Concomitants: Compound RN
3624163
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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6 of 83
7 of 83
Concomitants: Compound name
[14C]-beta-Phenylethylamine hydrochloride
Concomitants: Compound role
SUB
Target Name
Amine oxidase [flavin-containing] A [rat]
Target Synonyms
amine oxidase; mao-a; maoa; monoamine oxidase type a
Target Uniprot ID
p21396
Target, Subunit, Species
Amine oxidase [flavin-containing] A [rat]
Target Mutant/Chimera Details
Amine oxidase [flavin-containing] A [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
Metabolism/Transport
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain
Cell Fraction
Homogenate
Substance RN
3912379View in Reaxys
Substance Name
Phentermine HCl
Measurement Parameter
Ki (inhibition constant)
Unit
µM
Quantitative value
310
Deviation
90
Measurement pX
3.51
Metabolite RN
505944
Metabolite name
Ethanolamine
Concomitants: Compound RN
3624163
Concomitants: Compound name
[14C]-beta-Phenylethylamine hydrochloride
Concomitants: Compound role
SUB
Target Name
Amine oxidase [flavin-containing] A [rat]
Target Synonyms
amine oxidase; mao-a; maoa; monoamine oxidase type a
Target Uniprot ID
p21396
Target, Subunit, Species
Amine oxidase [flavin-containing] A [rat]
Target Mutant/Chimera Details
Amine oxidase [flavin-containing] A [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
Metabolism/Transport
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
Sprague Dawley rat
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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8 of 83
Organs/Tissues
liver
Cell Fraction
Homogenate
Substance RN
3912379View in Reaxys
Substance Name
Phentermine HCl
Substance Dose
0.0750000 mM
Measurement Parameter
% Inhibition
Unit
%
Quantitative value
0.89
Measurement pX
1
Metabolite RN
1453495
Metabolite name
5-hydroxyindole-3-acetaldehyde
Concomitants: Compound RN
3886526
Concomitants: Compound name
[14C]-5-HT creatinine sulfate
Concomitants: Compound role
SUB
Target Name
Amine oxidase [flavin-containing] A [rat]
Target Synonyms
amine oxidase; mao-a; maoa; monoamine oxidase type a
Target Uniprot ID
p21396
Target, Subunit, Species
Amine oxidase [flavin-containing] A [rat]
Target Mutant/Chimera Details
Amine oxidase [flavin-containing] A [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
Metabolism/Transport
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
liver
Cell Fraction
Homogenate
Substance RN
3912379View in Reaxys
Substance Name
Phentermine HCl
Substance Dose
0.130000 mM
Measurement Parameter
% Inhibition
Unit
%
Quantitative value
22
Measurement pX
1
Metabolite RN
1453495
Metabolite name
5-hydroxyindole-3-acetaldehyde
Concomitants: Compound RN
3886526
Concomitants: Compound name
[14C]-5-HT creatinine sulfate
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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9 of 83
10 of 83
Concomitants: Compound role
SUB
Target Name
Amine oxidase [flavin-containing] A [rat]
Target Synonyms
amine oxidase; mao-a; maoa; monoamine oxidase type a
Target Uniprot ID
p21396
Target, Subunit, Species
Amine oxidase [flavin-containing] A [rat]
Target Mutant/Chimera Details
Amine oxidase [flavin-containing] A [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
Metabolism/Transport
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
liver
Cell Fraction
Homogenate
Substance RN
3912379View in Reaxys
Substance Name
Phentermine HCl
Substance Dose
320 µM
Measurement Parameter
% Inhibition
Unit
%
Quantitative value
87
Measurement pX
4.32
Metabolite RN
1453495
Metabolite name
5-hydroxyindole-3-acetaldehyde
Concomitants: Compound RN
3886526
Concomitants: Compound name
[14C]-5-HT creatinine sulfate
Concomitants: Compound role
SUB
Target Name
Amine oxidase [flavin-containing] A [rat]
Target Synonyms
amine oxidase; mao-a; maoa; monoamine oxidase type a
Target Uniprot ID
p21396
Target, Subunit, Species
Amine oxidase [flavin-containing] A [rat]
Target Mutant/Chimera Details
Amine oxidase [flavin-containing] A [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
Metabolism/Transport
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
liver
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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11 of 83
12 of 83
Cell Fraction
Homogenate
Substance RN
3912379View in Reaxys
Substance Name
Phentermine HCl
Substance Dose
320 µM
Measurement Parameter
% Inhibition
Unit
%
Quantitative value
489
Measurement pX
4.77
Metabolite RN
505944
Metabolite name
Ethanolamine
Concomitants: Compound RN
3624163
Concomitants: Compound name
[14C]-beta-Phenylethylamine hydrochloride
Concomitants: Compound role
SUB
Target Name
Amine oxidase [flavin-containing] B
Target Synonyms
amine oxidase; mao-b; maob; monoamine oxidase type b
Target, Subunit, Species
Amine oxidase [flavin-containing] B
Target Mutant/Chimera Details
Amine oxidase [flavin-containing] B:Wild
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |enzyme; inhib. of Bioassay : MAO B: monoamine oxidase B; oxidation was monitored at 250 nm; further investigations using preincubation with title comp. for >= 15 min before addition of MAO B recombinant human liver MAO B was incubated in 50 mmol/l potassium phosphate pH 7.5, 0.5 percent (w/v) Triton X-100 at 25 deg C in presence of title comp.; MAO B-catalyzed oxidation of benzylamine was determined; spectrophotometric assay
Biological Species/NCBI ID
human
Substance RN
3912379View in Reaxys
Substance Name
70808
Substance Dose
1000 µM
Measurement Parameter
Ki (inhibition constant)
Unit
µM
Quantitative value
375
Measurement pX
3.43
Target Name
Amine oxidase [flavin-containing] A
Target Synonyms
amine oxidase; mao-a; maoa; monoamine oxidase type a
Target, Subunit, Species
Amine oxidase [flavin-containing] A
Target Mutant/Chimera Details
Amine oxidase [flavin-containing] A:Wild
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Bioassay Details
Effect : |enzyme; inhib. of Bioassay : MAO A: monoamine oxidase A; oxidation was monitored at 243 nm; further investigations using preincubation with title comp. for >= 15 min before addition of MAO A recombinant human liver MAO A incubated in 50 mmol/l potassium phosphate, pH 7.5, 0.5 percent (w/v) Triton X-100 at 25 deg C in presence of title comp.; MAO A-catalyzed oxidation of p-CF3-benzylamine was determined; spectrophotometric assay
Biological Species/NCBI ID
human
Substance RN
3912379View in Reaxys
Substance Name
70808
Substance Dose
1000 µM
Measurement Parameter
Ki (inhibition constant)
Unit
µM
Quantitative value
498
Measurement pX
3.3
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cmax
Unit
ng/mL
Quantitative value
219
Metabolite RN
7623052; 7623209
Metabolite name
M2; M1
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 14 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
AUC (0-24 h)
Unit
ng.h/mL
Quantitative value
3834
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Metabolite RN
7623052; 7623209
Metabolite name
M2; M1
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 15 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
tmax
Unit
hour
Quantitative value
3.36
Metabolite RN
7623052; 7623209
Metabolite name
M2; M1
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 16 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
t1/2 el
Unit
hour
Quantitative value
23.5
Metabolite RN
7623052; 7623209
Metabolite name
M2; M1
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 17 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cmin
Unit
ng/mL
Quantitative value
114
Metabolite RN
7623052; 7623209
Metabolite name
M2; M1
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 18 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cavg ss
Unit
ng/mL
Quantitative value
160
Metabolite RN
7623052; 7623209
Metabolite name
M2; M1
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 19 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cmax
Unit
ng/mL
Quantitative value
219
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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20 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
AUC (0-24 h)
Unit
ng.h/mL
Quantitative value
3834
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 21 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
tmax
Unit
hour
Quantitative value
3.36
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 22 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
t1/2 el
Unit
hour
Quantitative value
23.5
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
71/98
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Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 23 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cmin
Unit
ng/mL
Quantitative value
114
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 24 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cavg ss
Unit
ng/mL
Quantitative value
160
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 25 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cmax i/Cmax
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Quantitative value
1.01
Metabolite RN
7623052; 7623209
Metabolite name
M2; M1
Concomitants: Compound RN
3658031
Concomitants: Compound name
Orlistat
Concomitants: Compound role
ICP
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 26 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
AUC i/AUC (0-24 h)
Quantitative value
1.01
Metabolite RN
7623052; 7623209
Metabolite name
M2; M1
Concomitants: Compound RN
3658031
Concomitants: Compound name
Orlistat
Concomitants: Compound role
ICP
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 27 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cmin i/Cmin
Quantitative value
1.04
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Metabolite RN
7623052; 7623209
Metabolite name
M2; M1
Concomitants: Compound RN
3658031
Concomitants: Compound name
Orlistat
Concomitants: Compound role
ICP
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 28 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cavgss i/Cavgss
Quantitative value
1.01
Metabolite RN
7623052; 7623209
Metabolite name
M2; M1
Concomitants: Compound RN
3658031
Concomitants: Compound name
Orlistat
Concomitants: Compound role
ICP
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 29 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
t1/2 el i/t1/2 el
Quantitative value
1
Metabolite RN
7623052; 7623209
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
74/98
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Metabolite name
M2; M1
Concomitants: Compound RN
3658031
Concomitants: Compound name
Orlistat
Concomitants: Compound role
ICP
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 30 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cmax
Unit
ng/mL
Quantitative value
222
Metabolite RN
7623052; 7623209
Metabolite name
M2; M1
Concomitants: Compound RN
3658031
Concomitants: Compound name
Orlistat
Concomitants: Compound role
ICP
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 31 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
AUC (0-24 h)
Unit
ng.h/mL
Quantitative value
3887
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
75/98
2018-06-23 10:56:32
Metabolite RN
7623052; 7623209
Metabolite name
M2; M1
Concomitants: Compound RN
3658031
Concomitants: Compound name
Orlistat
Concomitants: Compound role
ICP
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 32 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
tmax
Unit
hour
Quantitative value
3.3
Metabolite RN
7623052; 7623209
Metabolite name
M2; M1
Concomitants: Compound RN
3658031
Concomitants: Compound name
Orlistat
Concomitants: Compound role
ICP
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 33 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
t1/2 el
Unit
hour
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
76/98
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Quantitative value
23.6
Metabolite RN
7623052; 7623209
Metabolite name
M2; M1
Concomitants: Compound RN
3658031
Concomitants: Compound name
Orlistat
Concomitants: Compound role
ICP
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 34 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cmin
Unit
ng/mL
Quantitative value
118
Metabolite RN
7623052; 7623209
Metabolite name
M2; M1
Concomitants: Compound RN
3658031
Concomitants: Compound name
Orlistat
Concomitants: Compound role
ICP
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 35 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Non Smoker
Substance RN
3912379View in Reaxys
Substance Name
Phentermine
Substance Dose
37.5000 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cavg ss
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Unit
ng/mL
Quantitative value
162
Metabolite RN
7623052; 7623209
Metabolite name
M2; M1
Concomitants: Compound RN
3658031
Concomitants: Compound name
Orlistat
Concomitants: Compound role
ICP
Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E; Journal of clinical pharmacology; vol. 42; nb. 9; (2002); p. 1011 - 1019, View in Reaxys 36 of 83
37 of 83
Target Name
adrenergic receptor [rat]
Target Synonyms
adrenergic receptor
Target, Subunit, Species
adrenergic receptor [rat]
Target Mutant/Chimera Details
adrenergic receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Organ contraction
Biological Species/NCBI ID
rat
Organs/Tissues
vas deferens
Substance RN
3912379View in Reaxys
Substance Name
17
Measurement Parameter
percentage
Unit
%
Measurement Object
of control max effect
Quantitative value
31
Target Name
adrenergic receptor [rat]
Target Synonyms
adrenergic receptor
Target, Subunit, Species
adrenergic receptor [rat]
Target Mutant/Chimera Details
adrenergic receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Organ contraction
Biological Species/NCBI ID
rat
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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38 of 83
Organs/Tissues
vas deferens
Substance RN
3912379View in Reaxys
Substance Name
17
Measurement Parameter
time
Unit
second
Measurement Object
onset of action
Quantitative value
30 - 90
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |transmitter releasing Bioassay : control: saline; ref.: fluoxetine rats administered with title comp.; blood collected every 15 min pre-dosing and at 15-min intervals for 90 min post-dosing; dialyzed; dialysates assayed for 5-hydroxytryptamine and 5-hydroxyindoleacetic acid using HPLC with electrochemical detection
Biological Species/NCBI ID
rat
Substance RN
3912379View in Reaxys
Substance Name
70808
Substance Dose
1 mg/kg
Substance Route of Adm.
intravenous administration
Qualitative Results
title comp. had very weak effect on 5-hydroxytryptamine levels; title comp. treatment did not affect plasma 5-hydroxyindoleacetic acid levels; diagram
Measurement Parameter
qualitative
Zolkowska, Dorota; Rothman, Richard B.; Baumann, Michael H.; Journal of Pharmacology and Experimental Therapeutics; vol. 318; nb. 2; (2006); p. 604 - 610, View in Reaxys 39 of 83
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |transmitter releasing Bioassay : control: saline; ref.: fluoxetine title comp. added to blood samples; microdialysis probes placed into blood samples; dialysate efflux collected for 15 min; assayed for 5-hydroxytryptamine levels
Biological Species/NCBI ID
rat
Substance RN
3912379View in Reaxys
Substance Name
70808
Substance Dose
0.300000 µM
Qualitative Results
title comp. significantly increased plasma 5-hydroxytryptamine levels only at 33 μmol/l; diagram
Measurement Parameter
qualitative
Zolkowska, Dorota; Rothman, Richard B.; Baumann, Michael H.; Journal of Pharmacology and Experimental Therapeutics; vol. 318; nb. 2; (2006); p. 604 - 610, View in Reaxys 40 of 83
Substance Effect
Antiobesity
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Measurement Parameter
qualitative
Qualitative value
@
; (2012); Type: Review, Lab: EFF_071212, Owner: EFFECT, Number: 000, Revision: 07.12.2012 00:00:00, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
79/98
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41 of 83
Substance Effect
Anorectic
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Measurement Parameter
qualitative
Qualitative value
@
; (2012); Type: Review, Lab: EFF_071212, Owner: EFFECT, Number: 000, Revision: 07.12.2012 00:00:00, View in Reaxys 42 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
AUC (0-24 h)
Unit
ng.h/mL
Quantitative value
1171.6
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 43 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cmax
Unit
ng/mL
Quantitative value
67.4
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 44 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
tmax
Unit
hour
Quantitative value
2
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 45 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
t1/2 el
Unit
hour
Quantitative value
19.5
Deviation
4.30000
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 46 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
AUC (0-24 h)
Unit
ng.h/mL
Quantitative value
1171.6
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
81/98
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Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 47 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cmax
Unit
ng/mL
Quantitative value
67.4
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 48 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
tmax
Unit
hour
Quantitative value
2
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 49 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
82/98
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Substance Dosing Regimen
Repeated
Measurement Parameter
AUC i/AUC (0-24 h)
Quantitative value
1.04
Concomitants: Compound RN
10610881; 10610881
Concomitants: Compound name
Taranabant; Taranabant
Concomitants: Compound role
ICP; ICP
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 50 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cmax i/Cmax
Quantitative value
0.99
Concomitants: Compound RN
10610881; 10610881
Concomitants: Compound name
Taranabant; Taranabant
Concomitants: Compound role
ICP; ICP
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 51 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
AUC (0-24 h)
Unit
ng.h/mL
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Quantitative value
1171.6
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 52 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cmax
Unit
ng/mL
Quantitative value
67.4
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 53 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
tmax
Unit
hour
Quantitative value
2
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 54 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Substance Dosing Regimen
Repeated
Measurement Parameter
t1/2 el
Unit
hour
Quantitative value
19.5
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 55 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
AUC i/AUC (0-24 h)
Quantitative value
1.08
Concomitants: Compound RN
10610881; 10610881
Concomitants: Compound name
Taranabant; Taranabant
Concomitants: Compound role
ICP; ICP
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 56 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cmax i/Cmax
Quantitative value
1.13
Concomitants: Compound RN
10610881; 10610881
Concomitants: Compound name
Taranabant; Taranabant
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Concomitants: Compound role
ICP; ICP
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 57 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
t1/2 el i/t1/2 el
Quantitative value
1.13
Concomitants: Compound RN
10610881; 10610881
Concomitants: Compound name
Taranabant; Taranabant
Concomitants: Compound role
ICP; ICP
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 58 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
AUC (0-24 h)
Unit
ng.h/mL
Quantitative value
1216.2
Concomitants: Compound RN
10610881; 10610881
Concomitants: Compound name
Taranabant; Taranabant
Concomitants: Compound role
ICP; ICP
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Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 59 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cmax
Unit
ng/mL
Quantitative value
66.59
Concomitants: Compound RN
10610881; 10610881
Concomitants: Compound name
Taranabant; Taranabant
Concomitants: Compound role
ICP; ICP
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 60 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
tmax
Unit
hour
Quantitative value
3
Concomitants: Compound RN
10610881; 10610881
Concomitants: Compound name
Taranabant; Taranabant
Concomitants: Compound role
ICP; ICP
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys
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61 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
AUC (0-24 h)
Unit
ng.h/mL
Quantitative value
1261.9
Concomitants: Compound RN
10610881; 10610881
Concomitants: Compound name
Taranabant; Taranabant
Concomitants: Compound role
ICP; ICP
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 62 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
Cmax
Unit
ng/mL
Quantitative value
76.49
Concomitants: Compound RN
10610881; 10610881
Concomitants: Compound name
Taranabant; Taranabant
Concomitants: Compound role
ICP; ICP
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 63 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
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Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
tmax
Unit
hour
Quantitative value
3
Concomitants: Compound RN
10610881; 10610881
Concomitants: Compound name
Taranabant; Taranabant
Concomitants: Compound role
ICP; ICP
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 64 of 83
Bioassay Category
Pharmacokinetic
Bioassay Name
Pharmacokinetic
Biological Species/NCBI ID
human Native American; human Black person; human Hispanic; Human Caucasian
Population State
Healthy; Healthy; Healthy; Healthy
Substance RN
3912379View in Reaxys
Substance Name
Phentermine hydrochloride
Substance Dose
15 mg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Repeated
Measurement Parameter
t1/2 el
Unit
hour
Quantitative value
22
Deviation
3.40000
Concomitants: Compound RN
10610881; 10610881
Concomitants: Compound name
Taranabant; Taranabant
Concomitants: Compound role
ICP; ICP
Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.; Journal of Clinical Pharmacology; vol. 49; nb. 10; (2009); p. 1228 1238, View in Reaxys 65 of 83
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
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Bioassay Details
Effect : |drug interaction Bioassay : further studies: title comp. dosed with cocaine (ca. 3-30 μmol/kg) rats trained to discriminate cocaine (29.4 μmol/kg, i.p.) from saline treated with title comp.; 5 or 15 min after rats tested in two-lever operant-conditioning chambers
Biological Species/NCBI ID
rat
Substance RN
3912379View in Reaxys
Substance Name
70808
Substance Dose
2 µmol/kg
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
ED50
Unit
µmol/kg
Quantitative value
7.09
Li, Su-Min; Campbell, Bettye L.; Katz, Jonathan L.; Journal of Pharmacology and Experimental Therapeutics; vol. 317; nb. 3; (2006); p. 1088 - 1096, View in Reaxys 66 of 83
Target Name
trace amine-associated receptor 1 [human]
Target Synonyms
ta1; taar1; tar-1; tar1; trace amine receptor 1; trace amine-associated receptor 1; trar1
Target Uniprot ID
q96rj0
Target, Subunit, Species
trace amine-associated receptor 1 [human]
Target Mutant/Chimera Details
trace amine-associated receptor 1 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Ca2+ mobilisation
Cells/Cell Lines
CHO cell line
Substance RN
3912379View in Reaxys
Substance Name
49
Measurement Parameter
EC50
Unit
nM
Quantitative value
5470
Deviation
1900
Measurement pX
5.26
Concomitants: Compound name
Calcium-3-dye
Concomitants: Compound role
MAR
Lewin, Anita H.; Navarro, Hernan A.; Wayne Mascarella; Bioorganic and Medicinal Chemistry; vol. 16; nb. 15; (2008); p. 7415 - 7423, View in Reaxys 67 of 83
Target Name
trace amine-associated receptor 1 [human]
Target Synonyms
ta1; taar1; tar-1; tar1; trace amine receptor 1; trace amine-associated receptor 1; trar1
Target Uniprot ID
q96rj0
Target, Subunit, Species
trace amine-associated receptor 1 [human]
Target Mutant/Chimera Details
trace amine-associated receptor 1 [human]:Wild
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Target Species (Bioactivity)
human
Target Transfection
Transfected
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Ca2+ mobilisation
Cells/Cell Lines
CHO cell line
Substance RN
3912379View in Reaxys
Substance Name
49
Measurement Parameter
Emax
Unit
%
Quantitative value
68
Deviation
4
Concomitants: Compound name
Calcium-3-dye
Concomitants: Compound role
MAR
Lewin, Anita H.; Navarro, Hernan A.; Wayne Mascarella; Bioorganic and Medicinal Chemistry; vol. 16; nb. 15; (2008); p. 7415 - 7423, View in Reaxys 68 of 83
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Lethal dose of the compound in rat after intraperitoneal administration
Biological Species/NCBI ID
rat
Substance RN
3912379View in Reaxys
Qualitative Results
81
Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
81
HOLM; HUUS; KOPF; MOLLER NIELSEN; PETERSEN; Acta pharmacologica et toxicologica; vol. 17; (1960); p. 121 136, View in Reaxys 69 of 83
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Lethal dose of the compound in rabbit after intravenous administration
Biological Species/NCBI ID
Leporidae
Substance RN
3912379View in Reaxys
Qualitative Results
15
Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
15
M. R. WARREN; D. G. MARSH; C. R. THOMPSON; R. S. SHELTON; T. J. BECKER; The Journal of pharmacology and experimental therapeutics; vol. 79; (1943); p. 187, View in Reaxys 70 of 83
Target Name
Phenylalanyl-tRNA Synthetase 2, Mitochondrial [Escherichia coli]
Target Synonyms
phenylalanyl-trna synthetase 2, mitochondrial
Target, Subunit, Species
Phenylalanyl-tRNA Synthetase 2, Mitochondrial [Escherichia coli]
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71 of 83
72 of 83
Target Mutant/Chimera Details
Phenylalanyl-tRNA Synthetase 2, Mitochondrial [Escherichia coli]:Wild
Target Species (Bioactivity)
Escherichia coli
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Negative free energies of binding to phenylalanyl-tRNA synthetase from Escherichia coli was determined
Biological Species/NCBI ID
Escherichia coli
Substance RN
3912379View in Reaxys
Qualitative Results
Delta F not calculated
Measurement Parameter
qualitative
Measurement Object
Delta F
Target Name
Phenylalanyl-tRNA Synthetase 2, Mitochondrial [Escherichia coli]
Target Synonyms
phenylalanyl-trna synthetase 2, mitochondrial
Target, Subunit, Species
Phenylalanyl-tRNA Synthetase 2, Mitochondrial [Escherichia coli]
Target Mutant/Chimera Details
Phenylalanyl-tRNA Synthetase 2, Mitochondrial [Escherichia coli]:Wild
Target Species (Bioactivity)
Escherichia coli
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibition constant of the compound towards ATP-PPi exchange catalyzed by phenylalanyl-tRNA synthetase from Escherichia coli
Biological Species/NCBI ID
Escherichia coli
Substance RN
3912379View in Reaxys
Measurement Parameter
Ki (inhibition constant)
Unit
µM
Qualitative value
=
Quantitative value
480
Measurement pX
3.32
Target Name
Phenylalanyl-tRNA Synthetase 2, Mitochondrial [Escherichia coli]
Target Synonyms
phenylalanyl-trna synthetase 2, mitochondrial
Target, Subunit, Species
Phenylalanyl-tRNA Synthetase 2, Mitochondrial [Escherichia coli]
Target Mutant/Chimera Details
Phenylalanyl-tRNA Synthetase 2, Mitochondrial [Escherichia coli]:Wild
Target Species (Bioactivity)
Escherichia coli
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Evaluated for inhibition of Phenylalanyl-tRNA synthetase (from Escherichia coli) catalyzed ATPPPi exchange
Biological Species/NCBI ID
Escherichia coli
Substance RN
3912379View in Reaxys
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73 of 83
74 of 83
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Qualitative value
=
Quantitative value
480000
Measurement pX
3.32
Target Name
Phenylalanyl-tRNA Synthetase 2, Mitochondrial [Escherichia coli]
Target Synonyms
phenylalanyl-trna synthetase 2, mitochondrial
Target, Subunit, Species
Phenylalanyl-tRNA Synthetase 2, Mitochondrial [Escherichia coli]
Target Mutant/Chimera Details
Phenylalanyl-tRNA Synthetase 2, Mitochondrial [Escherichia coli]:Wild
Target Species (Bioactivity)
Escherichia coli
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Negative free energies of binding to Phenylalanyl-tRNA synthetase from Escherichia coli
Biological Species/NCBI ID
Escherichia coli
Substance RN
3912379View in Reaxys
Measurement Parameter
qualitative
Qualitative value
Not Published
Bioassay Category
Pharmacokinetic
Bioassay Details
Time to reach peak blood concentration of the compound in human upon oral administration
Biological Species/NCBI ID
human
Substance RN
3912379View in Reaxys
Qualitative Results
4
Measurement Parameter
tmax
Unit
hour
Quantitative value
4
Clarke's Analysis of Drugs and Poisons, View in Reaxys 75 of 83
Bioassay Category
Pharmacokinetic
Bioassay Details
Peak blood concentration of the compound in human upon oral administration
Biological Species/NCBI ID
human
Substance RN
3912379View in Reaxys
Substance Route of Adm.
oral administration
Qualitative Results
0.1
Measurement Parameter
Cmax
Unit
µg/mL
Quantitative value
0.1
Clarke's Analysis of Drugs and Poisons, View in Reaxys 76 of 83
Bioassay Category
Metabolism/Transport
Bioassay Details
Volume of the distribution of the compound in human
Biological Species/NCBI ID
human
Substance RN
3912379View in Reaxys
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Qualitative Results
3-4
Measurement Parameter
Vd (volume of distribution)
Unit
L/kg
Quantitative value
3.5
Clarke's Analysis of Drugs and Poisons, View in Reaxys 77 of 83
Bioassay Category
Metabolism/Transport
Bioassay Details
Plasma half life of the compound
Biological Species/NCBI ID
human
Substance RN
3912379View in Reaxys
Qualitative Results
19-24
Measurement Parameter
t1/2 el
Unit
hour
Measurement Object
Half Life
Quantitative value
21.5
Clarke's Analysis of Drugs and Poisons, View in Reaxys 78 of 83
Bioassay Category
Pharmacokinetic
Bioassay Details
Urinary excretion of unchanged drug after 24 h of oral administration in human
Biological Species/NCBI ID
human
Substance RN
3912379View in Reaxys
Qualitative Results
70-80
Measurement Parameter
percentage of dose excreted in urine
Unit
%
Quantitative value
75
Clarke's Analysis of Drugs and Poisons, View in Reaxys 79 of 83
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Lethal dose of the compound in rat after oral administration
Biological Species/NCBI ID
rat
Substance RN
3912379View in Reaxys
Substance Route of Adm.
oral administration
Qualitative Results
188
Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
188
BECKER; Toxicology and applied pharmacology; vol. 3; (1961); p. 256 - 259, View in Reaxys 80 of 83
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Lethal dose of the compound in mouse after oral administration
Biological Species/NCBI ID
mouse
Substance RN
3912379View in Reaxys
Substance Route of Adm.
oral administration
Qualitative Results
154
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Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
154
BECKER; Toxicology and applied pharmacology; vol. 3; (1961); p. 256 - 259, View in Reaxys 81 of 83
Bioassay Category
Pharmacokinetic
Bioassay Details
Amount excreted during 72hrs
Biological Species/NCBI ID
human
Substance RN
3912379View in Reaxys
Qualitative Results
85
Measurement Parameter
Excretion
Unit
%
Quantitative value
85
Delbeke; Debackere; Arzneimittel-Forschung/Drug Research; vol. 36; nb. 1; (1986); p. 134 - 137, View in Reaxys 82 of 83
Bioassay Category
In Vivo (Animal models)
Bioassay Details
Chemorelease activity of compound was tested in mice heart by injecting norepinephrine-3H into tail vein of mice after sc administration of compound at 10 mg/kg
Biological Species/NCBI ID
mouse
Substance RN
3912379View in Reaxys
Substance Route of Adm.
subcutaneous administration
Measurement Parameter
percentage
Unit
%
Measurement Object
Norepinephrine-3H release
Qualitative value
=
Quantitative value
95
Concomitants: Compound name
[3H]Norepinephrine
Concomitants: Compound role
RAD
Daly; Creveling; Witkop; Journal of medicinal chemistry; vol. 9; nb. 3; (1966); p. 273 - 280, View in Reaxys 83 of 83
Bioassay Category
In Vivo (Animal models)
Bioassay Details
Activity of the compound against chemorelease of norepinephrine-[3H] from mouse heart at 10 mg/kg dose upon s.c. administration relative to control
Biological Species/NCBI ID
mouse
Organs/Tissues
heart
Substance RN
3912379View in Reaxys
Substance Route of Adm.
subcutaneous administration
Measurement Parameter
Activity
Unit
%
Qualitative value
=
Quantitative value
95
Concomitants: Compound name
[3H]Norepinephrine
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Concomitants: Compound role
RAD
Daly; Creveling; Witkop; Journal of medicinal chemistry; vol. 9; nb. 3; (1966); p. 273 - 280, View in Reaxys
Reaxys ID 4623759 View in Reaxys
3/6
H 2N
CAS Registry Number: 118132-96-0 Linear Structure Formula: C10H15N*C7H8O3S Molecular Formula: C7H8O3S*C10H15N Molecular Weight: 321.441 Type of Substance: isocyclic InChI Key: GIWRVBSOECGZLY-UHFFFAOYSA-N Note:
O O
S HO
Substance Label (1) Label References 6e
Koziara, Anna; Zwierzak, Andrzej; Tetrahedron Letters; vol. 28; nb. 51; (1987); p. 6513 - 6516, View in Reaxys
Druglikeness (1) 1 of 1
LogP
3.232
H Bond Donors
2
H Bond Acceptors
4
Rotatable Bonds
3
TPSA
88.77
Lipinski Number
4
Veber Number
2
Melting Point (2) 1 of 2
Melting Point [°C]
169 - 172
Zwierzak, Andrzej; Phosphorus, Sulfur and Silicon and the Related Elements; vol. 75; nb. 1-4; (1993); p. 51 - 54, View in Reaxys 2 of 2
Melting Point [°C]
169 - 172
Solvent (Melting Point)
CHCl3
Koziara, Anna; Zwierzak, Andrzej; Tetrahedron Letters; vol. 28; nb. 51; (1987); p. 6513 - 6516, View in Reaxys
Reaxys ID 18581811 View in Reaxys
4/6 2
H
CAS Registry Number: 1039678-74-4 Linear Structure Formula: C10H2 (2)H13N Molecular Formula: C10H15N Molecular Weight: 162.133 InChI Key: DHHVAGZRUROJKS-BEKAVNSESA-N Note:
2
H
2
2
H
2
H
H
NH 2 2
H H
2
2
H
2H 2
H
2H
2H
2
H
Substance Label (1) Label References 15-d
Ito, Nobuhiro; Watahiki, Tsutomu; Maesawa, Tsuneaki; Maegawa, Tomohiro; Sajiki, Hironao; Synthesis; nb. 9; (2008); p. 1467 - 1478; Art.No: F03608SS, View in Reaxys
Druglikeness (1) 1 of 1
LogP
2.179
H Bond Donors
1
H Bond Acceptors
1
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Rotatable Bonds
2
TPSA
26.02
Lipinski Number
4
Veber Number
2
Reaxys ID 18665544 View in Reaxys
5/6 Chemical Name: phentermine pamoate Linear Structure Formula: C10H15N*C23H16O6 Molecular Formula: C10H15N*C23H16O6 Molecular Weight: 537.612 InChI Key: IYIAKOKJRKKESY-UHFFFAOYSA-N Note:
H 2N
OHHO
O
OH
HO
O
Patent-Specific Data (1) Location in Patent References Page/Page column
Patent; King, Clifford Riley; Bristol, David W.; English, Michael L.; US2014/178480; (2014); (A1) English, View in Reaxys
Druglikeness (1) 1 of 1
H Bond Donors
5
H Bond Acceptors
5
Rotatable Bonds
6
TPSA
141.08
Lipinski Number
2
Veber Number
1
Solubility (MCS) (1) 1 of 1
Location
Paragraph 0212-0218
Comment (Solubility (MCS))
phentermine pamoate insolubility at pH 4.5 and 7.0
Patent; King, Clifford Riley; Bristol, David W.; English, Michael L.; US2014/178480; (2014); (A1) English, View in Reaxys IR Spectroscopy (1) 1 of 1
Description (IR Spectroscopy)
Bands; Spectrum
Solvent (IR Spectroscopy)
potassium bromide
Location
Paragraph 0077
Patent; King, Clifford Riley; Bristol, David W.; English, Michael L.; US2014/178480; (2014); (A1) English, View in Reaxys
Reaxys ID 18692515 View in Reaxys
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6/6
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Chemical Name: phentermine pamoate Linear Structure Formula: 2C10H15N*C23H16O6 Molecular Formula: 2C10H15N*C23H16O6 Molecular Weight: 686.848 InChI Key: IYIAKOKJRKKESY-UHFFFAOYSA-N Note:
H 2N 2
OHHO
O
OH
HO
O
Druglikeness (1) 1 of 1
H Bond Donors
5
H Bond Acceptors
5
Rotatable Bonds
6
TPSA
141.08
Lipinski Number
2
Veber Number
1
IR Spectroscopy (1) 1 of 1
Description (IR Spectroscopy)
FT-IR
Patent; Bristol, David William; King, Clifford Riley; Mitchener, JR., Joseph Pike; Audia, Vicki Haynes; US2008/293695; (2008); (A1) English, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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