2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil)

Page 1

Reaxys

PubChem

eMolecules

LabNetwork

Reactions (23)

Substances (1)

Structure

Citations (469)

Structure/Compound Data Chemical Name: Modafinil Reaxys Registry Number: 1978970

CAS Registry Number: 112111-43-0, 112111-47-4, 112111-49-6, 68693-11-8 Type of Substance: isocyclic Molecular Formula: C15H15NO2S Linear Structure Formula: C15H15NO2S Molecular Weight: 273.356 InChI Key: YFGHCGITMMYXAQ-UHFFFAOYSA-N

1

N° of preparations All Preps | All Reactions 20 prep out of 23 reactions.

Available Data

N° of ref.

Identification Physical Data (14) Spectra (21) Bioactivity (150) Other Data (327)

469

Synthesize | Hide Details Find similar Chemical Names and Synonyms Modafinil Identification Substance Label (21) Label

Reference

2

Jung, Jae-Chul; Lee, Yeonju; Son, Jee-Young; Lim, Eunyoung; Jung, Mankil; Oh, Seikwan

Molecules, 2012 , vol. 17, # 9 p. 10446 - 10458 Title/Abstract Full Text View citing articles Show Details

Cao, Jianjing; Slack, Rachel D.; Bakare, Oluyomi M.; Burzynski, Caitlin; Rais, Rana; Slusher, Barbara S.; Kopajtic, Theresa; Bonifazi, Alessandro; Ellenberger, Michael P.; Yano, Hideaki; He, Yi; Bi, Guo-Hua; Xi, Zheng-Xiong; Loland, Claus J.; Newman, Amy Hauck

Journal of Medicinal Chemistry, 2016 , vol. 59, # 23 p. 10676 - 10691 Title/Abstract Full Text View citing articles Show Details

RAC-MOD

Krasulova, Kristyna; Siller, Michal; Holas, Ondrej; Dvorak, Zdenek; Anzenbacher, Pavel

Xenobiotica, 2016 , vol. 46, # 4 p. 315 - 324


Title/Abstract Full Text View citing articles Show Details

3o

Neveselý, Tomáš; Svobodová, Eva; Chudoba, Josef; Sikorski, Marek; Cibulka, Radek

Advanced Synthesis and Catalysis, 2016 , vol. 358, # 10 p. 1654 - 1663 Title/Abstract Full Text View citing articles Show Details

5

KANDULA, Mahesh

Patent: WO2013/179153 A1, 2013 ; Title/Abstract Full Text Show Details

Kandula, Mahesh

Patent: US2015/141513 A1, 2015 ; Title/Abstract Full Text Show Details

10l

Šturala, Jiří; Boháčová, Soňa; Chudoba, Josef; Metelková, Radka; Cibulka, Radek

Journal of Organic Chemistry, 2015 , vol. 80, # 5 p. 2676 - 2699 Title/Abstract Full Text View citing articles Show Details

9h

Hartman, Tomáš; Šturala, Jiří; Cibulka, Radek

Advanced Synthesis and Catalysis, 2015 , vol. 357, # 16-17 p. 3573 - 3586 Title/Abstract Full Text View citing articles Show Details

(±)-1

Okunola-Bakare, Oluyomi M.; Cao, Jianjing; Kopajtic, Theresa; Katz, Jonathan L.; Loland, Claus J.; Shi, Lei; Newman, Amy Hauck

Journal of Medicinal Chemistry, 2014 , vol. 57, # 3 p. 1000 - 1013 Title/Abstract Full Text View citing articles Show Details

1

Lesur, Brigitte; Lin, Yin G.; Marcy, Val R.; Aimone, Lisa D.; Gruner, John; Bacon, Edward R.; Chatterjee, Sankar

Chemical Biology and Drug Design, 2013 , vol. 81, # 3 p. 429 - 432 Title/Abstract Full Text View citing articles Show Details

I

GENERICS [UK] LIMITED; MYLAN DEVELOPMENT CENTRE PRIVATE LIMITED

Patent: WO2008/149141 A2, 2008 ; Title/Abstract Full Text Show Details

200

MALLINCKRODT INC.

Patent: WO2007/70238 A2, 2007 ; Title/Abstract Full Text Show Details

(+/-)-3

Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale

Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details

Negwer8 5346

Taneja, Indu; Bruehl, Stephen; Robertson, David

Journal of Clinical Pharmacology, 2004 , vol. 44, # 12 p. 1425 - 1427 Title/Abstract Full Text View citing articles Show Details

CRL 40476-[f I]

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

CRL 40476-[f III]

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ;

CRL 40476-[f IV]

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ;

CRL 40476-[f VII]

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ;

CRL 40476-[f VI]

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ;

CRL 40476-[f V]

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ;

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details


Title/Abstract Full Text Show Details

M12: 6311

Wong, Y. Nancy; King, S. Peter; Laughton, Watson B.; McCormick, George C.; Grebow, Peter E.

Journal of Clinical Pharmacology, 1998 , vol. 38, # 3 p. 276 - 282 Title/Abstract Full Text View citing articles Show Details

MODA

Vezin; Daveloose; Debouzy; Fauvelle; Roussel; Viret

Bollettino Chimico Farmaceutico, 1994 , vol. 133, # 7 p. 476 - 481 Title/Abstract Full Text View citing articles Show Details

Label

Reference

CRL 40476

Lab. Lafon

Patent: DE2809625US4177290 , 19781979 ; Chem.Abstr., vol. 93, # 7872 Full Text Show Details

Patent-Specific Data (4) Related Markush Structure (RN)

Reference FECHTER, Cary Erwin

Patent: WO2016/209765 A1, 2016 ;

30987469

Title/Abstract Full Text Show Details

27378387; 27378388

THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES; NEWMAN, Amy Hauck; OKUNOLABAKARE, Oluyomi M.; CAO, Jianjing

Patent: WO2014/138518 A2, 2014 ; Title/Abstract Full Text Show Details

The Board of Trustees of the University of Arkansas

Patent: US2008/221216 A1, 2008 ;

18499450

Title/Abstract Full Text Show Details

MALLINCKRODT INC.

Patent: WO2007/70238 A2, 2007 ;

11339069

Title/Abstract Full Text Show Details

Physical Data Melting Point (6) Melting Point

Solvent (Melting Point)

159 160 °C

Location

Reference

Paragraph 0112

Kandula, Mahesh

Patent: US2015/141513 A1, 2015 ; Title/Abstract Full Text Show Details

161 162 °C

methanol

Paragraph 0112

Kandula, Mahesh

Patent: US2015/141513 A1, 2015 ; Title/Abstract Full Text Show Details

120 122 °C

161 162 °C

methanol

supporting information

Bogolubsky, Andrey V.; Moroz, Yurii S.; Mykhailiuk, Pavel K.; Ostapchuk, Eugeniy N.; Rudnichenko, Alexander V.; Dmytriv, Yurii V.; Bondar, Anna N.; Zaporozhets, Olga A.; Pipko, Sergey E.; Doroschuk, Roman A.; Babichenko, Liudmyla N.; Konovets, Anzhelika I.; Tolmachev, Andrey

ACS Combinatorial Science, 2015 , vol. 17, # 6 p. 348 - 354 Title/Abstract Full Text View citing articles Show Details

Paragraph 00101

KANDULA, Mahesh

Patent: WO2013/179153 A1, 2013 ; Title/Abstract Full Text Show Details

164 165 °C

isopropyl alcohol N,Ndimethyl-

Bicherov; Akopova; Spiglazov; Morkovnik

Russian Chemical Bulletin, 2010 , vol. 59, # 1 p. 91 - 101 Title/Abstract Full Text View citing articles Show Details


formamide SEPRACOR INC.

Patent: WO2005/63248 A1, 2005 ;

163 165 °C

Title/Abstract Full Text Show Details

Chromatographic Data (3) Chromatographic data

Original string

Location

Reference 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, 2015 , vol. 29, # 4 p. 367 - 384 Title/Abstract Full Text View citing articles Show Details

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, 2015 , vol. 29, # 4 p. 367 - 384 Title/Abstract Full Text Show Details

LC (Liquid chromatography)

TLC (Thin layer chromatography)

R&f %0.6

Kandula, Mahesh

Patent: US2015/141513 A1, 2015 ;

Paragraph 0112

Title/Abstract Full Text Show Details

TLC (Thin layer chromatography)

R&f% 0.6

Paragraph 00101

KANDULA, Mahesh

Patent: WO2013/179153 A1, 2013 ; Title/Abstract Full Text Show Details

Crystal Property Description (4) Colour & Other Properties white

Location

Reference

Paragraph 0112

Kandula, Mahesh

Patent: US2015/141513 A1, 2015 ; Title/Abstract Full Text Show Details

white

supporting information

Bogolubsky, Andrey V.; Moroz, Yurii S.; Mykhailiuk, Pavel K.; Ostapchuk, Eugeniy N.; Rudnichenko, Alexander V.; Dmytriv, Yurii V.; Bondar, Anna N.; Zaporozhets, Olga A.; Pipko, Sergey E.; Doroschuk, Roman A.; Babichenko, Liudmyla N.; Konovets, Anzhelika I.; Tolmachev, Andrey

ACS Combinatorial Science, 2015 , vol. 17, # 6 p. 348 - 354 Title/Abstract Full Text View citing articles Show Details

white

Paragraph 00101

KANDULA, Mahesh

Patent: WO2013/179153 A1, 2013 ; Title/Abstract Full Text Show Details

MALLINCKRODT INC.

Patent: WO2007/70238 A2, 2007 ;

white

Title/Abstract Full Text Show Details

TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.

Patent: WO2007/103221 A2, 2007 ; Title/Abstract Full Text Show Details

Solubility (MCS) (1) Solubility

Saturation

Temperature (Solubility (MCS))

Solvent (Solubility (MCS))

0.136678 g·l-1

in solution

25 °C

phosphate buffer

Reference Alelyunas, Yun W.; Empfield, James R.; McCarthy, Dennis; Spreen, Russell C.; Bui, Khanh; Pelosi-Kilby, Luciana; Shen, Cindy

Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 24 p. 7312 - 7316 Title/Abstract Full Text View citing articles Show Details

Spectra NMR Spectroscopy (15) Description (NMR Spectroscopy)

Nucleus (NMR Spectroscopy)

Coupling Nuclei

Solvents (NMR Spectroscopy)

Temperature (NMR Spectroscopy)

Frequency (NMR Spectroscopy)

Original Text (NMR Spectroscopy)

Location

Comment (NMR Spectroscopy)

Reference


Chemical shifts Spectrum

1H

chloroform-d1

300 MHz

supporting information

Neveselý, Tomáš; Svobodová, Eva; Chudoba, Josef; Sikorski, Marek; Cibulka, Radek

Advanced Synthesis and Catalysis, 2016 , vol. 358, # 10 p. 1654 - 1663 Title/Abstract Full Text View citing articles Show Details

Chemical shifts Spectrum

13C

chloroform-d1

101 MHz

supporting information

Neveselý, Tomáš; Svobodová, Eva; Chudoba, Josef; Sikorski, Marek; Cibulka, Radek

Advanced Synthesis and Catalysis, 2016 , vol. 358, # 10 p. 1654 - 1663 Title/Abstract Full Text View citing articles Show Details

Spectrum

1H

supporting information

Šturala, Jiří; Boháčová, Soňa; Chudoba, Josef; Metelková, Radka; Cibulka, Radek

Journal of Organic Chemistry, 2015 , vol. 80, # 5 p. 2676 - 2699 Title/Abstract Full Text View citing articles Show Details

Chemical shifts Spectrum

1H

dimethylsulfoxided6

500 MHz

supporting information

Bogolubsky, Andrey V.; Moroz, Yurii S.; Mykhailiuk, Pavel K.; Ostapchuk, Eugeniy N.; Rudnichenko, Alexander V.; Dmytriv, Yurii V.; Bondar, Anna N.; Zaporozhets, Olga A.; Pipko, Sergey E.; Doroschuk, Roman A.; Babichenko, Liudmyla N.; Konovets, Anzhelika I.; Tolmachev, Andrey

ACS Combinatorial Science, 2015 , vol. 17, # 6 p. 348 - 354 Title/Abstract Full Text View citing articles Show Details

Chemical shifts Spectrum

13C

dimethylsulfoxided6

125.7 MHz

supporting information

Bogolubsky, Andrey V.; Moroz, Yurii S.; Mykhailiuk, Pavel K.; Ostapchuk, Eugeniy N.; Rudnichenko, Alexander V.; Dmytriv, Yurii V.; Bondar, Anna N.; Zaporozhets, Olga A.; Pipko, Sergey E.; Doroschuk, Roman A.; Babichenko, Liudmyla N.; Konovets, Anzhelika I.; Tolmachev, Andrey

ACS Combinatorial Science, 2015 , vol. 17, # 6 p. 348 - 354 Title/Abstract Full Text View citing articles Show Details

Chemical shifts Spectrum

1H

dimethylsulfoxided6

24.84 °C

399.9 MHz

supporting information

Hartman, Tomáš; Šturala, Jiří; Cibulka, Radek

Advanced Synthesis and Catalysis, 2015 , vol. 357, # 16-17 p. 3573 - 3586 Title/Abstract Full Text View citing articles Show Details

Chemical shifts Spectrum

13C

dimethylsulfoxided6

24.84 °C

supporting information

Hartman, Tomáš; Šturala, Jiří; Cibulka, Radek

Advanced Synthesis and Catalysis, 2015 , vol. 357, # 16-17 p. 3573 - 3586 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

1H

chloroform-d1

Chemical shifts

1H

dimethylsulfoxided6

Vezin; Daveloose; Debouzy; Fauvelle; Roussel; Viret

Bollettino Chimico Farmaceutico, 1994 , vol. 133, # 7 p. 476 - 481 Title/Abstract Full Text View citing articles Show Details

Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale

Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

dimethylsulfoxided6

Vezin; Daveloose; Debouzy; Fauvelle; Roussel; Viret

Bollettino Chimico Farmaceutico, 1994 , vol. 133,

300 MHz

Bicherov; Akopova; Spiglazov; Morkovnik

Russian Chemical Bulletin, 2010 , vol. 59, # 1 p. 91 - 101 Title/Abstract Full Text View citing articles Show Details


# 7 p. 476 - 481 Title/Abstract Full Text View citing articles Show Details

Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale

Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details 1H

1H

1H

chloroform-d1

1H

chloroform-d1

1H

chloroform-d1

Spin-spin coupling constants

Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale

Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details

dimethylsulfoxided6

1H NMR (CDCl3): 3.223.27 ppm, d, 1H, (S(O)CH2); 3.63-3.68 ppm, d, 1H, (J=12.5 Hz), (S(O)CH2); 5.32 ppm, s, 1H, (S(O)CHPh2); 7.38 - 7.5 ppm, m, 10H, (Aromatic).

Signals given

3.22 -3.27 ppm d 1H S(O)CH2 3.63 -3.68 ppm d 1H (J = 12.5 Hz) S(O)CH2 5.32 ppm s 1H S(O)CHPh2 7.38 - 7.5 ppm m 10H Aromatic

Signals given

H-NMR (CDC13, 5 ppm): 3. 223. 27 (d, 1H); 3. 63-3. 68 (d, 1H) (J = 12 Hz); 5. 32 (s, 1H) ; 7. 38 7. 49 (m, 10 H).

Signals given

dimethylsulfoxided6

Dipharma S.p.A.

Patent: EP1466897 A1, 2004 ; Title/Abstract Full Text Show Details

DINAMITE DIPHARMA S.P.A. abbreviated DIPHARMA S.P.A.

Patent: US2004/192929 A1, 2004 ; Title/Abstract Full Text Show Details

DINAMITE DIPHARMA S.P.A., in abbreviated form DIPHARMA S.P.A.

Patent: WO2003/95423 A1, 2003 ; Title/Abstract Full Text Show Details

1H-1H

Vezin; Daveloose; Debouzy; Fauvelle; Roussel; Viret

Bollettino Chimico Farmaceutico, 1994 , vol. 133, # 7 p. 476 - 481 Title/Abstract Full Text View citing articles Show Details

IR Spectroscopy (1) Description (IR Spectroscopy)

Comment (IR Spectroscopy)

Reference

Bands

neat (no solvent, solid phase)

Bicherov; Akopova; Spiglazov; Morkovnik

Russian Chemical Bulletin, 2010 , vol. 59, # 1 p. 91 - 101 Title/Abstract Full Text View citing articles Show Details

Mass Spectrometry (5) Description (Mass Spectrometry)

Location

Comment (Mass Spectrometry)

Reference

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, 2015 , vol. 29, # 4 p. 367 - 384 Title/Abstract Full Text Show Details

electrospray ionisation

Jeong, Eun Sook; Kim, So-Hee; Cha, Eun-Ju; Lee, Kang Mi; Kim, Ho Jun; Lee, Sang-Won; Kwon, Oh-Seung; Lee, Jaeick


(ESI) spectrum

Rapid Communications in Mass Spectrometry, 2015 , vol. 29, # 4 p. 367 - 384 Title/Abstract Full Text View citing articles Show Details

APCI (atmospheric pressure chemical ionization) spectrum

Bogolubsky, Andrey V.; Moroz, Yurii S.; Mykhailiuk, Pavel K.; Ostapchuk, Eugeniy N.; Rudnichenko, Alexander V.; Dmytriv, Yurii V.; Bondar, Anna N.; Zaporozhets, Olga A.; Pipko, Sergey E.; Doroschuk, Roman A.; Babichenko, Liudmyla N.; Konovets, Anzhelika I.; Tolmachev, Andrey

ACS Combinatorial Science, 2015 , vol. 17, # 6 p. 348 - 354 Title/Abstract Full Text View citing articles Show Details

supporting information

Vonaparti; Lyris; Angelis; Panderi; Koupparis; Tsantili-Kakoulidou; Peters; Nielen; Georgakopoulos

Rapid Communications in Mass Spectrometry, 2010 , vol. 24, # 11 p. 1595 - 1609 Title/Abstract Full Text View citing articles Show Details

HRMS (High resolution mass spectrometry) TOFMS (Time of flight mass spectrum) ESI (Electrospray ionisation) LCMS (Liquid chromatography mass spectrometry) Spectrum 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, 2008 , vol. 43, # 7 p. 980 - 992 Title/Abstract Full Text View citing articles Show Details

Bioactivity Pharmacological Data (150) 1 of 150

Comment (Pharmacological Data)

Bioactivities present

Reference

Laboratoire L. Lafon

Patent: US4177290 A1, 1979 ; Title/Abstract Full Text Show Details

CHEMAGIS LTD.

Patent: US2002/183552 A1, 2002 ; Title/Abstract Full Text Show Details

CEPHALON, INC.

Patent: WO2003/99774 A1, 2003 ; Title/Abstract Full Text Show Details

Largeau, Denis; Oddon, Gilles

Patent: US2004/2547 A1, 2004 ; Title/Abstract Full Text Show Details

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

DINAMITE DIPHARMA S.P.A., in abbreviated form DIPHARMA S.P.A.

Patent: WO2003/95423 A1, 2003 ; Title/Abstract Full Text Show Details

DINAMITE DIPHARMA S.P.A. abbreviated DIPHARMA S.P.A.

Patent: US2004/192929 A1, 2004 ; Title/Abstract Full Text Show Details

Dipharma S.p.A.

Patent: EP1466897 A1, 2004 ; Title/Abstract Full Text Show Details

Orsymonde (Organisation de synthese Mondiale)

Patent: EP1477476 A1, 2004 ; Title/Abstract Full Text Show Details

PediaMed Pharmaceuticals, Inc.

Patent: US2004/259809 A1, 2004 ; Title/Abstract Full Text Show Details

Ray, Anup Kumar; Nandi, Indranil; Palaniswamy, Suresh; Davila, Pablo; Vora, Aakanksha Harshad

Patent: US2005/8704 A1, 2005 ; Title/Abstract Full Text Show Details

Ayala, William J.

Patent: US2005/31688 A1, 2005 ;


Title/Abstract Full Text Show Details

CEPHALON, INC.

Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details

MALLINCKRODT INC.?

Patent: WO2005/42479 A1, 2005 ; Title/Abstract Full Text Show Details

BECTON, DICKINSON and COMPANY

Patent: WO2005/46701 A1, 2005 ; Title/Abstract Full Text Show Details

Barbera, Gary; Doshi, Chetan Chhabildas; Patel, Mahendra R.; Davila, Pablo; Patel, Satishkumar Ambalal

Patent: US2005/249814 A1, 2005 ; Title/Abstract Full Text Show Details

Cypress Bioscience, Inc.

Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details

Melker, Richard J.; Gold, Mark S.

Patent: US2006/62734 A1, 2006 ; Title/Abstract Full Text Show Details

CEPHALON INC.

Patent: WO2006/30278 A1, 2006 ; Title/Abstract Full Text Show Details

CENTRE FOR ADDICTION AND MENTAL HEALTH

Patent: WO2006/32146 A1, 2006 ; Title/Abstract Full Text Show Details

2 of 150

Comment (Pharmacological Data)

Bioactivities present

Reference

Feuerstein, Seth; Coric, Vladimir

Patent: US2006/167068 A1, 2006 ; Title/Abstract Full Text Show Details

Carter, Andrew

Patent: US2006/222627 A1, 2006 ; Title/Abstract Full Text Show Details

Mutual Pharmaceutical Company, Inc.

Patent: US7122566 B1, 2006 ; Title/Abstract Full Text Show Details

MICELL TECHNOLOGIES, INC.

Patent: WO2007/11707 A2, 2007 ; Title/Abstract Full Text Show Details

NEUROHEALING PHARMACEUTICALS, INC.

Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details

Cypress Bioscience, Inc.

Patent: US2007/72946 A1, 2007 ; Title/Abstract Full Text Show Details

Mallinckrodt Inc.

Patent: US2007/129444 A1, 2007 ; Title/Abstract Full Text Show Details

MALLINCKRODT INC.

Patent: WO2007/70238 A2, 2007 ; Title/Abstract Full Text Show Details

BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG

Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details

TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.

Patent: WO2007/103221 A2, 2007 ; Title/Abstract Full Text Show Details

Cephalon France

Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details

BrainCells, Inc.

Patent: US2007/270449 A1, 2007 ; Title/Abstract Full Text Show Details

HIKMA PHARMACEUTICALS


Patent: US2007/275057 A1, 2007 ; Title/Abstract Full Text Show Details

QUESTCOR PHARMACEUTICALS, INC.

Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details

NEUROHEALING PHARMACEUTICALS, INC.

Patent: WO2008/21341 A2, 2008 ; Title/Abstract Full Text Show Details

CYPRESS BIOSCIENCE, INC.

Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details

BrainCells, Inc.

Patent: US2008/64671 A1, 2008 ; Title/Abstract Full Text Show Details

THERAQUEST BIOSCIENCES, INC.

Patent: WO2008/33351 A2, 2008 ; Title/Abstract Full Text Show Details

BRAINCELLS, INC.

Patent: WO2008/39863 A2, 2008 ; Title/Abstract Full Text Show Details

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

3 of 150

Comment (Pharmacological Data)

Bioactivities present

Reference

HAAS, Magali

Patent: US2008/103199 A1, 2008 ; Title/Abstract Full Text Show Details

Lab. L. Lafon S.A.

Patent: DE2809625 , 1978 ; Chem.Abstr., vol. 90, # 22644 Full Text Show Details

Lab. Lafon

Patent: DE2809625US4177290 , 19781979 ; Chem.Abstr., vol. 93, # 7872 Full Text Show Details

Saletu; Frey; Krupka; Anderer; Grunberger; Barbanoj

Arzneimittel-Forschung/Drug Research, 1989 , vol. 39, # 10 p. 1268 - 1273 Title/Abstract Full Text View citing articles Show Details

Vezin; Daveloose; Debouzy; Fauvelle; Roussel; Viret

Bollettino Chimico Farmaceutico, 1994 , vol. 133, # 7 p. 476 - 481 Title/Abstract Full Text View citing articles Show Details

Tanganelli; de la Mora; Ferraro; Mendez-Franco; Beani; Rambert; Fuxe

European Journal of Pharmacology, 1995 , vol. 273, # 1-2 p. 63 - 71 Title/Abstract Full Text View citing articles Show Details

Ferraro, Luca; Tanganelli, Sergio; O'Connor, William Thomas; Antonelli, Tiziana; Rambert, Francis; Fuxe, Kjell

European Journal of Pharmacology, 1996 , vol. 306, # 1-3 p. 33 - 39 Title/Abstract Full Text View citing articles Show Details

Wong, Y. Nancy; Simcoe, Donna; Hartman, Linda N.; Laughton, Watson B.; King, S. Peter; McCormick, George C.; Grebow, Peter E.

Journal of Clinical Pharmacology, 1999 , vol. 39, # 1 p. 30 - 40 Title/Abstract Full Text View citing articles Show Details

Robertson Jr., Philmore; Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael

Journal of Clinical Pharmacology, 2002 , vol. 42, # 2 p. 205 - 214 Title/Abstract Full Text View citing articles Show Details

Robertson Jr., Philmore; Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael

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Edgar, Dale M.; Seidel, Wesley F.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 283, # 2 p. 757 - 769 Title/Abstract Full Text View citing articles Show Details

Wong, Y. Nancy; Wang, Lixia; Hartman, Linda; Simcoe, Donna; Chen, Yusong; Laughton, Watson; Eldon, Richard; Markland, Colin; Grebow, Peter

Journal of Clinical Pharmacology, 1998 , vol. 38, # 10 p. 971 - 978 Title/Abstract Full Text View citing articles Show Details

Heitmann, Joerg; Cassel, Werner; Grote, Ludger; Bickel, Ulrich; Hartlaub, Udo; Penzel, Thomas; Peter, Joerg Hermann

Clinical Pharmacology and Therapeutics, 1999 , vol. 65, # 3 p. 328 - 335 Title/Abstract Full Text View citing articles Show Details

Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale

Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details

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Comment (Pharmacological Data)

Bioactivities present

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Comment (Pharmacological Data)

Bioactivities present

Reference

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Lopez; Arnulf; Drouot; Lecendreux; Dauvilliers

Revue Neurologique, 2017 , vol. 173, # 1-2 p. 8 - 18 Title/Abstract Full Text View citing articles Show Details

Harvanová, Marianna; Gondová, Taťána

Journal of Pharmaceutical and Biomedical Analysis, 2017 , vol. 138, p. 267 - 271 Title/Abstract Full Text View citing articles Show Details

Newsome, Scott D.; Aliotta, Philip J.; Bainbridge, Jacquelyn; Bennett, Susan E.; Cutter, Gary; Fenton, Kaylan; Lublin, Fred; Northrop, Dorothy; Rintell, David; Walker, Bryan D.; Weigel, Megan; Zackowski, Kathleen; Jones, David E.

International Journal of MS Care, 2017 , vol. 19, # 1 p. 42 - 56 Title/Abstract Full Text View citing articles Show Details

Touitou, Yvan; Reinberg, Alain; Touitou, David

Life Sciences, 2017 , vol. 173, p. 94 - 106 Title/Abstract Full Text View citing articles Show Details

Franke, Andreas G.; Gränsmark, Patrik; Agricola, Alexandra; Schühle, Kai; Rommel, Thilo; Sebastian, Alexandra; Balló, Harald E.; Gorbulev, Stanislav; Gerdes, Christer; Frank, Björn; Ruckes, Christian; Tüscher, Oliver; Lieb, Klaus

European Neuropsychopharmacology, 2017 , vol. 27, # 3 p. 248 - 260 Title/Abstract Full Text View citing articles Show Details

Nardone, Raffaele; Orioli, Andrea; Golaszewski, Stefan; Brigo, Francesco; Sebastianelli, Luca; Höller, Yvonne; Frey, Vanessa; Trinka, Eugen

Journal of Spinal Cord Medicine, 2017 , vol. 40, # 1 p. 8 - 16 Title/Abstract Full Text View citing articles Show Details

Jang, Sung Ho; Seo, Jeong Pyo

Medicine (United States), 2017 , vol. 96, # 7 art. no. E6103 Title/Abstract Full Text View citing articles Show Details

Ballester, Javier; Valentine, Gerald; Sofuoglu, Mehmet

Expert Review of Clinical Pharmacology, 2017 , vol. 10, # 3 p. 305 - 314 Title/Abstract Full Text View citing articles Show Details

Lopez, Régis; Barateau, Lucie; Evangelista, Elisa; Chenini, Sofiene; Robert, Philippe; Jaussent, Isabelle; Dauvilliers, Yves

Sleep, 2017 , vol. 40, # 1 Title/Abstract Full Text Show Details

Kaser, Muzaffer; Deakin, Julia B.; Michael, Albert; Zapata, Camilo; Bansal, Rachna; Ryan, Dragana; Cormack, Francesca; Rowe, James B.; Sahakian, Barbara J.

Biological Psychiatry: Cognitive Neuroscience and Neuroimaging, 2017 , vol. 2, # 2 p. 115 - 122 Title/Abstract Full Text View citing articles Show Details

Khalili-Mahani, Najmeh; Rombouts, Serge A. R. B.; van Osch, Matthias J. P.; Duff, Eugene P.; Carbonell, Felix; Nickerson, Lisa D.; Becerra, Lino; Dahan, Albert; Evans, Alan C; Soucy, Jean-Paul; Wise, Richard; Zijdenbos, Alex P.; van Gerven, Joop M.

Human Brain Mapping, 2017 , vol. 38, # 4 p. 2276 - 2325 Title/Abstract Full Text View citing articles Show Details

Krähenbüh, Stephan

Therapeutische Umschau, 2016 , vol. 73, # 11 p. 701 - 706 Title/Abstract Full Text Show Details

Rottoli, Mariarosa; La Gioia, Sara; Frigeni, Barbara; Barcella, Valeria

Expert Review of Neurotherapeutics, 2017 , vol. 17, # 4 p. 373 - 379 Title/Abstract Full Text Show Details

Kollb-Sielecka, Marta; Demolis, Pierre; Emmerich, Joseph; Markey, Greg; Salmonson, Tomas; Haas, Manuel

Sleep Medicine, 2017 , vol. 33, p. 125 - 129 Title/Abstract Full Text Show Details

Coulon, Philippe; Landisman, Carole E.

Neuron, 2017 , vol. 93, # 6 p. 1275 - 1295 Title/Abstract Full Text Show Details

Bennett, Trevor; Holloway, Katy


International Journal of Drug Policy, 2017 , vol. 44, p. 12 - 22 Title/Abstract Full Text Show Details

Nicholson, Paul J.; Wilson, Nigel

British Journal of General Practice, 2017 , vol. 67, # 656 p. 100 - 101 Title/Abstract Full Text Show Details

Liu, Feng; Wang, Xuefeng

Expert Review of Neurotherapeutics, 2017 , vol. 17, # 5 p. 475 - 485 Title/Abstract Full Text Show Details

Gan, Shaoyan; Yin, Junjie; Yao, Yuan; Liu, Yang; Chang, Denghu; Zhu, Dan; Shi, Lei

Organic and Biomolecular Chemistry, 2017 , vol. 15, # 12 p. 2647 - 2654 Title/Abstract Full Text Show Details

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Comment (Pharmacological Data)

Bioactivities present

Reference

Dowling, Geraldine; Kavanagh, Pierce V.; Talbot, Brian; O’Brien, John; Hessman, Gary; McLaughlin, Gavin; Twamley, Brendan; Brandt, Simon D.

Drug Testing and Analysis, 2017 , vol. 9, # 3 p. 518 - 528 Title/Abstract Full Text Show Details

Brandt, Simon D.; Kavanagh, Pierce V.

Drug Testing and Analysis, 2017 , vol. 9, # 3 p. 342 - 346 Title/Abstract Full Text Show Details

Kolderová, Natalie; Neveselý, Tomáš; Šturala, Jiří; Kuchař, Martin; Holakovský, Roman; Kohout, Michal

Chromatographia, 2017 , vol. 80, # 4 p. 547 - 557 Title/Abstract Full Text Show Details

Heersmink, Richard

Phenomenology and the Cognitive Sciences, 2017 , vol. 16, # 1 p. 17 - 32 Title/Abstract Full Text Show Details

Matoulek, Martin; Tuka, Vladimír; Fialová, Magdalena; Nevšímalová, Soňa; Šonka, Karel

Sleep Medicine, 2017 , vol. 34, p. 7 - 12 Title/Abstract Full Text Show Details

Johnson, Adrian; Hamilton, Trevor James

PeerJ, 2017 , vol. 2017, # 2 art. no. E2994 Title/Abstract Full Text Show Details

Inamoto, Yoshihiro; Lee, Stephanie J.

Haematologica, 2017 , vol. 102, # 4 p. 614 - 625 Title/Abstract Full Text Show Details

FECHTER, Cary Erwin

Patent: WO2016/209765 A1, 2016 ; Title/Abstract Full Text Show Details

Weiergräber, Marco; Ehninger, Dan; Broich, Karl

Medizinische Monatsschrift fur Pharmazeuten, 2017 , vol. 40, # 4 p. 154 - 166 Title/Abstract Full Text Show Details

Sim, Juhyun; Kim, Eunmi; Yang, Wonkyung; Woo, Sanghee; In, Sangwhan

Forensic Science International, 2017 , vol. 274, p. 91 - 98 Title/Abstract Full Text Show Details

Hodges, Sarah E.; Pittman, Brian; Morgan, Peter T.

Sleep, 2017 , vol. 40, # 3 art. no. ZSW069 Title/Abstract Full Text Show Details

Shin, Eun-Joo; Dang, Duy-Khanh; Tran, The-Vinh; Tran, Hai-Quyen; Jeong, Ji Hoon; Nah, Seung-Yeol; Jang, Choon-Gon; Yamada, Kiyofumi; Nabeshima, Toshitaka; Kim, Hyoung-Chun

Archives of Pharmacal Research, 2017 , vol. 40, # 4 p. 403 - 428 Title/Abstract Full Text Show Details

Kahn, René S.; Sommer, Iris E.; Murray, Robin M.; Meyer-Lindenberg, Andreas; Weinberger, Daniel R.; Cannon, Tyrone D.; O'Donovan, Michael; Correll, Christoph U.; Kane, John M.; Van Os, Jim; Insel, Thomas R.

Nature Reviews Disease Primers, 2015 , vol. 1, art. no. 15067 Title/Abstract Full Text Show Details

Sergeeva, Olga A.; De Luca, Roberto; Mazur, Karolina; Chepkova, Aissa N.; Haas, Helmut L.; Bauer, Andreas

Neuropharmacology, 2017 , vol. 119, p. 111 - 122 Title/Abstract Full Text Show Details

Hoffmann, Anika; Müller, Hermann L.

Minerva Endocrinologica, 2017 , vol. 42, # 2 p. 132 - 144 Title/Abstract Full Text Show Details

Wolf, Carl E.; Poklis, Justin L.; Cumpston, Kirk; Moss, Michael; Poklis, Alphonse

Drug Testing and Analysis, 2017 , vol. 9, # 4 p. 657 - 659 Title/Abstract Full Text Show Details

Punzi, Miriam; Gili, Tommaso; Petrosini, Laura; Caltagirone, Carlo; Spalletta, Gianfranco; Sensi, Stefano L.

Frontiers in Aging Neuroscience, 2017 , vol. 9, # MAR art. no. 85 Title/Abstract Full Text Show Details

Fayette; Gahérová; Móciková; Marková; Kozák; Horáček

Klinicka Onkologie, 2017 , vol. 30, # 2 p. 93 - 99 Title/Abstract Full Text Show Details

Drugs and Therapy Perspectives, 2017 , vol. 33, # 5 p. 222 - 226 Title/Abstract Full Text Show Details

Lashch; Boiko

Nevrologiya, Neiropsikhiatriya, Psikhosomatika, 2016 , vol. 8, # 1 p. 82 - 85 Title/Abstract Full Text Show Details

24 of 150

Comment (Pharmacological Data)

Bioactivities present

Reference

Mohammed, Zeid; Grunze, Heinz

Neuropsychiatry, 2016 , vol. 6, # 3 p. 96 - 111 Title/Abstract Full Text Show Details

Black, Sarah Wurts; Yamanaka, Akihiro; Kilduff, Thomas S.


Progress in Neurobiology, 2017 , vol. 152, p. 89 - 113 Title/Abstract Full Text Show Details

Grabb, Margaret C.; Gobburu, Jogarao V.S.

Progress in Neurobiology, 2017 , vol. 152, p. 38 - 57 Title/Abstract Full Text Show Details

Lazuras, Lambros; Ypsilanti, Antonia; Lamprou, Efthymios; Kontogiorgis, Christos

Substance Use and Misuse, 2017 , vol. 52, # 7 p. 950 - 958 Title/Abstract Full Text Show Details

Everts, Sarah

Chemical and Engineering News, 2017 , vol. 95, # 12 p. 25 - 26 Title/Abstract Full Text Show Details

Morley, Kirsten C.; Cornish, Jennifer L.; Faingold, Alon; Wood, Katie; Haber, Paul S.

Expert Opinion on Investigational Drugs, 2017 , vol. 26, # 5 p. 563 - 578 Title/Abstract Full Text Show Details

West, Caroline; Konjaria, Mari-Luiza; Shashviashvili, Natia; Lemasson, Elise; Bonnet, Pascal; Kakava, Rusudan; Volonterio, Alessandro; Chankvetadze, Bezhan

Journal of Chromatography A, 2017 , vol. 1499, p. 174 - 182 Title/Abstract Full Text Show Details

Lu, Cong; Shi, Zhe; Dong, Liming; Lv, Jingwei; Xu, Pan; Li, Yinghui; Qu, Lina; Liu, Xinmin

Phytotherapy Research, 2017 , vol. 31, # 5 p. 763 - 770 Title/Abstract Full Text Show Details

Bivard, Andrew; Lillicrap, Thomas; Krishnamurthy, Venkatesh; Holliday, Elizabeth; Attia, John; Pagram, Heather; Nilsson, Michael; Parsons, Mark; Levi, Christopher R.

Stroke, 2017 , vol. 48, # 5 p. 1293 - 1298 Title/Abstract Full Text Show Details

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Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Krasulova, Kristyna; Siller, Michal; Holas, Ondrej; Dvorak, Zdenek; Anzenbacher, Pavel

Xenobiotica, 2016 , vol. 46, # 4 p. 315 - 324 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Saroja, Sivaprakasam R.; Aher, Yogesh D.; Kalaba, Predrag; Aher, Nilima Y.; Zehl, Martin; Korz, Volker; Subramaniyan, Saraswathi; Miklosi, Andras G.; Zanon, Lisa; Neuhaus, Winfried; Höger, Harald; Langer, Thierry; Urban, Ernst; Leban, Johann; Lubec, Gert

Behavioural Brain Research, 2016 , vol. 312, p. 127 - 137 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Martínez-Guerrero, Lucy J.; Morales, Mark; Ekins, Sean; Wright, Stephen H.

Molecular Pharmacology, 2016 , vol. 90, # 3 p. 254 - 264 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

SK Biopharmaceuticals Co., Ltd.; Khayrallah, Moise A.; Bream, Gary; Butts, Stephen E.; Melnick, Susan Marie; Taylor, Duncan

Patent: US9464041 B2, 2016 ; Title/Abstract Full Text Show Details

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Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Cao, Jianjing; Slack, Rachel D.; Bakare, Oluyomi M.; Burzynski, Caitlin; Rais, Rana; Slusher, Barbara S.; Kopajtic, Theresa; Bonifazi, Alessandro; Ellenberger, Michael P.; Yano, Hideaki; He, Yi; Bi, Guo-Hua; Xi, Zheng-Xiong; Loland, Claus J.; Newman, Amy Hauck

Journal of Medicinal Chemistry, 2016 , vol. 59, # 23 p. 10676 - 10691 Title/Abstract Full Text View citing articles Show Details

Location

Paragraph

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

FECHTER, Cary Erwin

Patent: WO2016/209765 A1, 2016 ; Title/Abstract Full Text Show Details

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Location

Page/Page column

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details


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Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Zolkowska, Dorota; Andres-Mach, Marta; Prisinzano, Thomas E.; Baumann, Michael H.; Luszczki, Jarogniew J.

Psychopharmacology, 2015 , vol. 232, # 14 art. no. 3884, p. 2463 - 2479 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Okunola-Bakare, Oluyomi M.; Cao, Jianjing; Kopajtic, Theresa; Katz, Jonathan L.; Loland, Claus J.; Shi, Lei; Newman, Amy Hauck

Journal of Medicinal Chemistry, 2014 , vol. 57, # 3 p. 1000 - 1013 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES; NEWMAN, Amy Hauck; OKUNOLA-BAKARE, Oluyomi M.; CAO, Jianjing

Patent: WO2014/138518 A2, 2014 ; Title/Abstract Full Text Show Details

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Comment (Pharmacological Data)

physiological behaviour discussed

Reference

EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION; Suh, Suk Hyo; Jung, Jae Chul; Oh, Sei Kwan

Patent: US2014/296333 A1, 2014 ; Title/Abstract Full Text Show Details

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Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Gonzlez, Betina; Raineri, Mariana; Cadet, Jean Lud; Garca-Rill, Edgar; Urbano, Francisco J.; Bisagno, Veronica

Neuropharmacology, 2014 , vol. 87, p. 188 - 197 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

rat

Route of Application

intraperitoneal

Type (Pharmacological Data)

wake 3 h AUC

Value of Type (Pharmacological Data)

117 min

Reference

Lesur, Brigitte; Lin, Yin G.; Marcy, Val R.; Aimone, Lisa D.; Gruner, John; Bacon, Edward R.; Chatterjee, Sankar

Chemical Biology and Drug Design, 2013 , vol. 81, # 3 p. 429 - 432 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

rat

Route of Application

intraperitoneal

Type (Pharmacological Data)

wake 4 h AUC

Value of Type (Pharmacological Data)

117 min

Reference

Lesur, Brigitte; Lin, Yin G.; Marcy, Val R.; Aimone, Lisa D.; Gruner, John; Bacon, Edward R.; Chatterjee, Sankar

Chemical Biology and Drug Design, 2013 , vol. 81, # 3 p. 429 - 432 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transporter binding

Species or Test-System (Pharmacological Data)

not explicitly stated by authors

Further Details (Pharmacological Data)

inhibitory concentration (IC); IC50 related to: dopamine transporter


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Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

3.7 μmol/l

Reference

Lesur, Brigitte; Lin, Yin G.; Marcy, Val R.; Aimone, Lisa D.; Gruner, John; Bacon, Edward R.; Chatterjee, Sankar

Chemical Biology and Drug Design, 2013 , vol. 81, # 3 p. 429 - 432 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transporter binding

Species or Test-System (Pharmacological Data)

not explicitly stated by authors

Results

molecular target: dopamine transporter; species of target: rat

Reference

Lesur, Brigitte; Lin, Yin G.; Marcy, Val R.; Aimone, Lisa D.; Gruner, John; Bacon, Edward R.; Chatterjee, Sankar

Chemical Biology and Drug Design, 2013 , vol. 81, # 3 p. 429 - 432 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

De Bruyn, Tom; Van Westen, Gerard J.P.; IJzerman, Adriaan P.; Stieger, Bruno; De Witte, Peter; Augustijns, Patrick F.; Annaert, Pieter P.

Molecular Pharmacology, 2013 , vol. 83, # 6 p. 1257 - 1267 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

rat

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

100 mg/kg

Kind of Dosing (Pharmacological Data)

title compound administered for 4h

Further Details (Pharmacological Data)

wake promotion assay

Type (Pharmacological Data)

AUC

Value of Type (Pharmacological Data)

117 min

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2315 - 2317 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme activity; inhibition of

Species or Test-System (Pharmacological Data)

not explicitly stated by authors

Concentration (Pharmacological Data)

10 μmol/l

Further Details (Pharmacological Data)

inhibition rate related to: CYP 2D6

Type (Pharmacological Data)

inhibition rate

Value of Type (Pharmacological Data)

< 10 percent

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme activity; inhibition of

Species or Test-System (Pharmacological Data)

not explicitly stated by authors


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Concentration (Pharmacological Data)

10 μmol/l

Further Details (Pharmacological Data)

inhibition rate related to: CYP 3A4

Type (Pharmacological Data)

inhibition rate

Value of Type (Pharmacological Data)

< 10 percent

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme activity; inhibition of

Species or Test-System (Pharmacological Data)

not explicitly stated by authors

Further Details (Pharmacological Data)

IC50 related to: CYP 2C19

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

11 μmol/l

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme activity; inhibition of

Species or Test-System (Pharmacological Data)

not explicitly stated by authors

Results

molecular target: CYP 2C19

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

100 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. in 0.5percent methylcellulose/0.2percent tween-80 in distilled water

Further Details (Pharmacological Data)

rat wake promotion assay; PDP value observed 3h after dosing

Type (Pharmacological Data)

AUC

Value of Type (Pharmacological Data)

117 min

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

liver of human

Further Details

human liver S9 metabolism assay; PDP value observed at 2h; parent remaining related to: liver


(Pharmacological Data)

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Type (Pharmacological Data)

parent remaining

Value of Type (Pharmacological Data)

77 percent

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein binding affinity

Species or Test-System (Pharmacological Data)

not explicitly stated by authors

Further Details (Pharmacological Data)

IC50 related to: rat dopamine transporter

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

3.7 μmol/l

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein binding affinity

Species or Test-System (Pharmacological Data)

not explicitly stated by authors

Results

molecular target: rat dopamine transporter

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein uptake; inhibition of

Species or Test-System (Pharmacological Data)

not explicitly stated by authors

Further Details (Pharmacological Data)

IC50 related to: SERT

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

> 300 μmol/l

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein uptake; inhibition of

Species or Test-System (Pharmacological Data)

not explicitly stated by authors

Further Details (Pharmacological Data)

IC50 related to: rat dopamine transporter

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

4.3 μmol/l

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details


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Effect (Pharmacological Data)

protein uptake; inhibition of

Species or Test-System (Pharmacological Data)

not explicitly stated by authors

Further Details (Pharmacological Data)

IC50 related to: rat norepinephrine transporter

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

63.9 μmol/l

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein uptake; inhibition of

Species or Test-System (Pharmacological Data)

not explicitly stated by authors

Results

molecular target: rat dopamine transporter

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein uptake; inhibition of

Species or Test-System (Pharmacological Data)

not explicitly stated by authors

Results

molecular target: rat norepinephrine transporter

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme activity; inhibition of

Species or Test-System (Pharmacological Data)

not explicitly stated by authors

Further Details (Pharmacological Data)

IC50 related to: CYP2C19

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

11 μmol/l

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Marcy, Val R.; Lin, Yin Guo; Jones, Bruce; Aimone, Lisa D.; Gruner, John; Ator, Mark A.; Bacon, Edward R.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3751 - 3753 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme activity; inhibition of

Species or Test-System (Pharmacological Data)

not explicitly stated by authors

Results

molecular target: CYP2C19

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Marcy, Val R.; Lin, Yin Guo; Jones, Bruce; Aimone, Lisa D.; Gruner, John; Ator, Mark A.; Bacon, Edward R.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3751 - 3753 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

rat

Route of Application

intraperitoneal


59 of 150

60 of 150

61 of 150

62 of 150

Concentration (Pharmacological Data)

100 mg/kg

Further Details (Pharmacological Data)

wake-promoting activity over 3 h was measured; wake promotion assay

Type (Pharmacological Data)

AUC

Value of Type (Pharmacological Data)

117 min

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Marcy, Val R.; Lin, Yin Guo; Jones, Bruce; Aimone, Lisa D.; Gruner, John; Ator, Mark A.; Bacon, Edward R.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3751 - 3753 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein binding affinity

Species or Test-System (Pharmacological Data)

striata of rat

Further Details (Pharmacological Data)

DAT binding assay; DAT: dopamine transporter

Results

molecular target: dopamine transporter

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Marcy, Val R.; Lin, Yin Guo; Jones, Bruce; Aimone, Lisa D.; Gruner, John; Ator, Mark A.; Bacon, Edward R.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3751 - 3753 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein binding affinity

Species or Test-System (Pharmacological Data)

striata of rat

Further Details (Pharmacological Data)

DAT binding assay; DAT: dopamine transporter; IC50 related to: dopamine transporter

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

3.7 μmol/l

Reference

Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Marcy, Val R.; Lin, Yin Guo; Jones, Bruce; Aimone, Lisa D.; Gruner, John; Ator, Mark A.; Bacon, Edward R.; Chatterjee, Sankar

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3751 - 3753 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

wake-promoting

Species or Test-System (Pharmacological Data)

rat

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

100 mg/kg

Further Details (Pharmacological Data)

for control total awake time over 3 h was 65 min

Type (Pharmacological Data)

total awake time over 3 h (AUC)

Value of Type (Pharmacological Data)

117 min

Reference

Louvet, Philippe; Schweizer, Dominique; Gourdel, Marie-Edith; Riguet, Eric; Yue, Christoph; Marcy, Val R.; Lin, Yin Guo; Gruner, John; Lesur, Brigitte; Bacon, Edward R.; Chatterjee, Sankar

European Journal of Medicinal Chemistry, 2012 , vol. 54, p. 949 - 951 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

wake-promoting

Species or Test-System (Pharmacological Data)

rat

Route of Application

intraperitoneal

Concentration

100 mg/kg


(Pharmacological Data)

63 of 150

64 of 150

65 of 150

66 of 150

67 of 150

Further Details (Pharmacological Data)

for control total awake time over 3 h was 79.2 min

Type (Pharmacological Data)

total awake time over 3 h (AUC)

Value of Type (Pharmacological Data)

117 min

Reference

Louvet, Philippe; Schweizer, Dominique; Gourdel, Marie-Edith; Riguet, Eric; Yue, Christoph; Marcy, Val R.; Lin, Yin Guo; Gruner, John; Lesur, Brigitte; Bacon, Edward R.; Chatterjee, Sankar

European Journal of Medicinal Chemistry, 2012 , vol. 54, p. 949 - 951 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

monoamine transporter binding affinity

Species or Test-System (Pharmacological Data)

brain membranes of rat

Further Details (Pharmacological Data)

Ki related to: dopamine transporter

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

2520 nmol/l

Reference

Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck

ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

monoamine transporter binding affinity

Species or Test-System (Pharmacological Data)

brain membranes of rat

Results

molecular target: dopamine transporter

Reference

Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck

ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

locomotor activity; effect on

Species or Test-System (Pharmacological Data)

mouse

Concentration (Pharmacological Data)

100 - 560 mg/kg

Type (Pharmacological Data)

maximal locomotor activity

Value of Type (Pharmacological Data)

500 counts/min

Reference

Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck

ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

locomotor activity; effect on

Species or Test-System (Pharmacological Data)

mouse

Concentration (Pharmacological Data)

100 - 560 mg/kg

Type (Pharmacological Data)

dose for maximal activity

Value of Type (Pharmacological Data)

300 mg/kg

Reference

Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck

ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological

locomotor activity; effect on


Data)

68 of 150

69 of 150

70 of 150

Species or Test-System (Pharmacological Data)

mouse

Concentration (Pharmacological Data)

100 - 560 mg/kg

Type (Pharmacological Data)

time for maximal activity

Value of Type (Pharmacological Data)

1 h

Reference

Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck

ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transporter; inhibition of

Species or Test-System (Pharmacological Data)

HEK293-Flp-In cells; genetically modified/infected with: human OCT2

Concentration (Pharmacological Data)

20 μmol/l

Kind of Dosing (Pharmacological Data)

title comp. dissolved in DMSO

Further Details (Pharmacological Data)

OCT2: organic cation transporter 2 (solute carrier 22A2); HEK: human embryonic kidney; fluorescent probe substrate: 4-(4-(dimethylamino)styryl)-N-methyl-pyridinium (ASP+) (5 μmol/l); high-throughput assay; fluorimetry; inhibition rate related to: OCT2

Type (Pharmacological Data)

inhibition rate

Value of Type (Pharmacological Data)

18.3 percent

Location

supporting information

Reference

Kido, Yasuto; Matsson, Paer; Giacomini, Kathleen M.

Journal of Medicinal Chemistry, 2011 , vol. 54, # 13 p. 4548 - 4558 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transporter; inhibition of

Species or Test-System (Pharmacological Data)

HEK293-Flp-In cells; genetically modified/infected with: human OCT2

Concentration (Pharmacological Data)

20 μmol/l

Kind of Dosing (Pharmacological Data)

title comp. dissolved in DMSO

Further Details (Pharmacological Data)

OCT2: organic cation transporter 2 (solute carrier 22A2); HEK: human embryonic kidney; fluorescent probe substrate: 4-(4-(dimethylamino)styryl)-N-methyl-pyridinium (ASP+) (5 μmol/l); high-throughput assay; fluorimetry

Results

molecular target: human OCT2

Location

supporting information

Reference

Kido, Yasuto; Matsson, Paer; Giacomini, Kathleen M.

Journal of Medicinal Chemistry, 2011 , vol. 54, # 13 p. 4548 - 4558 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

cocaine substitution

Species or Test-System (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

<= 300 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in 5percent arabic gum solution; admin. as salt

Further Details (Pharmacological Data)

title comp. engenders cocaine-appropriate responding with 90.2percent substitution at 300 mg/kg; effective dose (ED)

Type (Pharmacological Data)

ED50


71 of 150

72 of 150

73 of 150

Value of Type (Pharmacological Data)

95.96 mg/kg

Reference

Paterson, Neil E.; Fedolak, Allison; Olivier, Berend; Hanania, Taleen; Ghavami, Afshin; Caldarone, Barbara

Pharmacology Biochemistry and Behavior, 2010 , vol. 95, # 4 p. 449 - 456 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme activity; inhibition of

Species or Test-System (Pharmacological Data)

fatty acid amide hydrolase of human

Concentration (Pharmacological Data)

1 μmol/l

Type (Pharmacological Data)

percent inhibition

Value of Type (Pharmacological Data)

-1.68 percent

Location

supporting information

Reference

Vincent, Fabien; Nguyen, Margaret T.; Emerling, Daniel E.; Kelly, Michael G.; Duncton, Matthew A.J.

Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 23 p. 6793 - 6796 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme activity; inhibition of

Species or Test-System (Pharmacological Data)

fatty acid amide hydrolase of human

Concentration (Pharmacological Data)

1 μmol/l

Results

molecular target: fatty acid amide hydrolase

Location

supporting information

Reference

Vincent, Fabien; Nguyen, Margaret T.; Emerling, Daniel E.; Kelly, Michael G.; Duncton, Matthew A.J.

Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 23 p. 6793 - 6796 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

delayed ejaculation; effect on

Species or Test-System (Pharmacological Data)

human

Route of Application

peroral

Method (Pharmacological Data)

Example 1. Delayed ejaculation with sublingually administered d-modafinil.The synthesis of (d)-(+)-modafinil has been described in the literature (see, e.g., Prisinzano et al., Tetrahedron Asymmetry, 15: 1053-1058 (2004); US Patent No. 4,927,855 ("Lafon synthesis"))- In accordance with the Lafon synthesis, the intermediate carboxylic acid was converted to the diastereomic salt mixture with (+) alpha-methylbenzylamine. The diastereomers were separated, and the appropriate chiral acid liberated from the salt form. The acid was converted to the methyl ester via esterification and reacted with ammonia/methanol solution to yield d-modafinil. The enantiomeric purity was in excess of 98percent-99percent.Initial formulation tests of modafinil (racemate) and pure d-modafinil revealed a bitter taste. Therefore, the pharmaceutical formulation included one or more taste-masking ingredients. The d-modafinil was mixed with various taste-masking agents, including pulverized mints, breath fresheners, and natural and artificial flavorings. The synthesized d-modafinil was compounded into a composition containing sugar, spearmint flavor, cinnamon flavor, gum arabic, gelatin, corn syrup, and dyes that could be administered sublingually. Formulations containing 100 mg of d-modafinil were prepared. Subject 1 took the above-described formulation of d-modafinil sublingually at 9:00 pm in the course of testing a composition containing d-modafinil for a different effect unrelated to sexual activity. Subject 1 reported that unexpectedly the time to ejaculate during sexual activity was significantly longer than usual by a factor of about two to three times. A week later, Subject 1 took the formulation sublingually for a second time and, again, reported that the time to ejaculate during sexual intercourse was significantly delayed by a factor of approximately two to three times.The data demonstrate that sublingual administration of d-modafinil can provide a desirable delay of ejaculation during sexual activity, that the effect is drug-dependent, and that the effect is reversible.

Results

delay in ejaculation during sexual activity was experienced by patients treated with 200 mg of the title compound

Location

Page/Page column 19-20

Reference

NEUROHEALING PHARMACEUTICALS, INC.

Patent: WO2008/21341 A2, 2008 ; Title/Abstract Full Text Show Details

74 of 150

Effect (Pharmacological Data)

transmitter releasing

Species or Test-System (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intraperitoneal

Concentration

75 - 150 mg/kg


(Pharmacological Data)

75 of 150

76 of 150

77 of 150

Kind of Dosing (Pharmacological Data)

suspended in 0.3percent carboxymethylcellulose (CMC) in saline

Method (Pharmacological Data)

hypothalamic histamine release in freely moving rats examined using in vivo microdialysis; dialysate samples collected every 20 min for 3 h after title comp. injection and assayed for histamine by high performance chromatography-fluometric method

Further Details (Pharmacological Data)

control: 0.3percent CMC; reference comp.: methylphenidate (3 mg/kg, i.p.)

Results

title comp. increased histamine release immediately after administration with gradual reduction within 1 h and 2 h at low and high doses, respectively; methylphenidate had no effect; fig.

Reference

Ishizuka, Tomoko; Murakami, Masahiro; Yamatodani, Atsushi

European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 209 - 215 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or Test-System (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

75 - 150 mg/kg

Kind of Dosing (Pharmacological Data)

suspended in 0.3percent carboxymethylcellulose (CMC) in saline

Method (Pharmacological Data)

locomotor activity counts automatically recorded in 20-min bins by infrared sensor for 3 h after title comp. administration

Further Details (Pharmacological Data)

control: 0.3percent CMC; reference comp.: methylphenidate (3 mg/kg, i.p.)

Results

title comp. increased locomotor activity immediately after administration to 300percent and 600percent at low and high doses, respectively; at high dose effect was similar to methylphenidate; fig.

Reference

Ishizuka, Tomoko; Murakami, Masahiro; Yamatodani, Atsushi

European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 209 - 215 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or Test-System (Pharmacological Data)

C57BL mouse

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

150 mg/kg

Kind of Dosing (Pharmacological Data)

suspended in 0.3percent carboxymethylcellulose (CMC) in saline

Method (Pharmacological Data)

locomotor activity counts automatically recorded every 20 min by infrared sensor until 4 h after title comp. administration; testing carried out during the light phase

Further Details (Pharmacological Data)

further investigation on mechanism of action using depletion of neuronal histamine through pretreatment with α-fluoromethylhistidine; control: 0.3percent CMC; reference comp.: methylphenidate (20 mg/kg, i.p.)

Results

title comp. increased locomotor activity similarly to methylphenidate; mechanism of action of title comp. (but not methylphenidate) involved activation of central histaminergic system; fig.

Reference

Ishizuka, Tomoko; Murakami, Masahiro; Yamatodani, Atsushi

European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 209 - 215 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or Test-System (Pharmacological Data)

C57BL mouse

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

150 mg/kg

Kind of Dosing

suspended in 0.3percent carboxymethylcellulose (CMC) in saline


(Pharmacological Data)

78 of 150

Method (Pharmacological Data)

cumulative counts of locomotor activity automatically recorded by infrared sensor during 2 h after title comp. administration at 00:00 the active period of mice (dark phase) or at the light phase

Further Details (Pharmacological Data)

control: 0.3percent CMC; reference comp.: methylphenidate (20 mg/kg, i.p.)

Results

title comp. increased locomotor activity similarly to methylphenidate after administration at the light phase; after treatment at dark phase title comp. was less potent than methylphenidate; fig.

Reference

Ishizuka, Tomoko; Murakami, Masahiro; Yamatodani, Atsushi

European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 209 - 215 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

sleep movement disorders; effect on

Species or Test-System (Pharmacological Data)

non-obese with periodic limb movement disorder (PLMD), restless leg syndrome (RLS) without apnea and primary snoring of human

Sex

female

Route of Application

peroral

Method (Pharmacological Data)

Example 2. Subject Administered 50 mg of ModafinilA 53 year old non-obese female, 61 kg, with sleep study diagnosed PLMD with RLS without apnea, and Primary snoring, took modafinil 50 mg by mouth between 8 am and noon. No urge to move legs in the evenings occurred and no leg jerks during sleep were observed by her partner. The patient noted increased restfulness and her partner noticed an absence of .imb movements and snoring while asleep. Example 3. Subject Administered 100 mg of ModafinilA 53 year old non-obese female, 61 kg, with sleep study diagnosed PLMD with RLS without apnea and Primary snoring, took modafinil 100 mg by mouth in the morning. No urge to move legs in the evenings occurred and no leg jerks during sleep were observed by her partner. The patient noted increased restfulness and her partner noticed an absence of limb movements and snoring while asleep.Example 4. Continuous use evening dosageA 54 year old non-obese female, 61 kg, with sleep study diagnosedPLMD with RLS without apnea and Primary snoring, took modafinil 50 mg by mouth 1-3 hours prior to bedtime. Limb movements and the urge to move the limb and associated sensations while awake were greatly reduced after approximately 90 minutes. The patient then took 25 mg of modafiniS as needed and noted that symptoms were either completely relieved or greatly diminished. Chronic use every day for periods of 5 to 7 days produced periods free from RLS and PLMD symptoms, which returned immediately after stopping the drug.

Results

title compound treatment at 50 and 100 mg between 8 am and noon and in the morning, respectively, showed no urge to move legs in the evenings occurred and no leg jerks during sleep were observed by her partner; increased restfulness was noted by the patient and her partner noticed an absence of limb movements and snoring while asleep; treatment with 50 mg title compound 1-3 hours prior to bedtime showed great reduction of limb movement, the urge to move the limb and associated (comment)

Location

Page/Page column 8-9

Reference

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

79 of 150

Effect (Pharmacological Data)

sleep movement disorders; effect on

Species or Test-System (Pharmacological Data)

non-obese with periodic limb movement disorder (PLMD), restless leg syndrome (RLS) with apnea and primary snoring of human

Sex

female

Route of Application

peroral

Method (Pharmacological Data)

Example 5. Continuous use morning dosage A 53 year old non-obese female, 61 kg, with sleep study diagnosedPLMD with RLS with apnea and Primary snoring, took modafinil 50 mg or 25 mg by mouth in the morning. Limb movements and the urge to move the limb and associated sensations while awake were greatly reduced. The lower dosage of 25 mg failed to entirely remove symptoms. Either 50 mg or 25 mg was used intermittently for a period of 14 months. Chronic use every day for periods of up to 11 days produced periods free from RLS and PLMD symptoms, which returned immediately after stopping the drug. The sleep partner noted a marked decrease in snoring.

Results

title compound treatment at 50 mg and 25 mg in the morning showed great reduction in limb movements, the urge to move the limb and associated sensations while awake; lower dosage of 25 mg title compound failed to entirely remove symptoms; chronic use every day for periods up to 11 days produced periods free from RLS and PLMD symptoms, which returned immediately after stopping the drug; decrease in snoring was observed by the sleeping partner

Location

Page/Page column 9

Reference

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

80 of 150

Effect (Pharmacological Data)

sleep movement disorders; effect on

Species or Test-System (Pharmacological Data)

non-obese with restless leg syndrome (RLS), periodic limb movement in sleep (PLMS) and primary snoring of human

Sex

female

Route of Application

peroral

Method (Pharmacological Data)

Example 6. Sleep Study Results, evening dosageA non-obese female subject with no outstanding medical history other than restless leg syndrome and PLMS of 6 years duration, and Primary snoring, age 54, 60 kg, was entered into an overnight sleep study in a specialist hospital sleep disorder center. Subject was monitored by polysomnography recording method identifying sleep stages and their durations, detection and measurements of apneas, detection and measurement of PLM (periodic limb movements, snoring and measurement of pψ2, heart rate and arterial pressure. Sleep stages were identified using electroencephalograph^ and electromyographic recording. Oxygen saturation was measured by transcutaneous oximetric measurement and revealed no apnea. Baseline studies without drug administration showed that


the subject exhibited multiple PLMs during sleep and significant snoring episodes. After oral administration of 50 mg modafinil in the evening PLMs were not detected during sleep as illustrated in Drawing 1. Snoring as represented by the Snore Index was reduced 70percent Results

title compound tretament at 50 mg reduced snoring by 70percent as represented by the snore index score, however, periodic limb movements (PLMs) were not detected; figure is given

Location

Page/Page column title page; 4; 9; 1/1

Reference

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

81 of 150

Effect (Pharmacological Data)

H-reflex frequency dependent depression; restoration of

Species or Test-System (Pharmacological Data)

Sprague-Dawley rat

Sex

female

Route of Application

peroral

Method (Pharmacological Data)

Section 3Modafinil Restored Frequency Dependent Depression of the H-Reflex in Spinally Transected RatsMethods:Rats were spinally transected as in Section 1 of this Example. One group of rats received no exercise after transection. A second group of rats was treated with passive exercise using the motorized bicycle exercise trainer, as in Section 1. Passive exercise was begun within 7 days of transection. A third group of transected rats were not exercised but were given 3 mg/Kg modafinil per day. A 100 mg modafinil pill was ground by mortar and pestle and mixed with 9 ml of syrup and 1 ml of water. The dose to the animal was 0.1 ml p.o. daily (3 mg/Kg/day). Modafinil was started between 48 hours and 7 days after transection. A fourth group of rats was untransected normal controls. Each group contained 9 to 12 rats.At 30 days after transection, the H-reflex of each rat was measured as in Section 1.Results:The H-reflex of the four groups of rats was measured at 30 days after transection at stimulation frequencies from 0.2 to 10 Hz. The four groups of rats were normal controls (control), transected and untreated for 30 days after transection (Tx-30), transected and treated solely with 3 mg/Kg/day modafinil p.o. for 30 days (Mod), and transected and treated solely with passive exercise for 30 days (MBET 30). The results are shown in FIG. D1.FIG. 6 shows that as you increase the stimulation for 0.2 to 10 Hz, the H-reflex amplitude in intact rats (control) decreases markedly. In rats that were transected and tested 30 days after surgery (Tx-30), the amplitude of the reflex did not habituate-that is, there was hyper-reflexia. In rats that were transected and MBET begun within 7 days after surgery and exercised for 30 days (MBET 30), the reflex amplitude decreased as in intact animals, indicating that passive exercise led to a normalization of the hyper-reflexia. In animals that were transected and not exercised but given daily doses of modafinil beginning 7 days after surgery (Mod), the reflexes were normalized, indicating that modafinil also alleviated hyper-reflexia.Hyper-reflexia is a component of spasticity, so that normalization of hyper-reflexia indicates a reduction or elimination of spasticity. These studies demonstrated that oral administration of modafinil, which is used to promote waking in narcoleptic subjects, was effective in reducing hyper-reflexia after spinal transection

Results

title compound administration at 3 mg/kg/day normalized the reflexes of the transected mouse; figure is given

Location

Page/Page column 2; 6-7; Sheet 6

Reference

The Board of Trustees of the University of Arkansas

Patent: US2008/221216 A1, 2008 ; Title/Abstract Full Text Show Details

82 of 150

Effect (Pharmacological Data)

neuronal differentiation; stimulation of

Species or Test-System (Pharmacological Data)

neural stem cells (hNSCs) of human

Method (Pharmacological Data)

FIG. 9 is a dose-response curve showing effect of the neurogenic agents MKC-231 and modafinil (adrenergic agonist) in combination on neuronal differentiation of human neural stem cells compared to the effect of either agent alone. When run independently, each compound was tested in a concentration response curve ranging from 0.01 μM to 31.6 μM. In combination, the compounds were combined at equal concentrations at each point (for example, the first point in the combined curve consisted of a test of 0.01 μM MKC-231 and 0.01 μM modafinil). Data is presented as the percentage of the neuronal positive control, with basal media values subtracted. When used alone, EC50 was observed at an MKC-231 concentration of 8.6 μM or a modafinil concentration estimated to be 83 μM (based on extrapolation of the observed data). When used in combination, neurogenesis is greatly enhanced: EC50 was observed at a combination of MKC-231 and modafinil at concentrations of 1.1 μM each, resulting in a synergistic combination index of 0.14.; Example 8Effects of Modafinil in Combination with the MKC-231 on Differentiation of Human Neural Stem CellsHuman neural stem cells (hNSCs) were isolated and grown in monolayer culture, plated, treated with varying concentrations of MKC-231 in the presence or absence of modafinil, and stained with TUJ-1 antibody for the detection of neuronal differentiation as described in above. Mitogen-free test media with a positive control for neuronal differentiation was used along with basal media without growth factors as a negative control.Results are shown in FIG. 9, which shows concentration response curves of neuronal differentiation after background media values are subtracted. The concentration response curves of the combination of MKC-231 with modafinil are shown with the concentration response curves either agent alone. The data is presented as a percent of neuronal positive control. The data indicate that the combination of MKC-231 with modafinil resulted in synergistically enhanced neuronal differentiation relative to that that produced by either agent alone.

Type (Pharmacological Data)

EC50

Value of Type (Pharmacological Data)

83 μmol/l

Results

title compound dose-dependently increases neuronal differentiation at concentration from 0.01 to 31.6 μM; figure is given

Location

Page/Page column 3; 40-41; sheet 9

Reference

BrainCells, Inc.

Patent: US2008/64671 A1, 2008 ; Title/Abstract Full Text Show Details

83 of 150

Effect (Pharmacological Data)

neuroregulatoric

Species or Test-System (Pharmacological Data)

129Sv mouse


84 of 150

85 of 150

86 of 150

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

32 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in 20percent dimethylsulfoxide

Method (Pharmacological Data)

title comp. administered; polygraphic records performed within 14 h and scored by 30-s epochs for W, SWS and PS; W, SWS and PS amount as well as latencies to SWS and PS determined

Further Details (Pharmacological Data)

further investigation using HDC knockout mice; W: wakefulness; SWS: slow wave sleep; PS: paradoxical sleep; HDC: histidine decarboxylase

Results

title comp. increased W and decreased SWS and PS; this effect did not depend on HDC

Reference

Parmentier; Anaclet; Guhennec; Brousseau; Bricout; Giboulot; Bozyczko-Coyne; Spiegel; Ohtsu; Williams; Lin

Biochemical Pharmacology, 2007 , vol. 73, # 8 p. 1157 - 1171 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neuroregulatoric

Species or Test-System (Pharmacological Data)

129Sv mouse

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

32 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in 20percent dimethylsulfoxide

Method (Pharmacological Data)

title comp. administered; polygraphic records performed within 14 h and EEG power spectra recorded

Further Details (Pharmacological Data)

further investigation using HDC knockout mice; EEG: electroencephalogram; HDC: histidine decarboxylase

Results

title comp. suppressed cortical slow activity (δ and slow ψ); this effect did not depend on HDC

Reference

Parmentier; Anaclet; Guhennec; Brousseau; Bricout; Giboulot; Bozyczko-Coyne; Spiegel; Ohtsu; Williams; Lin

Biochemical Pharmacology, 2007 , vol. 73, # 8 p. 1157 - 1171 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or Test-System (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

32 - 128 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. (Provigil, Alertec and Vigiler) dissolved in water containing 0.1percent DMSO and adminisered via gavage at a volume of 1 ml/kg

Method (Pharmacological Data)

rats trained to discriminate cocaine/amphetamine from saline injection for delivery of food pellet; admin. with title comp.; response rates determined after 10-240 min delay

Further Details (Pharmacological Data)

control: vehicle

Results

title comp. at 64 and 128 mg/kg induced higher response rates than at 32 mg/kg; title comp. partially substituted for cocaine/amphetamine discriminative stimulus with substitution being time-dependent and most pronounced at 60-120 min; diagrams

Reference

Dopheide, Marsha M.; Morgan, Russell E.; Rodvelt, Kelli R.; Schachtman, Todd R.; Miller, Dennis K.

European Journal of Pharmacology, 2007 , vol. 568, # 1-3 p. 112 - 123 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or Test-System (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

32 mg/kg


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Kind of Dosing (Pharmacological Data)

title comp. (Provigil, Alertec and Vigiler) dissolved in water vehicle containing 0.1percent DMSO and adminisered via gavage at a volume of 1 ml solution/kg

Method (Pharmacological Data)

rats trained to discriminate cocaine/amphetamine from saline injection for delivery of food pellet; administered with title comp.; 50 min later, cocaine/amphetamine administered; response rates determined after 10 min delay

Further Details (Pharmacological Data)

control: vehicle

Results

title comp. augmented the discriminative stimulus of cocaine and amphetamine; diagram

Reference

Dopheide, Marsha M.; Morgan, Russell E.; Rodvelt, Kelli R.; Schachtman, Todd R.; Miller, Dennis K.

European Journal of Pharmacology, 2007 , vol. 568, # 1-3 p. 112 - 123 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or Test-System (Pharmacological Data)

striatal slices of Sprague-Dawley rat

Sex

male

Concentration (Pharmacological Data)

0.01 - 300 μmol/l

Kind of Dosing (Pharmacological Data)

title comp. (Provigil, Alertec and Vigiler) used

Method (Pharmacological Data)

test system preloaded with <3H>dopamine; superfused with buffer containing title comp. for 6 min followed by buffer without title comp. for 20 min; filtered; radioactivity determined by liquid scintillation spectroscopy

Further Details (Pharmacological Data)

control: without title comp.; reference compounds: amphetamine, nicotine; further study: effect of nomifensine, mecamylamine on activity of title comp.

Results

title comp. at 100 and 300 μM increased the <3H>overflow in a concentration-dependent manner compared to control; at 0.01-30 μM, no effect was observed; title comp. effect attenuated by nomifensine but not by mecamylamine; diagrams, table

Reference

Dopheide, Marsha M.; Morgan, Russell E.; Rodvelt, Kelli R.; Schachtman, Todd R.; Miller, Dennis K.

European Journal of Pharmacology, 2007 , vol. 568, # 1-3 p. 112 - 123 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or Test-System (Pharmacological Data)

striatal slices of Sprague-Dawley rat

Sex

male

Concentration (Pharmacological Data)

0.01 - 30 μmol/l

Kind of Dosing (Pharmacological Data)

title comp. (Provigil, Alertec and Vigiler) used

Method (Pharmacological Data)

test system preloaded with <3H>dopamine; superfused with buffer containing title comp. for 10 min followed by amphetamine (1/3 μmol/l) for 6 min; filtered; radioactivity determined by liquid scintillation spectroscopy

Further Details (Pharmacological Data)

control: without title comp.

Results

title comp. signif. diminished <3H>overflow evoked by 1 μmol/l amphetamine but only 30 μmol/l diminished <3H>overflow evoked by 3 μmol/l amphetamine; diagram

Reference

Dopheide, Marsha M.; Morgan, Russell E.; Rodvelt, Kelli R.; Schachtman, Todd R.; Miller, Dennis K.

European Journal of Pharmacology, 2007 , vol. 568, # 1-3 p. 112 - 123 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or Test-System (Pharmacological Data)

striatal slices of Sprague-Dawley rat

Sex

male

Concentration (Pharmacological Data)

0.01 - 30 μmol/l

Kind of Dosing (Pharmacological Data)

title comp. (Provigil, Alertec and Vigiler) used

Method (Pharmacological Data)

test system preloaded with <3H>dopamine; superfused with buffer containing title comp. for 10 min followed by nicotine for 6 min; filtered; radioactivity determined by liquid scintillation spectroscopy

Further Details (Pharmacological Data)

control: without title comp.

Comment

No effect


(Pharmacological Data)

90 of 150

Reference

Dopheide, Marsha M.; Morgan, Russell E.; Rodvelt, Kelli R.; Schachtman, Todd R.; Miller, Dennis K.

European Journal of Pharmacology, 2007 , vol. 568, # 1-3 p. 112 - 123 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

wakefulness; effect on

Species or Test-System (Pharmacological Data)

human

Route of Application

sublingual

Method (Pharmacological Data)

Double blind study of sub-lingual d-modafinil composition in a normal human volunteer.The goal of this test was to confirm the suitability of the sublingual formulation and to ascertain if the purported short acting d-modafinil test article, under conditions of being very tired near to bedtime, had an affect on wakefulness.The test subject was given three vials: one vial containing the base formulation (as in Example 1) to test the taste and delivery means, and two coded vials. One of the coded vials contained 100 mg of d-modafinil formulation, and the second coded vial contained placebo (an equivalent amount of formulation).The subject was instructed to place the contents of the test formulation under the tongue, to allow the formulation to dissolve over two minutes, and to rinse any residual material with some water. ResultsSubject reported that the taste of the base formulation was pronounced, but tolerable. At 11 : 15 p.m. in the evening, the contents of one coded vial was placed under the tongue, allowed to dissolve over two minutes, and any residual was rinsed with some water. A strong taste remained for some time. The test subject then reported reading in bed, dozing on and off for EPO approximately 1.5 hours. After the room was darkened, the subject reported sleeping lighter, and awakening at least once at 3:15 a.m. during the night.On a following evening at 11 : 15 p.m., the contents of the second coded vial was similarly placed under the tongue, allowed to dissolve over two minutes under the tongue and rinsed. The test subject reported reading in bed until 12:50 a.m., then darkening the room and sleeping undisturbed all night until the morning.At both evenings the test subject reported being equally very tired. Approximately one week before these tests, the same subject took 200 mg racemic modafinil (Provigil.(R).) at 10 p.m. and reported a very pronounced effect, essentially being keep awake through the night to 5 a.m. Before unblinding the test articles, the subject recorded that one of the test articles was active, but neither test substance kept him awake as strongly or as long as the 200 mg racemic modafinil. After unblinding the test articles, it was confirmed that the coded vial with the reported activity contained 100 mg d-modafnil.

Results

approximately one week before these tests, the same subject took 200 mg test compound and reported a very pronounced effect

Location

Page/Page column 20; 21

Reference

NEUROHEALING PHARMACEUTICALS, INC.

Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details

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Effect (Pharmacological Data)

neuronal differentiation; effect on

Species or Test-System (Pharmacological Data)

human neural stem cells (hNSCs)

Method (Pharmacological Data)

Example 21 Effects of the 5-HT1a Agonist Buspirone in Combination with Modafinil on Differentiation of Human Neural Stem Cells Human neural stem cells (hNSCs) were isolated and grown in monolayer culture, plated, treated with varying concentrations of buspirone in the presence or absence of modafinil, and stained with TUJ-1 antibody for the detection of neuronal differentiation or GFAP antibody for the detection of astrocyte differentiation, as described above. Mitogen-free test media with a positive control for neuronal differentiation was used along with basal media without growth factors as a negative control. Results are shown in FIGS. 39 and 40, which show concentration response curves of neuronal and astrocyte differentiation respectively, after background media values are subtracted. The concentration response curves of the combination of buspirone with modafinil are shown with the concentration response curves of buspirone or modafinil alone. The data is presented as a percent of neuronal or astrocyte positive control. The data indicate that the combination of buspirone with modafinil resulted in consistent neuronal differentiation with a simultaneous decrease in astrocyte differentiation relative to that produced by buspirone alone.

Type (Pharmacological Data)

EC50

Value of Type (Pharmacological Data)

12.5 μmol/l

Results

Figure is given.

Location

Page/Page column 6; 45; sheet 39

Reference

BrainCells, Inc.

Patent: US2007/270449 A1, 2007 ; Title/Abstract Full Text Show Details

92 of 150

Effect (Pharmacological Data)

astrocyte differentiation; effect on

Species or Test-System (Pharmacological Data)

human neural stem cells (hNSCs)

Method (Pharmacological Data)

Example 21 Effects of the 5-HT1a Agonist Buspirone in Combination with Modafinil on Differentiation of Human Neural Stem Cells Human neural stem cells (hNSCs) were isolated and grown in monolayer culture, plated, treated with varying concentrations of buspirone in the presence or absence of modafinil, and stained with TUJ-1 antibody for the detection of neuronal differentiation or GFAP antibody for the detection of astrocyte differentiation, as described above. Mitogen-free test media with a positive control for neuronal differentiation was used along with basal media without growth factors as a negative control. Results are shown in FIGS. 39 and 40, which show concentration response curves of neuronal and astrocyte differentiation respectively, after background media values are subtracted. The concentration response curves of the combination of buspirone with modafinil are shown with the concentration response curves of buspirone or modafinil alone. The data is presented as a percent of neuronal or astrocyte positive control. The data indicate that the combination of buspirone with modafinil resulted in consistent neuronal differentiation with a simultaneous decrease in astrocyte differentiation relative to that produced by buspirone alone.

Type (Pharmacological Data)

EC50

Value of Type (Pharmacological Data)

> 31.6 μmol/l


Results

Figure is given.

Location

Page/Page column 6; 45; sheet 40

Reference

BrainCells, Inc.

Patent: US2007/270449 A1, 2007 ; Title/Abstract Full Text Show Details

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Effect (Pharmacological Data)

behavioural symptoms

Species or Test-System (Pharmacological Data)

Syrian hamster

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

100 - 300 mg/kg

Kind of Dosing (Pharmacological Data)

suspended in 0.25 percent carboxymethylcellulose

Method (Pharmacological Data)

hamsters were kept under 14-/10-h LD cycle and implanted with s.c. electrodes into the scull and nuchal muscle; 7 days later they were treated with title comp. at ZT 6 and EEG was recorded for 12 h, behavioral state was scored

Further Details (Pharmacological Data)

control: vehicle; LD: light-dark; ZT: zeitgeber time; EEG: electroencephalogram; ZT 6 is 6 h before lights off

Results

title comp. dose-dependently increased wakefulness at the expense of slow-wave and paradoxical sleep; at 300 mg/kg title comp. produced almost completely wakefulness for 6 h, paradoxical sleep was almost completely suppressed during 12 h

Reference

Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or Test-System (Pharmacological Data)

Syrian hamster

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

300 mg/kg

Kind of Dosing (Pharmacological Data)

suspended in 0.25 percent carboxymethylcellulose

Method (Pharmacological Data)

hamsters were kept under 14-/10-h LD cycle and treated with title comp. at ZT 6; they were videotaped in home cages for 3 h and the amount of time spent in various behaviors was analyzed

Further Details (Pharmacological Data)

control: vehicle; LD: light-dark; ZT: zeitgeber time; ZT 6 is 6 h before lights off; behaviors: active wake, quiet wake, behavioral sleep, grooming, feeding and drinking

Results

title comp. increased the percentage of total wakefulness and quiet wakefulness and significantly decreased the percentage of behavioral sleep and grooming

Reference

Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or Test-System (Pharmacological Data)

Syrian hamster

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

150 - 300 mg/kg

Kind of Dosing (Pharmacological Data)

suspended in 0.25 percent carboxymethylcellulose

Method (Pharmacological Data)

hamsters were kept under 14-/10-h LD cycle and treated with title comp. at ZT 6; the lights were then turned off and left off for 4 days, phase shifts were measured

Further Details (Pharmacological Data)

control: vehicle; LD: light-dark; ZT: zeitgeber time; phase shifts were measured by comparing the time of the onset of spontaneous activity (main period of daily wheel running) before and after treatment

Comment

No effect


(Pharmacological Data)

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Reference

Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or Test-System (Pharmacological Data)

Syrian hamster

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

300 mg/kg

Kind of Dosing (Pharmacological Data)

suspended in 0.25 percent carboxymethylcellulose

Method (Pharmacological Data)

hamsters were kept under 14-/10-h LD cycle and subjected to 1 night of LL; after that they were treated with title comp. at ZT 4, the lights were turned off at ZT 6 and left off for 4 days; phase shifts were measured

Further Details (Pharmacological Data)

control: vehicle; LD: light-dark; LL: constant light; ZT: zeitgeber time; phase shifts were measured by comparing the time of the onset of spontaneous activity (main period of daily wheel running) before and after treatment

Comment (Pharmacological Data)

No effect

Reference

Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or Test-System (Pharmacological Data)

Syrian hamster

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

300 mg/kg

Kind of Dosing (Pharmacological Data)

suspended in 0.25 percent carboxymethylcellulose

Method (Pharmacological Data)

hamsters were kept under 14-/10-h LD cycle and treated with title comp. at ZT 6 or ZT 12; lights were turned off at ZT 12 and left off for 4-7 days; the effect on phase shifts induced by 15-min light pulse (ca. 190 lx) at ZT 13 of treatment day measured

Further Details (Pharmacological Data)

control: vehicle; LD: light-dark; ZT: zeitgeber time; phase shifts were measured by comparing the time of the onset of spontaneous activity (main period of daily wheel running) during 3 days before treatment and on days 2, 3 and 6 after

Comment (Pharmacological Data)

No effect

Reference

Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or Test-System (Pharmacological Data)

Syrian hamster

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

300 mg/kg

Kind of Dosing (Pharmacological Data)

suspended in 0.25 percent carboxymethylcellulose

Method (Pharmacological Data)

hamsters were kept under 14-/10-h LD cycle, lights were turned off at ZT 12; at ZT 17 animals were treated with title comp. and the effect on phase shifts induced by 15-min light pulse (ca. 190 lx) at ZT 18 was measured; lights remained off for 4-7 days

Further Details (Pharmacological Data)

control: vehicle; LD: light-dark; ZT: zeitgeber time; phase shifts were measured by comparing the time of the onset of spontaneous activity (main period of daily wheel running) during 3 days before treatment and on days 2, 3 and 6 after

Comment (Pharmacological Data)

No effect


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101 of 150

Reference

Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or Test-System (Pharmacological Data)

Syrian hamster

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

300 mg/kg

Kind of Dosing (Pharmacological Data)

suspended in 0.25 percent carboxymethylcellulose

Method (Pharmacological Data)

hamsters kept under 14-/10-h LD cycle were subjected to 1 night of LL; then they were treated with title comp. at ZT 4 and confined to a new wheel at ZT 6; the lights were turned off during confinement and left off for 4 days; phase shifts were measured

Further Details (Pharmacological Data)

control: vehicle; LD: light-dark; LL: constant light; ZT: zeitgeber time; phase shifts were measured by comparing the time of the onset of spontaneous activity (main period of daily wheel running) before and after treatment

Comment (Pharmacological Data)

No effect

Reference

Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or Test-System (Pharmacological Data)

Syrian hamster

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

300 mg/kg

Kind of Dosing (Pharmacological Data)

suspended in 0.25 percent carboxymethylcellulose

Method (Pharmacological Data)

hamsters kept under 14-/10-h LD cycle were subjected to 1 night of LL; then they were treated with title comp. at ZT 4 and confined to a new wheel at ZT 6 (for 3 h); lights turned off at ZT 6 and the effect on wheel running activity analyzed for 18 h

Further Details (Pharmacological Data)

control: vehicle; LD: light-dark; LL: constant light; ZT: zeitgeber time

Results

title comp. decreased the number of 18-h cumulative wheel revolutions by 55.4 percent; the number of wheel revolutions during wheel confinement was decreased by 53.3 percent

Reference

Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or Test-System (Pharmacological Data)

Syrian hamster

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

300 mg/kg

Kind of Dosing (Pharmacological Data)

suspended in 0.25 percent carboxymethylcellulose

Method (Pharmacological Data)

hamsters kept under 14-/10-h LD cycle were subjected to 1 night of LL; then they were treated with title comp. at ZT 4 and the lights were turned off at ZT 6; the effect on wheel running activity was analyzed for 18 h

Further Details (Pharmacological Data)

control: vehicle; LD: light-dark; LL: constant light; ZT: zeitgeber time

Results

title comp. decreased the number of 18-h cumulative wheel revolutions by 51.5 percent

Reference

Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details


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105 of 150

Effect (Pharmacological Data)

receptor; binding activity

Species or Test-System (Pharmacological Data)

Macaca mulatta, rhesus monkey

Sex

male and female

Route of Application

intravenous

Concentration (Pharmacological Data)

2 - 8 mg/kg

Method (Pharmacological Data)

title comp. administered; after 1 h <11C>CFT or <11C>altropane injected i.v.; DAT or NET, resp., occupancy measured using positron emission tomography imagine

Further Details (Pharmacological Data)

CFT: 2β-carbomethoxy-3β-4-(fluorophenyl)tropane; DAT: dopamine transporter; NET: norepinephrine transporter; methylphenidate used as reference comp.

Results

title comp. occupied 35percent and 53percent of DAT sites in striatum at 5 and 8 mg/kg, resp., when <11C>CFT probe was used; at 8 mg/kg decreased <11C>altropane binding by 67percent; effect comparable to that of methylphenidate; no effect at 2 mg/kg (table, figures)

Reference

Madras, Bertha K.; Xie, Zhihua; Lin, Zhicheng; Jassen, Amy; Panas, Helen; Lynch, Laurie; Johnson, Ryan; Livni, Eli; Spencer, Thomas J.; Bonab, Ali A.; Miller, Gregory M.; Fischman, Alan J.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 2 p. 561 - 569 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or Test-System (Pharmacological Data)

HEK293 cells

Method (Pharmacological Data)

radioligand binding assay performed; cells transfected with DAT incubated with <3H>DA in presence of title comp.; radioactivity measured using scintillation fluid

Further Details (Pharmacological Data)

DAT: dopamine transporter

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

4360 nmol/l

Reference

Madras, Bertha K.; Xie, Zhihua; Lin, Zhicheng; Jassen, Amy; Panas, Helen; Lynch, Laurie; Johnson, Ryan; Livni, Eli; Spencer, Thomas J.; Bonab, Ali A.; Miller, Gregory M.; Fischman, Alan J.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 2 p. 561 - 569 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or Test-System (Pharmacological Data)

HEK293 cells

Method (Pharmacological Data)

transport assay performed; cells transfected with DAT pretreated with title comp.; incubated with <3H>DA at 25 deg C for 10 min in darkness; radioactivity measured using scintillation fluid

Further Details (Pharmacological Data)

DAT: dopamine transporter; reference comp. (IC50, nmol/l): methylphenidate (25.4), benztropine (213), bupropion (1088)

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

6390 nmol/l

Reference

Madras, Bertha K.; Xie, Zhihua; Lin, Zhicheng; Jassen, Amy; Panas, Helen; Lynch, Laurie; Johnson, Ryan; Livni, Eli; Spencer, Thomas J.; Bonab, Ali A.; Miller, Gregory M.; Fischman, Alan J.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 2 p. 561 - 569 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or Test-System (Pharmacological Data)

HEK293 cells

Method (Pharmacological Data)

transport assay performed; cells transfected with NET pretreated with title comp.; incubated with <3H>norepinephrine at 25 deg C for 10 min in darkness; radioactivity measured using scintillation fluid

Further Details (Pharmacological Data)

NET: norepinephrine transporter; reference comp. (IC50, nmol/l): methylphenidate (26.5), benztropine (667)

Type (Pharmacological Data)

IC50


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107 of 150

108 of 150

109 of 150

Value of Type (Pharmacological Data)

35600 nmol/l

Reference

Madras, Bertha K.; Xie, Zhihua; Lin, Zhicheng; Jassen, Amy; Panas, Helen; Lynch, Laurie; Johnson, Ryan; Livni, Eli; Spencer, Thomas J.; Bonab, Ali A.; Miller, Gregory M.; Fischman, Alan J.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 2 p. 561 - 569 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or Test-System (Pharmacological Data)

HEK293 cells

Method (Pharmacological Data)

transport assay performed; cells transfected with NET pretreated with title comp.; incubated with <3H>dopamine at 25 deg C for 10 min in darkness; radioactivity measured using scintillation fluid

Further Details (Pharmacological Data)

NET: norepinephrine transporter

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

170000 nmol/l

Reference

Madras, Bertha K.; Xie, Zhihua; Lin, Zhicheng; Jassen, Amy; Panas, Helen; Lynch, Laurie; Johnson, Ryan; Livni, Eli; Spencer, Thomas J.; Bonab, Ali A.; Miller, Gregory M.; Fischman, Alan J.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 2 p. 561 - 569 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or Test-System (Pharmacological Data)

HEK293 cells

Method (Pharmacological Data)

transport assay performed; cells transfected with SERT pretreated with title comp.; incubated with <3H>serotonin at 25 deg C for 10 min in darkness; radioactivity measured using scintillation fluid

Further Details (Pharmacological Data)

SERT: serotonin transporter; reference comp.: benztropine (IC50 = 21660 nmol/l)

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

> 500 μmol/l

Reference

Madras, Bertha K.; Xie, Zhihua; Lin, Zhicheng; Jassen, Amy; Panas, Helen; Lynch, Laurie; Johnson, Ryan; Livni, Eli; Spencer, Thomas J.; Bonab, Ali A.; Miller, Gregory M.; Fischman, Alan J.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 2 p. 561 - 569 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or Test-System (Pharmacological Data)

Macaca mulatta, rhesus monkey

Sex

male and female

Route of Application

intravenous

Concentration (Pharmacological Data)

2 - 8 mg/kg

Method (Pharmacological Data)

title comp. administered; after 1 h <11C>MeNER injected i.v.; NET occupancy measured using positron emission tomography imagine

Further Details (Pharmacological Data)

MeNER: (S,S)-2-(α-(2-methoxyphenoxy)benzyl)morpholine; NET: norepinephrine transporter

Results

title comp. occupied 16percent and 44percent of NET sites in thalamus at 5 and 8 mg/kg, resp.; no effect at 2 mg/kg (table, figures)

Reference

Madras, Bertha K.; Xie, Zhihua; Lin, Zhicheng; Jassen, Amy; Panas, Helen; Lynch, Laurie; Johnson, Ryan; Livni, Eli; Spencer, Thomas J.; Bonab, Ali A.; Miller, Gregory M.; Fischman, Alan J.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 2 p. 561 - 569 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or Test-System (Pharmacological Data)

HEK293 cells

Concentration

Ca. 1E-09 - 0.0001 mol/l


(Pharmacological Data)

110 of 150

Method (Pharmacological Data)

cells expressing or not human DAT, NET or SERT transfected with TA1 and CRE-luc reporter system; treated with title comp. alone or in presence of PEA for 18 h; lysed; TA1 activation determined by measuring luciferase conc.

Further Details (Pharmacological Data)

DAT: dopamine transporter; NET: norepinephrine transporter; SERT: serotonin transporter; TA1: trace amine receptor; CRE: cAMP response element; PEA: phenethylamine

Results

title comp. sign. increased TA1 activity in presence of DAT at 100 μmol/l; no effect on TA1 activity alone or in presence of NET or SERT; at 10 μmol/l in presence of PEA sign. activated TA1 in presence of DAT or NET, but not SERT (figure)

Reference

Madras, Bertha K.; Xie, Zhihua; Lin, Zhicheng; Jassen, Amy; Panas, Helen; Lynch, Laurie; Johnson, Ryan; Livni, Eli; Spencer, Thomas J.; Bonab, Ali A.; Miller, Gregory M.; Fischman, Alan J.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 2 p. 561 - 569 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

self-injurious behavior; effect on

Species or Test-System (Pharmacological Data)

human

Sex

female

Method (Pharmacological Data)

Example 2; Treatment of a 45-Year-Old Female with Self-Injurious Behavior Using Riluzole; Patient 2 was a 45-year-old woman with a long history of borderline personality disorder, major depression, obsessive-compulsive disorder and generalized anxiety disorder. She had a several year history of engaging in self-injurious behavior such as hitting herself until she bruised, banging her head, and cutting herself. These self-injurious behaviors and the cravings to cut worsened under times of stress. She was previously treated with intensive psychotherapy, cognitive behavioral therapy, and pharmacotherapy. Medication management included treatment trials, either alone or in combination, of the following medications: EFFEXOR, ZOLOFT (sertaline HCl), TOPAMAX (topirimate), ATIVAN (lorazepam), trazodone, ABILIFY AND NEURONTIN (gabapentin). Riluzole, a glutamate modulating agent, was added to her medication regimen which consisted of ZOLOFT 200 mg each day, RISPERDAL (risperidone) 2 mg at bedtime, KLONOPIN 1 mg three times per day and PROVIGIL (modafinil) 200 mg a day. Riluzole was dosed at 50 mg twice a day. She reported a marked attenuation and ultimately, complete cessation of the desire to engage in self-injurious behaviors. Similar to the first case, the cessation in self-injurious behaviors occurred between week 2 and 3 of treatment with riluzole. Patient 2 has not engaged in any self-injurious behaviors in over six months, which represents the longest period of time that she has not engaged in self-injurious behavior over the last several years.

Results

treatment with title compound (200 mg once daily) in combination with zoloft (200 mg once daily), risperidone (2 mg once daily), klonopin (1 mg, 3 times per day) and riluzole (50 mg twice a day) caused a marked attenuation and ultimately, complete cessation of the desire to engage in self-injurious behaviors

Location

Page/Page column 7

Reference

Feuerstein, Seth; Coric, Vladimir

Patent: US2006/167068 A1, 2006 ; Title/Abstract Full Text Show Details

111 of 150

Effect (Pharmacological Data)

blood pressure; effect on

Species or Test-System (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Method (Pharmacological Data)

RESEARCH DESIGNType of Design and Sub-Groups of Problem Gamblers. We assessed the effects of a 200-mg oral dose of modafinil in a placebo-controlled, fully counterbalanced, double blind, between-within design. The within-subjects factor was Treatment: drug vs. placebo. The between-subjects factor was Sequence of Treatment: Half of the subjects received modafinil on test session 1 and placebo on test session 2; the other half received the treatments in reverse order.Subjects Subjects were 6 problem gamblers as defined by scores > 5 on the South Oaks Gambling Screen (SOGS; Lesieur Blume, 1987) and on the DSM-IV (APA, 1994).Each subject underwent two procedurally identical (except for drug treatment) test sessions. On each session, subjects received their assigned drug treatment and underwent a 15-minute gambling episode on a slot-machine version Electronic Gaming Device (EGD). Subjective, cognitive, and behavioral indices were assessed at multiple time points throughout each session (see details below).General Reliability and Validity of Tasks and Dependent Measures.Modified visual analogue scales Modified Visual Analogue Scales (m-VAS; 0-10) measure (a) Desire to Gamble, (b) Confidence to Refrain from Gambling. M-VAS ratings are widely used tools for assessing drug effects (Fischman Foltin, 1991), and their sensitivity to drug effects in problem gamblers has been validated in our two previous drug studies (Zack Poulos, 2004; Zack, Poulos Desmond, 2004). M-VAS ratings also assess the subjective pleasurable or rewarding effects of the gambling episode (i.e., Enjoyment, Excitement, and perceived 'High'). M- VAS measures of gambling reward have been validated in previous published studies (Loba, Stewart, Klein, Blackburn, 2001), as well as in our recent haloperidol study (Zack, Poulos Desmond, 2004).M-VAS Measure of Interest in Everyday Activities To assess the effects of modafinil on subjective (i.e., state) boredom proneness during the test sessions, we used an m-VAS scale (0-10) to rate agreement with the following statement: "Right now, I could find interest in any one of a variety of everyday activities."Addiction Research Center Inventory (ARCI) Relevant sub-scales of the ARCI (Haertzen, 1965) assess responses to the drug treatment at several points within each test session (see Session Timeline below). The ARCI is a standardized index of drug effects that measures a range of EPO subjective, mental, emotional and physical responses to psychoactive drugs. The ARCI has been used to assess the modulating effects of modafnil on subjective responses to cocaine (Dackis et al., 2003).Stop Signal Task We use the most recent version of the Stop-Signal Task, which employs an algorithm to compute mean inhibitory latency to the stop signal (also known as Stop SignalReaction Time; SSRT). This task provides a behavioral index of inhibitory control: The faster the SSRT, the better is the inhibitory control. Performance on this task has been shown to correlate positively with scores on the Eysenck Impulsiveness Scale in heterogeneous samples (Logan, Schachar, Tannock, 1997). The task has been widely validated in terms of its sensitivity to drug effects, including modafinil, as well as in clinical populations (e.g., ADHD patients; For details, see Turner et al. 2004).Gambling/Slot Machine Episode As in previous laboratory gambling studies (Loba et al., 2001), subjects are given cash credits with which to bet. They are required to play for 15 minutes. Play stops if a subject exhausts all credits. To increase validity and provide an incentive to do well on the slot machine, subjects are advised that they will receive a monetary bonus at the end of the study proportional to the number of credits they win on each session. This is also noted in the consent form. For ethical reasons, all subjects in fact receive an identical bonus of USD80 (USD40 x 2 sessions) in addition to their participation fee. We use an El

Results

there was only minor fluctuation in blood pressure due to the game under modafinil (figure is given)

Location

Page/Page column 5; 8; 12; 18; sheet 4

Reference

CENTRE FOR ADDICTION AND MENTAL HEALTH

Patent: WO2006/32146 A1, 2006 ; Title/Abstract Full Text Show Details


112 of 150

113 of 150

Effect (Pharmacological Data)

analgesic, other

Species or Test-System (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration (Pharmacological Data)

400 mg

Kind of Dosing (Pharmacological Data)

daily for 2 days

Method (Pharmacological Data)

12 healthy subjects in randomized, double-blind crossover study; 2 h after the second dose responses in acute pain tests assessed (finger pressure pain task using Forgione-Barber pain stimulator, 10 min rest, then forearm ischemic pain task)

Further Details (Pharmacological Data)

both acute pain tests evaluated using verbal numeric rating scale and by completing McGill Pain Questionnaire

Comment (Pharmacological Data)

No effect

Reference

Taneja, Indu; Bruehl, Stephen; Robertson, David

Journal of Clinical Pharmacology, 2004 , vol. 44, # 12 p. 1425 - 1427 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

beagle dog

Sex

male

Route of Application

peroral

Method (Pharmacological Data)

polymorphic forms of title comp. racemate administered as single dose; blood samples collected predose and 0.5 to 24 h post-dose; plasma title comp. concentrations determined by validated high-pressure liquid chromatography

Results

title comp. Cmax = 18.60 μg/ml, C4h = 15.37 μg/ml, AUC0-24h = 164.80 h*μg/ml

Location

Page 44-46

Reference

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

114 of 150

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

beagle dog

Sex

male

Route of Application

peroral

Method (Pharmacological Data)

polymorphic forms of title comp. racemate administered as single dose; blood samples collected predose and 0.5 to 24 h post-dose; plasma title comp. concentrations determined by validated high-pressure liquid chromatography

Results

title comp. conc. increased in time-dependent manner with Cmax = 18.60 μg/ml , Tmax = 3.00 h

Location

Page 44; 46-47

Reference

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

115 of 150

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

beagle dog

Sex

male

Route of Application

peroral

Method (Pharmacological Data)

polymorphic forms of title comp. racemate administered as single dose; blood samples collected predose and 0.5 to 24 h post-dose; plasma title comp. concentrations determined by validated high-pressure liquid chromatography

Results

title comp. Cmax = 24.98 μg/ml, C4h = 21.23 μg/ml, AUC0-24h = 200.69 h*μg/ml Page 44-46


Location Reference

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

116 of 150

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

beagle dog

Sex

male

Route of Application

peroral

Method (Pharmacological Data)

polymorphic forms of title comp. racemate administered as single dose; blood samples collected predose and 0.5 to 24 h post-dose; plasma title comp. concentrations determined by validated high-pressure liquid chromatography

Results

title comp. conc. increased in time-dependent manner with Cmax = 18.72 μg/ml, Tmax = 1.67 h

Location

Page 44; 46-47

Reference

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

117 of 150

118 of 150

Effect (Pharmacological Data)

drug interaction

Species or Test-System (Pharmacological Data)

human

Sex

female

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

200 mg once daily for 7 d from day 6 - 8 of 28-d menstrual cycle 2, followed by 400 mg once daily for two last weeks of cycle 2 and 1-st week of cycle 3; given with 240 ml of water

Method (Pharmacological Data)

Ortho Tri-Cyclen given throughout cycles 1, 2, and 1-st wk of cycle 3; 24-h blood sampled on cycle 2 day 5 - 7 and last treatment day; ethinyl estradiol plasma conc. measured by HPLC with ultraviolet detection

Further Details (Pharmacological Data)

Ortho Tri-Cyclen: 0.035 mg ethinyl estradiol with 0.180 - 0.250 progestin norgestimate, p.o.; AUC(0-τ): area under conc.-time curve; Cmax/Ctrough: maximum/minimum plasma conc., resp.; tmax: time to Cmax:; t1/2: half-life; placebo control

Results

in title comp. group ethinyl estradiol AUC(0-τ) was significantly decreased from cycle 2 to cycle 3 by 18 percent, Cmax by 11 percent, and tmax by 0.3 h; no significant difference in t1/2, Ctrough, and terminal elimination rate constant

Reference

Robertson Jr., Philmore; Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael

Clinical Pharmacology and Therapeutics, 2002 , vol. 71, # 1 p. 46 - 56 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

human

Sex

female

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

200 mg once daily for 7 d from day 6 - 8 of 28-d menstrual cycle 2, followed by 400 mg once daily for two last weeks of cycle 2 and 1-st week of cycle 3; given with 240 ml of water

Method (Pharmacological Data)

title comp. given with Ortho Tri-Cyclen and triazolam (0.125 mg added on days 5 - 7 of cycles 2 and 3); 24-h blood sampled at last treatment day; title comp. and metabolites 1/2 (title comp. acid/sulfone, resp.) plasma conc. measured by HPLC

Further Details (Pharmacological Data)

Ortho Tri-Cyclen: 0.035 mg ethinyl estradiol with 0.180 - 0.250 progestin norgestimate, p.o., for cycles 1, 2, 1-st wk of cycle 3; AUC(0-τ): area under curve; Cmax/trough: max/minimum plasma conc., resp.; tmax: time to Cmax:; t1/2: half-life

Half-life Time (Pharmacological Data)

11.4 h

Results

title comp./metabolite 1/2 AUC(0-τ) = 131/51/105 μg*h/ml, Cmax = 13.4/6.1/5.2 μg/ml, Ctrough = 2.4/0.4/4.3 μg/ml, tmax = 1.8/2.8/4.8 h, terminal rate constant for elimination from plasma = 0.062/0.128/- (resp.); metabolite 1/2 t1/2 = 5.5/- h

Metabolite (Pharmacological Data)

modafinil acid [Reaxys RN: 6650982] ; Modafinil sulfone [Reaxys RN: 9199801]

Reference

Robertson Jr., Philmore; Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael

Clinical Pharmacology and Therapeutics, 2002 , vol. 71, # 1 p. 46 - 56 Title/Abstract Full Text View citing articles Show Details


119 of 150

120 of 150

121 of 150

122 of 150

Effect (Pharmacological Data)

releasing hormones

Species or Test-System (Pharmacological Data)

human

Sex

female

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

200 mg once daily for 7 d from day 6 - 8 of 28-d menstrual cycle 2, followed by 400 mg once daily for two last weeks of cycle 2 and 1-st week of cycle 3; given with 240 ml of water

Method (Pharmacological Data)

title comp. given with Ortho Tri-Cyclen and triazolam (0.125 mg added on days 5 - 7 of cycles 2 and 3, p.o.); 24-h blood sampled on day 5 - 7 of cycle 2 and on last treatment day; FSH and LH plasma conc. determined

Further Details (Pharmacological Data)

Ortho Tri-Cyclen: 0.035 mg ethinyl estradiol with 0.180 - 0.250 progestin norgestimate, p.o., for cycles 1, 2, and 1-st wk of cycle 3; FSH: follicle-stimulating hormone; LH: luteinizing hormone; placebo control

Results

no significant differences in title comp./placebo groups in mean changes from cycle 2 to 3 in FSH, LH plasma conc.; title comp./placebo mean change in plasma FSH conc. increased by 0.4/0.1 mIU/L, mean LH plasma conc. increased by 0.4/0.2 mIU/L (resp.)

Reference

Robertson Jr., Philmore; Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael

Clinical Pharmacology and Therapeutics, 2002 , vol. 71, # 1 p. 46 - 56 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

toxicity

Species or Test-System (Pharmacological Data)

human

Sex

female

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

200 mg once daily for 7 d from day 6 - 8 of 28-d menstrual cycle 2, followed by 400 mg once daily for two last weeks of cycle 2 and 1-st week of cycle 3; given with 240 ml of water

Method (Pharmacological Data)

title comp. (group A) given with Ortho Tri-Cyclen and triazolam (0.125 mg added on days 5 - 7 of cycles 2 and 3, p.o.); blood and urine sampled at screening visit, and on last treatment day; adverse events recorded

Further Details (Pharmacological Data)

Ortho Tri-Cyclen: 0.035 mg ethinyl estradiol with 0.180 - 0.250 progestin norgestimate, p.o., for cycles 1, 2, and 1-st wk of cycle 3; placebo control (group B)

Results

adverse events were mild or moderate; in groups A and B most frequent were headache/asthenia/nausea/dizziness/metrorrhagia/pain/dysmenorrhea/anorexia in 72/50/33/28/22/17/17/17 and 53/58/11/11/5/5/5/0 percent, resp.

Reference

Robertson Jr., Philmore; Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael

Clinical Pharmacology and Therapeutics, 2002 , vol. 71, # 1 p. 46 - 56 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; induction of

Species or Test-System (Pharmacological Data)

human

Sex

female

Route of Application

peroral

Concentration (Pharmacological Data)

200 mg

Kind of Dosing (Pharmacological Data)

200 mg once daily for 7 d from day 6 - 8 of 28-d menstrual cycle 2, followed by 400 mg once daily for two last weeks of cycle 2 and 1-st week of cycle 3; given with 240 ml of water

Method (Pharmacological Data)

title comp. (group A) given with Ortho Tri-Cyclen and triazolam (0.125 mg added on days 5 - 7 of cycles 2 and 3, p.o.); blood and urine sampled at screening visit and on last treatment day; alkaline phosphatase levels determined

Further Details (Pharmacological Data)

Ortho Tri-Cyclen: 0.035 mg ethinyl estradiol + 0.180 - 0.250 progestin norgestimate, for cycle 1, 2, and 1-st wk of cycle 3; placebo control (group B)

Results

statistically significant increase observed in mean change from baseline for alkaline phosphatase, greater in group A vs group B, without clinically significant abnormal alkaline phosphatase levels for any subject

Reference

Robertson Jr., Philmore; Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael

Clinical Pharmacology and Therapeutics, 2002 , vol. 71, # 1 p. 46 - 56 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

drug interaction

Species or Test-System (Pharmacological Data)

human

Sex

female peroral


Route of Application

123 of 150

124 of 150

125 of 150

Kind of Dosing (Pharmacological Data)

200 mg once daily for 7 d from day 6 - 8 of 28-d menstrual cycle 2, followed by 400 mg once daily for two last weeks of cycle 2 and 1-st week of cycle 3; given with 240 ml of water

Method (Pharmacological Data)

Ortho Tri-Cyclen given for cycle 1, 2, and 1-st wk of cycle 3, p.o.; 0.125 mg triazolam added on days 5 - 7 of cycles 2 and 3, p.o.; 24-h blood sampled on cycle 2 days 5 - 7 and on last day of treatment; triazolam plasma conc. measured by HPLC

Further Details (Pharmacological Data)

Ortho Tri-Cyclen: 0.035 mg ethinyl estradiol with 0.180-0.250 progestin norgestimate; AUC(0-τ): area under curve; Cmax/trough: max/minimum plasma conc., resp.; tmax: time to Cmax:; t1/2: half-life; λ: elimination rate constant; placebo control

Results

in title comp. group triazolam AUC(0-τ) significantly changed from cycle 2 to cycle 3 by -59 percent, Cmax by -42 percent, λ by 51 percent, t1/2 by -35 percent

Reference

Robertson Jr., Philmore; Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael

Clinical Pharmacology and Therapeutics, 2002 , vol. 71, # 1 p. 46 - 56 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration (Pharmacological Data)

200 - 400 mg

Kind of Dosing (Pharmacological Data)

title comp. (100 mg TB) admin. once-daily, early morning (200 mg on days 1-7; 400 mg on days 8-28) alone/in combination with once-daily, MAD of Dex (20 mg on days 22-28)

Method (Pharmacological Data)

open-label, randomized, single-period, parallel-group, single-center study; healthy subjects (13 Caucasians, 2 others) in groups (GPs) received title comp. with/without Dex; blood collected pre- and post-dosing (day 21, 28) upto 24 h; PK detd. by HPLC

Further Details (Pharmacological Data)

control: placebo; group 1: title comp.+dextroamphetamine (Dex); group 2: title comp. alone; safety and tolerability also studied; TB: tablets; MAD: mid-afternoon doses

Results

mean changes in PK parameters for title comp. and its two circulating metabolites between group 1 and 2 were not statistically signif. different, except Cmax for modafinil acid; mild to moderate adverse events reported; tables, diagram

Reference

Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael; Robertson Jr., Philmore

Journal of Clinical Pharmacology, 2002 , vol. 42, # 4 p. 450 - 460 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

biotransformation

Species or Test-System (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration (Pharmacological Data)

200 - 400 mg

Kind of Dosing (Pharmacological Data)

title comp. (100 mg tablets) admin. once-daily, early morning (200 mg on d 1-7; 400 mg on d 8-28) alone/in combination with once-daily, mid-afternoon doses of Dex (20 mg on d 22-28)

Method (Pharmacological Data)

open-label, randomized, single-period, parallel-group, single-center study; healthy subjects (13 Caucasians, 2 others) in groups (GPs) received title comp. with/without Dex; blood collected pre- and post-dosing (d 21 and 28) upto 24 h; PK detd. by HPLC

Further Details (Pharmacological Data)

control: placebo; group (GP) 1: title comp.+dextroamphetamine (DEX); GP 2: title comp. alone; MTPC: mean trough plasma conc.; MC: mean changes; PK: pharmacokinetic parameters

Results

MTPC of metabolites on d 19-21 and 26-28 was similar within treatment GPs; MTPC of acid was similar between GPs but sulfone was higher in GP 1 than GP 2; MC in PK between GPs were not signif. different except Cmax for acid metabolite; diagrams, tables

Metabolite (Pharmacological Data)

modafinil acid [Reaxys RN: 6650982] ; Modafinil sulfone [Reaxys RN: 9199801]

Reference

Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael; Robertson Jr., Philmore

Journal of Clinical Pharmacology, 2002 , vol. 42, # 4 p. 450 - 460 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration

200 mg


(Pharmacological Data)

126 of 150

127 of 150

128 of 150

Kind of Dosing (Pharmacological Data)

200 mg title comp. (PROVIGIL(R)) was admin. on days 1-7 and 400 mg on days 8-28; title comp. (PROVIGIL(R)) was admin. as a single dose with 240 ml of water

Method (Pharmacological Data)

open-label, randomized, single period study; healthy subjects received title comp.; methylphenidate was administered on days 22-28; blood sampled at pre- and 24 h post dosing; plasma concentration of title comp. was determined by HPLC; PK calculated

Further Details (Pharmacological Data)

PK: pharmacokinetic parameters

Half-life Time (Pharmacological Data)

11 - 11.5 h

Results

mean trough plasma concentrations (μg/ml) of title comp. was ranged from 2.1 to 2.5; AUC0-24 (μg*h/ml), Cmax (μg/ml), tmax (h), t1/2 (h) of title comp., on day 21/day 28 were 143.8/139.4, 13.5/13.3, 1.9/2.1, 11.5/11.0, respectively; table, fig.

Reference

Hellriegel; Arora; Nelson; Robertson P.

Journal of Clinical Pharmacology, 2001 , vol. 41, # 8 p. 895 - 904 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration (Pharmacological Data)

200 mg

Kind of Dosing (Pharmacological Data)

200 mg title comp. (PROVIGIL(R)) was admin. on days 1-7 and 400 mg on days 8-28; title comp. (PROVIGIL(R)) was admin. as a single dose with 240 ml of water

Method (Pharmacological Data)

open-label, randomized, single period study; healthy subjects received title comp.; blood sampled at pre- and 24 h post dosing; plasma concentration of title comp. was determined by HPLC; pharmacokinetic parameters calculated

Half-life Time (Pharmacological Data)

12.6 - 14.2 h

Results

mean trough plasma concentrations (μg/ml) of title comp. was ranged from 2.5 to 4.4; AUC0-24 (μg*h/ml), Cmax (μg/ml), tmax (h), t1/2 (h) of title comp., on day 21/day 28 were 151.8/147.7, 13.5/14.3, 2.1/2.3, 14.2/12.6, respectively; table, fig.

Reference

Hellriegel; Arora; Nelson; Robertson P.

Journal of Clinical Pharmacology, 2001 , vol. 41, # 8 p. 895 - 904 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

biotransformation

Species or Test-System (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration (Pharmacological Data)

200 mg

Kind of Dosing (Pharmacological Data)

200 mg title comp. (PROVIGIL(R)) was admin. on days 1-7 and 400 mg on days 8-28; title comp. (PROVIGIL(R)) was admin. as a single dose with 240 ml of water

Method (Pharmacological Data)

open-label, randomized, single period study; healthy subjects received title comp.; blood sampled at pre- and 24 h post dosing; plasma concentration of title comp. metabolites were determined by HPLC; pharmacokinetic parameters calculated

Further Details (Pharmacological Data)

title comp. metabolites: title comp. acid and title comp. sulfone

Results

AUC0-24, Cmax and tmax of title comp. acid/title comp. sulfone on day 21 were 49.1/138.9 μg*h/ml, 4.8/7.1 μg/ml and 2.9/10.3 h, respectively; table, fig.

Metabolite (Pharmacological Data)

modafinil acid [Reaxys RN: 6650982] ; Modafinil sulfone [Reaxys RN: 9199801]

Reference

Hellriegel; Arora; Nelson; Robertson P.

Journal of Clinical Pharmacology, 2001 , vol. 41, # 8 p. 895 - 904 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

adverse effect

Species or Test-System (Pharmacological Data)

human

Sex

male and female


129 of 150

130 of 150

131 of 150

Route of Application

peroral

Concentration (Pharmacological Data)

200 mg

Kind of Dosing (Pharmacological Data)

200 mg title comp. (PROVIGIL(R)) was admin. on days 1-7 and 400 mg on days 8-28; title comp. (PROVIGIL(R)) was admin. as a single dose with 240 ml of water

Method (Pharmacological Data)

open-label, randomized, single period study; healthy subjects were treated with title comp.; adverse events were observed

Results

adverse events were observed in 47 and 77 percent of subjects administered with 200 and 400 mg title comp., respectively; most commonly reported adverse event was headache (69 percent of subjects); tables

Reference

Hellriegel; Arora; Nelson; Robertson P.

Journal of Clinical Pharmacology, 2001 , vol. 41, # 8 p. 895 - 904 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

human

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

200 - 800 mg

Kind of Dosing (Pharmacological Data)

200, 400, 600 or 800 mg once daily for 7 d

Method (Pharmacological Data)

single-center, randomized, double-blind, placebo-controlled, ascending-dose trial in normal, healthy volunteers; levels of title comp., its l and d enantiomers, and metabolites in blood and urine (HPLC); Cmax. Tmax, AUC, VD, OC, PC and RC

Further Details (Pharmacological Data)

safety and tolerability determined; oral, plasma and renal clearance (OC, PC and RC, resp.); VD = volume of distribution

Half-life Time (Pharmacological Data)

Ca. 15 h

Results

title comp. had a rapid oral absorption rate; eliminated primarily by metabolism with dose- and time-independent pharmacokinetics; d-enantiomer eliminated 3-fold faster than l; 200-600 mg generally well tolerated; PC ca. 50 ml/min, VD ca. 0.8 l/kg

Reference

Wong, Y. Nancy; Simcoe, Donna; Hartman, Linda N.; Laughton, Watson B.; King, S. Peter; McCormick, George C.; Grebow, Peter E.

Journal of Clinical Pharmacology, 1999 , vol. 39, # 1 p. 30 - 40 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

biotransformation

Species or Test-System (Pharmacological Data)

human

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

200 - 800 mg

Kind of Dosing (Pharmacological Data)

200, 400, 600 or 800 mg once daily for 7 d

Method (Pharmacological Data)

single-center, randomized, double-blind, placebo-controlled, ascending-dose trial in normal, healthy volunteers; levels of title comp., its l and d enantiomers, and metabolites in blood and urine (HPLC)

Half-life Time (Pharmacological Data)

Ca. 15 h

Results

title comp. eliminated primarily by metabolism

Metabolite (Pharmacological Data)

modafinil acid [Reaxys RN: 6650982] ; Modafinil sulfone [Reaxys RN: 9199801]

Reference

Wong, Y. Nancy; Simcoe, Donna; Hartman, Linda N.; Laughton, Watson B.; King, S. Peter; McCormick, George C.; Grebow, Peter E.

Journal of Clinical Pharmacology, 1999 , vol. 39, # 1 p. 30 - 40 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

cardiotonic

Species or Test-System (Pharmacological Data)

human

Sex

male


132 of 150

133 of 150

134 of 150

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

200 mg in the morning and 100 mg at midday for 2 d

Method (Pharmacological Data)

systolic/diastolic blood pressure (SBP/DBP) and HR measured before and for up to 24 h after 1-st title comp. dose (including vigilance, psychometry, ergometry, total daytime, NREM/REM, total sleep) by continuous intraarterial blood pressure monitoring

Further Details (Pharmacological Data)

26 healthy men aged 20 - 60 with mild-moderate obstructive sleep apnea; HR: heart rate; NREM/REM: nonrapid/rapid eye movement, resp.; time-weighted mean arterial pressure (MAP), MAP values and heart rate for different periods calculated; placebo control

Results

title comp. had no significant effect on time-weighted MAP, MAP and HR at nocturnal sleep and under resting conditions in daytime, caused significant increase in SBP at ergometric and psychometric tests and in DBP at ergometric test (table, figure)

Reference

Heitmann, Joerg; Cassel, Werner; Grote, Ludger; Bickel, Ulrich; Hartlaub, Udo; Penzel, Thomas; Peter, Joerg Hermann

Clinical Pharmacology and Therapeutics, 1999 , vol. 65, # 3 p. 328 - 335 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

psychotonic

Species or Test-System (Pharmacological Data)

human

Sex

male

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

200 mg in the morning and 100 mg at midday

Method (Pharmacological Data)

daytime sleepiness determined by Multiple Sleep Latency Test (MSLT) and vigilance test performed; sleep latency for MSLT and reaction time for vigilance test measured

Further Details (Pharmacological Data)

26 healthy subjects aged 20 - 60 with mild to moderate obstructive sleep apnea; placebo control

Results

title comp. significantly shortened mean reaction time for vigilance test (to 1.23 s vs. control 1.46 s, resp.), significantly prolonged mean sleep latency (to 14.71 min vs. control 9.09 min), improving both from clear pathologic to ca. normal values

Reference

Heitmann, Joerg; Cassel, Werner; Grote, Ludger; Bickel, Ulrich; Hartlaub, Udo; Penzel, Thomas; Peter, Joerg Hermann

Clinical Pharmacology and Therapeutics, 1999 , vol. 65, # 3 p. 328 - 335 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

breath stimulant

Species or Test-System (Pharmacological Data)

human

Sex

male

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

200 mg in the morning and 100 mg at midday for 2 d

Method (Pharmacological Data)

respiration monitored by thermistor (oronasal airflow), thoracic and abdominal bands (uncalibrated inductive respiratory plethysmography), and oxygen saturation (pulse oximetry)

Further Details (Pharmacological Data)

26 healthy subjects aged 20 - 60 with mild to moderate obstructive sleep apnea; respiratory disturbance index (number of apneas and hypopneas) calculated; placebo control

Results

title comp. insignificantly decreased respiratory disturbance index to 32.5 events/h vs. 33.9 events/h in control

Reference

Heitmann, Joerg; Cassel, Werner; Grote, Ludger; Bickel, Ulrich; Hartlaub, Udo; Penzel, Thomas; Peter, Joerg Hermann

Clinical Pharmacology and Therapeutics, 1999 , vol. 65, # 3 p. 328 - 335 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

toxicity

Species or Test-System (Pharmacological Data)

human

Sex

male

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

200 mg given in the morning and 100 mg at midday for 2 d

Method (Pharmacological Data)

subjects were assessed for adverse events; routine laboratory tests performed

Further Details (Pharmacological Data)

26 healthy subjects aged 20 - 60 with mild to moderate obstructive sleep apnea; placebo control

Results

title comp. caused total of 7 adverse events; one adverse event (supraventricular tachycardia) was serious; routine laboratory tests showed no clinically relevant


changes

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Reference

Heitmann, Joerg; Cassel, Werner; Grote, Ludger; Bickel, Ulrich; Hartlaub, Udo; Penzel, Thomas; Peter, Joerg Hermann

Clinical Pharmacology and Therapeutics, 1999 , vol. 65, # 3 p. 328 - 335 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration (Pharmacological Data)

200 mg

Kind of Dosing (Pharmacological Data)

two 100 mg tablets of title comp. administered with 240 mL of water

Method (Pharmacological Data)

blood and urine samples collected at timed intervals up to 72 h postdose; title comp. and its metabolites conc. determined in plasma and urine by HPLC

Further Details (Pharmacological Data)

young males and females (26-29 years) and elderly males (63 years) were treated; Cmax: maximum plasma conc.; tmax: time to Cmax; CL/F: plasma oral clearance; V/D: apparent volume of distribution; CLrenal: renal clearance

Half-life Time (Pharmacological Data)

10.5 - 14.4 h

Results

title comp. Cmax = 5.20, 4.81, 4.21 μg/ml, tmax = 1.7, 2.0, 1.7 h, AUC = 61.3, 67.7, 57.0 μg*h/ml and CL/F = 0.88, 0.63, 0.72 ml/min/kg for young females, elderly males and young males, respectively; no difference in CLrenal and V/F

Reference

Wong, Y. Nancy; King, S. Peter; Simcoe, Donna; Gorman, Steve; Laughton, Watson; McCormick, George C.; Grebow, Peter

Journal of Clinical Pharmacology, 1999 , vol. 39, # 3 p. 281 - 288 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration (Pharmacological Data)

200 mg

Kind of Dosing (Pharmacological Data)

two 100 mg tablets of title comp. administered with 240 mL of water

Method (Pharmacological Data)

blood and urine samples collected at timed intervals up to 72 h postdose; title comp. and its metabolites conc. determined in plasma and urine by HPLC

Further Details (Pharmacological Data)

young males and females (26-29 years) and elderly males (63 years) were treated; MRTpo: mean residence time

Results

title comp. exhibited stereospecific pharmacokinetics: d-/l-title comp. enantiomers MRTpo (hr) values of 5.72/16.8, 4.83/14.2, 5.90/20.5 for young males, young females and elderly males, respectively (table)

Comment (Pharmacological Data)

Further metabolite(s)

Reference

Wong, Y. Nancy; King, S. Peter; Simcoe, Donna; Gorman, Steve; Laughton, Watson; McCormick, George C.; Grebow, Peter

Journal of Clinical Pharmacology, 1999 , vol. 39, # 3 p. 281 - 288 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

biotransformation

Species or Test-System (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration (Pharmacological Data)

200 mg

Kind of Dosing (Pharmacological Data)

two 100 mg tablets of title comp. administered with 240 mL of water

Method (Pharmacological Data)

blood and urine samples collected at timed intervals up to 72 h postdose; title comp. and its metabolites conc. determined in plasma and urine by HPLC


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Further Details (Pharmacological Data)

young males and females (26-29 years) and elderly males (63 years) were treated

Results

modafinil acid was the major urinary metabolite; percent of title comp. dose excreted in urine as modafinil acid = 35, 60 , 51 for young females, elderly males and young males, respectively

Metabolite (Pharmacological Data)

modafinil acid [Reaxys RN: 6650982] ; Modafinil sulfone [Reaxys RN: 9199801]

Comment (Pharmacological Data)

Further metabolite(s)

Reference

Wong, Y. Nancy; King, S. Peter; Simcoe, Donna; Gorman, Steve; Laughton, Watson; McCormick, George C.; Grebow, Peter

Journal of Clinical Pharmacology, 1999 , vol. 39, # 3 p. 281 - 288 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

biotransformation

Species or Test-System (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration (Pharmacological Data)

200 mg

Kind of Dosing (Pharmacological Data)

two 100 mg tablets of title comp. administered with 240 mL of water

Method (Pharmacological Data)

blood and urine samples collected at timed intervals up to 72 h postdose; title comp. and its metabolites conc. determined in plasma and urine by HPLC

Further Details (Pharmacological Data)

young males and females (26-29 years) and elderly males (63 years) were treated

Metabolite (Pharmacological Data)

d-modafinil [Reaxys RN: 10016759] ; l-modafinil [Reaxys RN: 10018841]

Reference

Wong, Y. Nancy; King, S. Peter; Simcoe, Donna; Gorman, Steve; Laughton, Watson; McCormick, George C.; Grebow, Peter

Journal of Clinical Pharmacology, 1999 , vol. 39, # 3 p. 281 - 288 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics; modulation of

Species or Test-System (Pharmacological Data)

human

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

200 mg

Method (Pharmacological Data)

title comp. given in combination with dextroamphetamine (10 mg); blood samples collected up to 48 h; plasma dextroamphetamine conc. measured by LC/MS/MS, its pharmacokinetic parameters calculated

Further Details (Pharmacological Data)

control: dextroamphetamine alone

Comment (Pharmacological Data)

No effect

Reference

Wong, Y. Nancy; Wang, Lixia; Hartman, Linda; Simcoe, Donna; Chen, Yusong; Laughton, Watson; Eldon, Richard; Markland, Colin; Grebow, Peter

Journal of Clinical Pharmacology, 1998 , vol. 38, # 10 p. 971 - 978 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

human

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

200 mg

Method (Pharmacological Data)

title comp. administered, blood samples collected up to 48 h; plasma title comp. and metabolites conc. measured by HPLC, pharmacokinetic parameters calculated

Further Details (Pharmacological Data)

AUC: area under serum conc.-time curve; Cmax: maximum serum conc.; tmax: time to Cmax; Cl/F: apparent oral clearance


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Half-life Time (Pharmacological Data)

11.3 h

Results

Cmax = 4.83 μg/ml; tmax = 1.8 h; AUC = 60.1 μg*h/ml; Cl/F = 0.81 ml/min/kg (table)

Metabolite (Pharmacological Data)

modafinil acid [Reaxys RN: 6650982] ; Modafinil sulfone [Reaxys RN: 9199801]

Reference

Wong, Y. Nancy; Wang, Lixia; Hartman, Linda; Simcoe, Donna; Chen, Yusong; Laughton, Watson; Eldon, Richard; Markland, Colin; Grebow, Peter

Journal of Clinical Pharmacology, 1998 , vol. 38, # 10 p. 971 - 978 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

drug interaction

Species or Test-System (Pharmacological Data)

human

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

200 mg

Kind of Dosing (Pharmacological Data)

single dose, two 100-mg tablets

Method (Pharmacological Data)

pharmacokinetic interaction with 40 mg threo-methylphenidate studied in 21 healthy men (27.6 +/- 6.2 years, 74.7 +/- 9.0 kg); title comp. and metabolites determined in plasma by HPLC from blood sampled up to 48 h postdose; adverse events recorded

Further Details (Pharmacological Data)

open-label 3 * 3 Latin square, randomized, single-dose, crossover study; threo-methylphenidate enantiomers determined in plasma by LC/MS/MS from blood sampled up to 18 h postdose

Half-life Time (Pharmacological Data)

12.3 h

Results

significant increases in tmax for title comp. (from 0.5-3.0 h to 1.0-6.0 h) and modafinil acid (from 1.0-4.0 h to 2.0-6.0 h); no effect on pharmacokinetic parameters of threo-methylphenidate enantiomers; no serious adverse events; graphs, tables

Metabolite (Pharmacological Data)

modafinil acid [Reaxys RN: 6650982] ; Modafinil sulfone [Reaxys RN: 9199801]

Reference

Wong, Y. Nancy; King, S. Peter; Laughton, Watson B.; McCormick, George C.; Grebow, Peter E.

Journal of Clinical Pharmacology, 1998 , vol. 38, # 3 p. 276 - 282 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-System (Pharmacological Data)

human

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

200 mg

Kind of Dosing (Pharmacological Data)

single dose, two 100-mg tablets

Method (Pharmacological Data)

pharmacokinetics studied in 21 healthy men (27.6 +/- 6.2 years, 74.7 +/- 9.0 kg); title comp. and metabolites determined in plasma by HPLC from blood sampled up to 48 h postdose

Further Details (Pharmacological Data)

open-label study

Half-life Time (Pharmacological Data)

12.2 h

Results

parameters for title comp. / modafinil acid: Cmax 4.10 / 1.91 μg/ml, tmax 2.0 (0.5-3.0) / 3.0(1.0-4.0) h, AUC0-infinity 56.9 / 22.6 γ*h/ml, total systemic plasma clearance of title comp. 62.0 ml/min; graphs, table

Metabolite (Pharmacological Data)

modafinil acid [Reaxys RN: 6650982] ; Modafinil sulfone [Reaxys RN: 9199801]

Reference

Wong, Y. Nancy; King, S. Peter; Laughton, Watson B.; McCormick, George C.; Grebow, Peter E.

Journal of Clinical Pharmacology, 1998 , vol. 38, # 3 p. 276 - 282 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antisedative

Species or Test-System (Pharmacological Data)

Wistar rat


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Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

30 - 300 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. suspended in sterile 0.25 percent methylcellulose

Method (Pharmacological Data)

rats treated with title comp. 5 h after lights on; LMA (every 10 s) and Tb (every min) monitored via i.p. telemetry; sleep-wakefulness determined by EEG every 10 s

Further Details (Pharmacological Data)

control: vehicle; reference comp.: METH (methamphetamine); LMA: locomotor activity; Tb: body temperature; EEG: electroencephalogram

Results

during the first 3 h posttreatment, title comp. dose-dependently increased wake time (diagram); title comp. did not produce rebound hypersomnolence and increased LMA less than METH

Reference

Edgar, Dale M.; Seidel, Wesley F.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 283, # 2 p. 757 - 769 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

increase of dopamine release

Species or Test-System (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

30 - 300 mg/kg

Kind of Dosing (Pharmacological Data)

doses in 0.5 percent arabic gum solution

Method (Pharmacological Data)

rat weight 300-350 g; 5-7 rats/group; halothane-anaesthesia; microdialysis probe implantation into intermediate nucleus accumbens; title comp. injection; perfusate collected every 20 min for 120 min; reverse-phase HPLC-ED

Further Details (Pharmacological Data)

time - dopamine release curve

Results

title comp. dose-dependently increased accumbens dopamine release, reaching peak effect at 40 min after injection from 100 to 300 mg/kg, but not at 30 mg/kg (diagram given)

Reference

Ferraro, Luca; Tanganelli, Sergio; O'Connor, William Thomas; Antonelli, Tiziana; Rambert, Francis; Fuxe, Kjell

European Journal of Pharmacology, 1996 , vol. 306, # 1-3 p. 33 - 39 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

decrease of GABA release

Species or Test-System (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

30 - 300 mg/kg

Kind of Dosing (Pharmacological Data)

doses in 0.5 percent arabic gum solution

Method (Pharmacological Data)

rat weight 300-350 g; 7 rats/group; halothane-anaesthesia; microdialysis probe implantation into intermediate nucleus accumbens; title comp. injection; perfusate collected every 20 min for 120 min; reverse-phase HPLC-ED

Further Details (Pharmacological Data)

time - γ-aminobutyric acid (GABA) release curve

Results

title comp. dose-dependently decreased accumbens GABA release from 100 to 300 mg/kg, but not at 30 mg/kg (diagram given)

Reference

Ferraro, Luca; Tanganelli, Sergio; O'Connor, William Thomas; Antonelli, Tiziana; Rambert, Francis; Fuxe, Kjell

European Journal of Pharmacology, 1996 , vol. 306, # 1-3 p. 33 - 39 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

Species or Test-System (Pharmacological Data)

guinea pig

Sex

male and female

Route of Application

subcutaneous


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Concentration (Pharmacological Data)

30 mg/kg

Method (Pharmacological Data)

γ-aminobutyric acid outfow (AAO, mass-fragmentography) from parietal cortex with or without pretreatment with 125 μg i.c.v. 5,7-dihydroxytriptamine (5,7-DHT, 7 d befor exp.); dopamine (D) and noradrenaline (N) levels in the cortex (HPLC)

Results

rapid and long-lasting inhibition of AAO; 5,7-DHT pretreatment caused slight increase, instead of decrease, in AAO; D not affected; N enhanced significantly

Reference

Tanganelli; de la Mora; Ferraro; Mendez-Franco; Beani; Rambert; Fuxe

European Journal of Pharmacology, 1995 , vol. 273, # 1-2 p. 63 - 71 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

Species or Test-System (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

30 mg/kg

Method (Pharmacological Data)

γ-aminobutyric acid outfow (AAO) from parietal cortex (mass-fragmentography)

Results

rapid and long-lasting inhibition of AAO

Reference

Tanganelli; de la Mora; Ferraro; Mendez-Franco; Beani; Rambert; Fuxe

European Journal of Pharmacology, 1995 , vol. 273, # 1-2 p. 63 - 71 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

Species or Test-System (Pharmacological Data)

guinea pig

Sex

male and female

Route of Application

subcutaneous

Concentration (Pharmacological Data)

30 mg/kg/d

Exposure Period (Pharmacological Data)

8 d

Method (Pharmacological Data)

γ-aminobutyric acid outfow (AAO, mass-fragmentography) from parietal cortex with or without pretreatment with 125 μg i.c.v. 5,7-dihydroxytriptamine (5,7-DHT, 7 d befor exp.) or 35.8 ng/kg i.p. prazosin (P, 30 min befor admin. of title comp.)

Further Details (Pharmacological Data)

noradrenalin (N), 5-hydroxytriptamine (5-HT) and dopamine (D) levels (HPLC)

Results

significantly inhibited AAO; 5,7-DHT pretreatment caused consistent and prolonged enhancement in AAO; D not affected; N enhanced significantly; counter-acted 5,7DHT-induced reduction on 5-HT level; treatment with P completely prevented increase of AAO

Reference

Tanganelli; de la Mora; Ferraro; Mendez-Franco; Beani; Rambert; Fuxe

European Journal of Pharmacology, 1995 , vol. 273, # 1-2 p. 63 - 71 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

agonist

Species or Test-System (Pharmacological Data)

Wistar rat brain

Sex

male

Concentration (Pharmacological Data)

1 - 1000 μmol/l

Method (Pharmacological Data)

brain slices of patogen-free rats incubated in Krebs-Ringer medium containing 1 μM <3H>-γ-aminobutyric acid (<3H>GABA); <3H>GABA uptake and release (scintillation spectrometry); glutamic acid decarboxylase activity

Comment (Pharmacological Data)

No effect

Reference

Tanganelli; de la Mora; Ferraro; Mendez-Franco; Beani; Rambert; Fuxe

European Journal of Pharmacology, 1995 , vol. 273, # 1-2 p. 63 - 71 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

effect on sleep architecture, sleep and awakening quality in elderlies

Reference

Saletu; Frey; Krupka; Anderer; Grunberger; Barbanoj


Arzneimittel-Forschung/Drug Research, 1989 , vol. 39, # 10 p. 1268 - 1273 Title/Abstract Full Text View citing articles Show Details

Other Data Use (327) Use Pattern

Location

Reference

Pharmaceuticals

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details

acute pain in combination with analgesic

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details

acute pain in combination with antihistamine

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details

acute pain in combination with barbiturate

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details

acute pain in combination with benzodiazepine

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details

acute pain in combination with kappa receptor agonist

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details

acute pain in combination with non-steroidal anti-inflammatory agent

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details

acute pain in combination with opioid mu receptor agonist

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details

acute pain in combination with opioid receptor agonist

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details

anethesia in combination with analgesic

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details

anethesia in combination with antihistamine

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details

anethesia in combination with barbiturate

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details

anethesia in combination with benzodiazepine

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details

anethesia in combination with kappa receptor agonist

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details


anethesia in combination with non-steroidal anti-inflammatory agent

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

Title/Abstract Full Text Show Details

anethesia in combination with opioid mu receptor agonist

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

Title/Abstract Full Text Show Details

anethesia in combination with opioid receptor agonist

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

Title/Abstract Full Text Show Details

chronic pain in combination with analgesic

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

Title/Abstract Full Text Show Details

chronic pain in combination with antihistamine

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

Title/Abstract Full Text Show Details

chronic pain in combination with barbiturate

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

Title/Abstract Full Text Show Details

Use Pattern

Location

Reference

chronic pain in combination with benzodiazepine

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

chronic pain in combination with kappa receptor agonist

chronic pain in combination with non-steroidal anti-inflammatory agent

chronic pain in combination with opioid mu receptor agonist

chronic pain in combination with opioid receptor agonist

for treating drug abuse in combination with analgesic

for treating drug abuse in combination with antihistamine

for treating drug abuse in combination with barbiturate

for treating drug abuse in combination with benzodiazepine

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details


Title/Abstract Full Text Show Details

for treating drug abuse in combination with kappa receptor agonist

for treating drug abuse in combination with non-steroidal anti-inflammatory agent

for treating drug abuse in combination with opioid mu receptor agonist

for treating drug abuse in combination with opioid receptor agonist

obstructive sleep apnea in combination with analgesic

obstructive sleep apnea in combination with antihistamine

obstructive sleep apnea in combination with barbiturate

obstructive sleep apnea in combination with benzodiazepine

obstructive sleep apnea in combination with kappa receptor

obstructive sleep apnea in combination with non-steroidal anti-inflammatory agent

obstructive sleep apnea in combination with opioid mu receptor agonist

obstructive sleep apnea in combination with opioid receptor agonist

preventing or deterring abuse of the therapeutic agent in combination with analgesic

preventing or deterring abuse of the therapeutic agent in combination with antihistamine

preventing or deterring abuse of the therapeutic agent in combination with barbiturate

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

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preventing or deterring abuse of the therapeutic agent in combination with benzodiazepine

preventing or deterring abuse of the therapeutic agent in combination with kappa receptor agonist

preventing or deterring abuse of the therapeutic agent in combination with non-steroidal anti-inflammatory agent

preventing or deterring abuse of the therapeutic agent in combination with opioid mu receptor agonist

preventing or deterring abuse of the therapeutic agent in combination with opioid receptor agonist

sleep apnea in combination with analgesic

sleep apnea in combination with antihistamine

sleep apnea in combination with barbiturate

sleep apnea in combination with benzodiazepine

sleep apnea in combination with kappa receptor agonist

sleep apnea in combination with non-steroidal anti-inflammatory agent

sleep apnea in combination with opioid mu receptor agonist

sleep apnea in combination with opioid receptor agonist

Pharmaceuticals

abuse deterrent in combination with an abuse deterrent active

Kleine-Levin syndrome

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

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HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 62-67

HSU, John

Patent: WO2017/15309 A1, 2017 ;

Page/Page column title page; 32-34

SELA, Yoram; LAMENSDORF, Itschak

Patent: WO2016/181218 A1, 2016 ;

Page/Page column title page; 32-34

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Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

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Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

SELA, Yoram; LAMENSDORF, Itschak

Patent: WO2016/181218 A1, 2016 ; Title/Abstract Full Text Show Details

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck;


CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

Parkinson disease

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

Periodic Lim Movement Disorders (PLMD)

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

Pharmaceuticals

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

alertness disorders

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

anxiety disorders

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

attention deficit hyperactivity disorder (ADHD)

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

attention disorders

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

bipolar disorder

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

breathing difficulty and fatigue, notably due to cancer, neurodegenerative disorders, menopause, traumatic brain injuries, viral infection or post-myelitis, or to fibromyalgia

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

cataplexy in narcoleptic patients

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

central sleep apnea

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ;


Title/Abstract Full Text Show Details

chronic renal failure

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

circadian rhythm disorders

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

dementia

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

dependence or addiction (to games, drugs, alcohol, tobacco, etc.)

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

depression

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

disorders after sleep restriction or sleep deprivation

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

enhancing the memory

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

excessive daytime sleepiness (EDS)

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

fecal or urinary incontinence

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

hyperphagia

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

idiopathic hypersomnia

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details


in combination with flecainide

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

insomnia

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

insufficient sleep time

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

jet-lag

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

liver failure

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

maintaining healthy subjects awake for long-lasting periods of time

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

malaise

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

manic episode

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

medication-induced somnolence (due to benzodiazepines, barbiturates, sleeping pills, antidepressants, anti-psychotics...)

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

mood disorders

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

multiple sclerosis

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

narcolepsy (with or without cataplexy)

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu


Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

neuromuscular disorders

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

obesity

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

obsessive-compulsive disorder

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

obstructive sleep apnea/hypopnea (SAHOS)

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

parasomnia

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

post-traumatic stress disorder (PTSD)

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

premature ejaculation

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

respiratory disorders

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

restless legs syndrome (RLS)

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

rheumatologic disorders

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

schizophrenia

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details


senility

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

shift work sleep disorder

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

sleep disorders

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

sleepiness

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

stroke

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

structural brain disorders

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

tinnitus

Page/Page column 41-42

COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu

Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details

psychostimulant

Ayala, William J.

Patent: US2005/31688 A1, 2005 ; Title/Abstract Full Text Show Details

H. LUNDBECK A/S Patent: WO2009/76961 A1, 2009 ; Title/Abstract Full Text Show Details

alpha1-adrenergic agonist

QUESTCOR PHARMACEUTICALS, INC.

Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details

in combination with alpha2-adrenergic agonist or baclofen

QUESTCOR PHARMACEUTICALS, INC.

Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details

somnolence

QUESTCOR PHARMACEUTICALS, INC.

Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details

lethargy

QUESTCOR PHARMACEUTICALS, INC.

Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details


dizziness

QUESTCOR PHARMACEUTICALS, INC.

Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details

drowsiness

QUESTCOR PHARMACEUTICALS, INC.

Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details

lightheadedness

QUESTCOR PHARMACEUTICALS, INC.

Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details

increased weakness

QUESTCOR PHARMACEUTICALS, INC.

Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details

confusion

QUESTCOR PHARMACEUTICALS, INC.

Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details

unsteadiness

QUESTCOR PHARMACEUTICALS, INC.

Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details

clumsiness

QUESTCOR PHARMACEUTICALS, INC.

Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details

pain

QUESTCOR PHARMACEUTICALS, INC.

Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details

attenuating muscle spasticity

QUESTCOR PHARMACEUTICALS, INC.

Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details

Premature ejaculation (PE)

NEUROHEALING PHARMACEUTICALS, INC.

Patent: WO2008/21341 A2, 2008 ; Title/Abstract Full Text Show Details

Excessive daytime sleepiness (EDS)

NEUROHEALING PHARMACEUTICALS, INC.

Patent: WO2008/21341 A2, 2008 ; Title/Abstract Full Text Show Details

Cognitive dysfunction associated with fibromyalgia

CYPRESS BIOSCIENCE, INC.

Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details

Cognitive dysfunction associated with fibromyalgia syndrome (FMS)

CYPRESS BIOSCIENCE, INC.

Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details

Cognitive dysfunction

CYPRESS BIOSCIENCE, INC.

Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details

fibromyalgia syndrome (FMS)

CYPRESS BIOSCIENCE, INC.

Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details

Pain

CYPRESS BIOSCIENCE, INC.

Patent: WO2008/21932 A2, 2008 ;


Title/Abstract Full Text Show Details

Fatigue

CYPRESS BIOSCIENCE, INC.

Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details

Symptoms of cognitive dysfunction

CYPRESS BIOSCIENCE, INC.

Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details

Symptoms associated with fibromyalgia

CYPRESS BIOSCIENCE, INC.

Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details

fibromyalgia

CYPRESS BIOSCIENCE, INC.

Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details

quality of life

CYPRESS BIOSCIENCE, INC.

Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details

Mood

CYPRESS BIOSCIENCE, INC.

Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details

active ingredient of multimodal abuse resistant pharmaceutical composition

THERAQUEST BIOSCIENCES, INC.

Patent: WO2008/33351 A2, 2008 ; Title/Abstract Full Text Show Details

active ingredient of multimodal extended release pharmaceutical composition

THERAQUEST BIOSCIENCES, INC.

Patent: WO2008/33351 A2, 2008 ; Title/Abstract Full Text Show Details

active ingredient of multimodal extended release abuse resistant pharmaceutical composition

THERAQUEST BIOSCIENCES, INC.

Patent: WO2008/33351 A2, 2008 ; Title/Abstract Full Text Show Details

Neurogenic agent

BRAINCELLS, INC.

Patent: WO2008/39863 A2, 2008 ; Title/Abstract Full Text Show Details

sleepiness

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

CEPHALON, INC.

Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details

Cephalon France

Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details

QUESTCOR PHARMACEUTICALS, INC.

Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details

tiredness

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

QUESTCOR PHARMACEUTICALS, INC.

Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details


Promote wakefulness

INTRA-CELLULAR THERAPIES, INC.

Patent: WO2008/63505 A1, 2008 ; Title/Abstract Full Text Show Details

Regulate sleep

INTRA-CELLULAR THERAPIES, INC.

Patent: WO2008/63505 A1, 2008 ; Title/Abstract Full Text Show Details

Restless leg syndrome (RLS)

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

Periodic limb movement in sleep (PLMS)

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

Snoring ICSD 780.53-1

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

Snoring

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

unpleasant leg sensations associated with unwanted leg movements

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

unwanted involuntary leg movements at rest

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

unwanted involuntary leg movements awake

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

unwanted involuntary leg movements asleep

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

Restless leg syndrome (RLS) symptoms

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

Excessive sleepiness associated with narcolepsy

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

Excessive sleepiness associated with obstructive sleep apnea/hypopnea syndrome (OSA/HS)

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

Shift work sleep disorder (SWSD)

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

Allows restful sleep

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

unpleasant sensation to move the leg

LAVIN, Thomas, N.


Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

unpleasant urgency to move the leg

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

undesired involuntary limb movements

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

Primary snoring unrelated to sleep apnea

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

Primary snoring

LAVIN, Thomas, N.

Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details

Pharmaceutical composition for treating disease, disorder, or medical condition mediated by histamine H3 receptor activity

JANSSEN PHARMACEUTICA N.V.

Patent: WO2008/109336 A1, 2008 ; Title/Abstract Full Text Show Details

adrenergic agonist

BrainCells, Inc.

Patent: US2007/270449 A1, 2007 ; Title/Abstract Full Text Show Details

BrainCells, Inc.

Patent: US2008/64671 A1, 2008 ; Title/Abstract Full Text Show Details

diseases and conditions of the central and peripheral nervous system

BrainCells, Inc.

Patent: US2008/64671 A1, 2008 ; Title/Abstract Full Text Show Details

neurogenic agent

BrainCells, Inc.

Patent: US2007/270449 A1, 2007 ; Title/Abstract Full Text Show Details

BrainCells, Inc.

Patent: US2008/64671 A1, 2008 ; Title/Abstract Full Text Show Details

additional active ingredient of a composition comprising a neurogenic agent and suitable for treating nervous system disorders

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

second neurogenic agent that enhances a neurogenic effect of the first neurogenic agent

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

nerve cell trauma

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

psychiatric condition

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

neurologically related condition

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

neural stem cell disorder

BrainCells, Inc.


Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

neural progenitor cell disorder

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

degenerative disease of the retina

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

ischemic disorder

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

affective disorder

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

depression

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

CEPHALON, INC.

Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details

Cephalon France

Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

major depression

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

refractory depression

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

hypomania

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

panic attacks

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

anxiety

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

excessive elation

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

bipolar depression

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

bipolar disorder

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ;


Title/Abstract Full Text Show Details

seasonal mood disorder

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

schizophrenia

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

psychosis

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

lissencephaly syndrome

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

anxiety syndrome

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

anxiety disorder

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

phobia

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

stress

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

stress syndrome

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

cognitive function disorder

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

aggression

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

drug abuse

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

alcohol abuse

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

obsessive compulsive behavior syndrome

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details


borderline personality disorder

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

non-senile dementia

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

post-pain depression

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

postpartum depression

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

cerebral palsy

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

post traumatic stress disorder (PTSD)

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

learning disorder

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

autism

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

attention deficit disorder

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

sleep disorder

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

cognitive disorder

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

epilepsy

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

temporal lobe epilepsy

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

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HAAS, Magali

Patent: US2008/103199 A1, 2008 ; Title/Abstract Full Text Show Details

narcolepsy

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

CEPHALON, INC.

Patent: WO2005/27890 A1, 2005 ;


Title/Abstract Full Text Show Details

BrainCells, Inc.

Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details

GENERICS [UK] LIMITED; MYLAN DEVELOPMENT CENTRE PRIVATE LIMITED

Patent: WO2008/149141 A2, 2008 ; Title/Abstract Full Text Show Details

GENERICS [UK] LIMITED; MYLAN DEVELOPMENT CENTRE PRIVATE LIMITED

Patent: WO2008/149141 A2, 2008 ;

obstructive sleep apnoea/hypopnoea syndrome (OSAHS)

Title/Abstract Full Text Show Details

GENERICS [UK] LIMITED; MYLAN DEVELOPMENT CENTRE PRIVATE LIMITED

Patent: WO2008/149141 A2, 2008 ;

shift work sleep disorder (SWSD)

Title/Abstract Full Text Show Details

NEUROHEALING PHARMACEUTICALS, INC.

Patent: WO2007/13962 A2, 2007 ;

promoting CNS stimulation as an adrenergic agonist; activates glutamatergic circuits while inhibiting GABA; inhibits of dopamine reuptake, indirect inhibits of noradrenalin reuptake in the VLPO and orexin activation; has partial alpha 1B-adrenergic agonist effects by directly stimulating the receptors

Use Pattern promoting or enhancing the state of wakefulness

Location

Title/Abstract Full Text Show Details

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Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details

promoting or enhancing the state of alertness

NEUROHEALING PHARMACEUTICALS, INC.

Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details

central nervous system stimulation

NEUROHEALING PHARMACEUTICALS, INC.

Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details

excessive daytime sleepiness (EDS)

NEUROHEALING PHARMACEUTICALS, INC.

Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details

individuals who suffer from narcolepsy

NEUROHEALING PHARMACEUTICALS, INC.

Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details

promoting a patient's recovery from anesthesia

NEUROHEALING PHARMACEUTICALS, INC.

Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details

attention deficit disorder (ADD)

NEUROHEALING PHARMACEUTICALS, INC.

Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details

attention deficit hyperactivity disorder (ADHD)

NEUROHEALING PHARMACEUTICALS, INC.

Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details

neurorehabilitation program

NEUROHEALING PHARMACEUTICALS, INC.

Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details

treat an impaired neurological function

NEUROHEALING PHARMACEUTICALS, INC.

Patent: WO2007/13962 A2, 2007 ;


Title/Abstract Full Text Show Details

Pharmaceutical agent for a coated coronary stent

MICELL TECHNOLOGIES, INC.

Patent: WO2007/11707 A2, 2007 ; Title/Abstract Full Text Show Details

Long-term therapy for fibromyalgia syndrome (FMS)

Cypress Bioscience, Inc.

Patent: US2007/72946 A1, 2007 ; Title/Abstract Full Text Show Details

Fibromyalgia

Cypress Bioscience, Inc.

Patent: US2007/72946 A1, 2007 ; Title/Abstract Full Text Show Details

Acute pain

Cypress Bioscience, Inc.

Patent: US2007/72946 A1, 2007 ; Title/Abstract Full Text Show Details

Long-term therapy of a pain symptom associated with fibromyalgia syndrome

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Patent: US2007/72946 A1, 2007 ; Title/Abstract Full Text Show Details

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Mallinckrodt Inc.

Patent: US2007/129444 A1, 2007 ; Title/Abstract Full Text Show Details

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Mallinckrodt Inc.

Patent: US2007/129444 A1, 2007 ; Title/Abstract Full Text Show Details

adrenoceptor agonist

BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG

Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details

Attention Deficit Hyperactivity Disorder (ADHD)

BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG

Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details

Attention Deficit Hyperactivity Disorder (ADHD) predominantly impulsivity type

BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG

Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details

Attention Deficit Hyperactivity Disorder (ADHD) predominantly inattentive type

BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG

Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details

Attention Deficit Hyperactivity Disorder (ADHD) predominantly hyperactive-impulsive type

BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG

Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details

Attention Deficit Hyperactivity Disorder (ADHD) predominantly not otherwise specified

BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG

Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details

Attention Deficit Disorder (ADD)

BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG

Patent: WO2007/93624 A2, 2007 ;


Title/Abstract Full Text Show Details

tablets

HIKMA PHARMACEUTICALS

Patent: US2007/275057 A1, 2007 ; Title/Abstract Full Text Show Details

modulator of α1-adrenergic receptor

BrainCells, Inc.

Patent: US2007/270449 A1, 2007 ; Title/Abstract Full Text Show Details

Stimulant

PediaMed Pharmaceuticals, Inc.

Patent: US2004/259809 A1, 2004 ; Title/Abstract Full Text Show Details

Melker, Richard J.; Gold, Mark S.

Patent: US2006/62734 A1, 2006 ; Title/Abstract Full Text Show Details

sleep apnea

CEPHALON, INC.

Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details

Cypress Bioscience, Inc.

Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details

alpha-1 adrenergic receptor agonist

Cypress Bioscience, Inc.

Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details

sleep related breathing disorder

Cypress Bioscience, Inc.

Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details

therapy

Cypress Bioscience, Inc.

Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details

pharmaceutical composition

Cypress Bioscience, Inc.

Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details

combination therapy

Cypress Bioscience, Inc.

Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details

daytime drowsiness

Cypress Bioscience, Inc.

Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details

adjuvant therapy with positive airway pressure (PAP) therapy

Cypress Bioscience, Inc.

Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details

improving patient tolerance to positive airway pressure therapy

Cypress Bioscience, Inc.

Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details

sleep hypopnea

Cypress Bioscience, Inc.

Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details

modify biotransformation of drugs to metabolites; CYP inducer

Carter, Andrew

Patent: US2006/222627 A1, 2006 ;


Title/Abstract Full Text Show Details

Restenosis

Carter, Andrew

Patent: US2006/222627 A1, 2006 ; Title/Abstract Full Text Show Details

vascular disease

Carter, Andrew

Patent: US2006/222627 A1, 2006 ; Title/Abstract Full Text Show Details

Neointimal hyperplasia

Carter, Andrew

Patent: US2006/222627 A1, 2006 ; Title/Abstract Full Text Show Details

inhibitor of CYP2C19

Mutual Pharmaceutical Company, Inc.

Patent: US7122566 B1, 2006 ; Title/Abstract Full Text Show Details

inducer of CYP1A2

Mutual Pharmaceutical Company, Inc.

Patent: US7122566 B1, 2006 ; Title/Abstract Full Text Show Details

Impulse control disorders

CENTRE FOR ADDICTION AND MENTAL HEALTH

Patent: WO2006/32146 A1, 2006 ; Title/Abstract Full Text Show Details

promotion of wakefulness

Cephalon France

Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details

treatment of Parkinson's disease

Cephalon France

Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details

cerebral ischemia

Cephalon France

Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details

stroke

Cephalon France

Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details

eating disorders

Cephalon France

Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details

stimulation of appetite and weight gain

Cephalon France

Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details

treatment of attention deficit hyperactivity disorder

Cephalon France

Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details

treatment of attention deficit hyperactivity fatigue

Cephalon France

Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details

improvement of cognitive dysfunction

Cephalon France

Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details


CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ;

shift work

Title/Abstract Full Text Show Details

Cephalon France

Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ;

sleep apneas

Title/Abstract Full Text Show Details

Cephalon France

Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ;

sleep disorders

Title/Abstract Full Text Show Details

Cephalon France

Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details

Neurotransmitter modulator

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JANSSEN PHARMACEUTICA, N.V.

Patent: WO2006/66197 A1, 2006 ; Title/Abstract Full Text Show Details

component of pharmaceutical compositions

Ray, Anup Kumar; Nandi, Indranil; Palaniswamy, Suresh; Davila, Pablo; Vora, Aakanksha Harshad

Patent: US2005/8704 A1, 2005 ; Title/Abstract Full Text Show Details

energizer

Ayala, William J.

Patent: US2005/31688 A1, 2005 ; Title/Abstract Full Text Show Details

invigorant

Ayala, William J.

Patent: US2005/31688 A1, 2005 ; Title/Abstract Full Text Show Details

nervous system stimulant

Ayala, William J.

Patent: US2005/31688 A1, 2005 ; Title/Abstract Full Text Show Details

altering the somnolent state of a mammal

CEPHALON, INC.

Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details

disorders of sleep and wakefulness

CEPHALON, INC.

Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details

excessive daytime sleepiness

CEPHALON, INC.

Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details

urinary incontinence

CEPHALON, INC.

Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details

multiple sclerosis fatigue

CEPHALON, INC.

Patent: WO2005/27890 A1, 2005 ;


Title/Abstract Full Text Show Details

ADHD

CEPHALON, INC.

Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details

Alzheimer's disorder

CEPHALON, INC.

Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details

ischemia

CEPHALON, INC.

Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details

acute day-time sleepiness attack

BECTON, DICKINSON and COMPANY

Patent: WO2005/46701 A1, 2005 ; Title/Abstract Full Text Show Details

active component of composition having improved solubility of a hydrophobic drug and a compound having at least one carboxylic acid moiety for treating schizophrenia

Barbera, Gary; Doshi, Chetan Chhabildas; Patel, Mahendra R.; Davila, Pablo; Patel, Satishkumar Ambalal

Patent: US2005/249814 A1, 2005 ; Title/Abstract Full Text Show Details

excessive sleepiness

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

CEPHALON, INC.

Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details

obstructive sleep apnea

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

CEPHALON, INC.

Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details

Improving sleep quality

SEPRACOR INC.

Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details

insomnia

SEPRACOR INC.

Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details

transient insomnia

SEPRACOR INC.

Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details

short-term insomnia

SEPRACOR INC.

Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details

chronic insomnia

SEPRACOR INC.

Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details

Parkinson's disease

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

CEPHALON, INC.


Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details

SEPRACOR INC.

Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details

cerebral tissue from ischemia

SEPRACOR INC.

Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details

urinary and fecal incontinence

SEPRACOR INC.

Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details

sleep apneas of central origin

SEPRACOR INC.

Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details

Component of composition for treating allergic reactions and other histamine-mediated symptoms

PediaMed Pharmaceuticals, Inc.

Patent: US2004/259809 A1, 2004 ; Title/Abstract Full Text Show Details

To reduce or alleviate the sedation caused by the antihistamine

PediaMed Pharmaceuticals, Inc.

Patent: US2004/259809 A1, 2004 ; Title/Abstract Full Text Show Details

appetite stimulant

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

attention disorders

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

central nervous system disorders

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

depressive mood

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

excessive sleepiness associated with a disease

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

excessive sleepiness associated with narcolepsy

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

fatigue

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

food behavior disorders

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ;


Title/Abstract Full Text Show Details

hyperactivity (ADHD)

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

hypersomnia in cancer patients

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

hypersomnia

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

idiopathic hypersomnia

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

jet lag

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

neurodegenerative diseases

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

particularly tiredness and fatigue associated with multiple sclerosis

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

protecting cerebral tissue from ischemia

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

relieve severe pain

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

stimulating cognitive functions

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

time lag

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

vigilance disorders associated with Steinert's disease

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

vigilance disorders

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details


weak sunlight (sundowning)

CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE

Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details

treatment of narcolepsia

CHEMAGIS LTD.

Patent: EP1260501 A1, 2002 ; Title/Abstract Full Text Show Details


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