Query Query
Results
Date
3 substances in Reaxys
2018-06-10 19h:39m:50s (UTC)
Na2 + O–
O– P
O O
1. Query
O
Search as: As drawn ))
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Reaxys ID 12826505 View in Reaxys
1/3 O P O
2
Na +
Chemical Name: fospropofol disodium; fospropofol; phosphoric acid mono(2,6-diisopropylphenoxymethyl)ester disodium; Aquavan(R); GPI15715; disodium (2,6-diisopropylphenoxy)methyl phosphate; Ophosphonooxymethyl propofol disodium salt Linear Structure Formula: C13H19O5P(2-)*2Na(1+) Molecular Formula: C13H19O5P*2Na Molecular Weight: 332.244 InChI Key: FVLUXVLPXDIGAK-UHFFFAOYSA-L Note:
O– O–
O
Substance Label (4) Label References 35
Qin, Linlin; Ren, Lei; Wan, Songlin; Liu, Guoliang; Luo, Xinfeng; Liu, Zhenhong; Li, Fangqiong; Yu, Yan; Liu, Jianyu; Wei, Yonggang; Journal of Medicinal Chemistry; vol. 60; nb. 9; (2017); p. 3606 - 3617, View in Reaxys
Formula I
Patent; Shanxi Synthetic Pharmaceutical Co., Ltd.; Jiangsu Tiandi Renhe Pharmaceutical Co., Ltd.; Zhang Qiyuan; (10 pag.); CN106674270; (2017); (A) Chinese, View in Reaxys
1
Patent; Yichang humanwell pharmaceutical Co., Ltd; Li, Lie; Li, Jie; Fu, Yigang; Wang, Min; Xu, Huabin; Ye, Xia; (15 pag.); CN103172658; (2016); (B) Chinese, View in Reaxys
5, GPI 15715
Kumpulainen, Hanna; Jaervinen, Tomi; Mannila, Anne; Leppaenen, Jukka; Nevalainen, Tapio; Maentylae, Antti; Vepsaelaeinen, Jouko; Rautio, Jarkko; European Journal of Pharmaceutical Sciences; vol. 34; nb. 2-3; (2008); p. 110 - 117, View in Reaxys
Patent-Specific Data (4) References Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys Patent; MGI GP, INC.; WO2007/8869; (2007); (A1) English, View in Reaxys Patent; GUILFORD PHARMACEUTICALS, INC.; WO2006/33911; (2006); (A2) English, View in Reaxys Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys Druglikeness (1) 1 of 1
LogP
2.524
H Bond Donors
0
H Bond Acceptors
4
Rotatable Bonds
6
TPSA
91.46
Lipinski Number
4
Veber Number
2
Density (1) 1 of 1
Measurement Temperature 22.84 [°C] Type (Density)
crystallographic
Location
Paragraph 0034
Patent; Shanxi Synthetic Pharmaceutical Co., Ltd.; Jiangsu Tiandi Renhe Pharmaceutical Co., Ltd.; Zhang Qiyuan; (10 pag.); CN106674270; (2017); (A) Chinese, View in Reaxys Crystal Property Description (1) Colour & Other Location Properties white
supporting informa- Yang, Jun; Yin, Wang; Liu, Jin; Wang, Yu; Zhou, Cheng; Kang, Yi; Zhang, Wen-Sheng; Bition oorganic and Medicinal Chemistry Letters; vol. 23; nb. 6; (2013); p. 1813 - 1816, View in Reaxys
Crystal System (1) Crystal System Location Monoclinic
References
Paragraph 0034
References Patent; Shanxi Synthetic Pharmaceutical Co., Ltd.; Jiangsu Tiandi Renhe Pharmaceutical Co., Ltd.; Zhang Qiyuan; (10 pag.); CN106674270; (2017); (A) Chinese, View in Reaxys
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Solubility (MCS) (1) 1 of 1
Location
Page/Page column 2; 4; 5
Comment (Solubility (MCS))
soluble in water
Patent; Yichang humanwell pharmaceutical Co., Ltd; Li, Lie; Li, Jie; Fu, Yigang; Wang, Min; Xu, Huabin; Ye, Xia; (15 pag.); CN103172658; (2016); (B) Chinese, View in Reaxys Space Group (1) Space Group
Location
Comment (Space Group)
References
14
Paragraph 0034
a = 19.755 Å; b = 5.7663 Å; c = 15.425 Å; β = 103.226 °; Z = 4; T = 296 K; Method = X-ray diffraction
Patent; Shanxi Synthetic Pharmaceutical Co., Ltd.; Jiangsu Tiandi Renhe Pharmaceutical Co., Ltd.; Zhang Qiyuan; (10 pag.); CN106674270; (2017); (A) Chinese, View in Reaxys
NMR Spectroscopy (5) 1 of 5
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
1H
Coupling Nuclei
1H
Solvents (NMR Spectroscopy)
water-d2
Temperature (NMR Spectroscopy) [°C]
25
Frequency (NMR Spectro- 300 scopy) [MHz] Location
supporting information
Yang, Jun; Yin, Wang; Liu, Jin; Wang, Yu; Zhou, Cheng; Kang, Yi; Zhang, Wen-Sheng; Bioorganic and Medicinal Chemistry Letters; vol. 23; nb. 6; (2013); p. 1813 - 1816, View in Reaxys 2 of 5
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
13C
Solvents (NMR Spectroscopy)
water-d2
Temperature (NMR Spectroscopy) [°C]
25
Location
supporting information
Yang, Jun; Yin, Wang; Liu, Jin; Wang, Yu; Zhou, Cheng; Kang, Yi; Zhang, Wen-Sheng; Bioorganic and Medicinal Chemistry Letters; vol. 23; nb. 6; (2013); p. 1813 - 1816, View in Reaxys 3 of 5
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectroscopy)
D2O
Temperature (NMR Spectroscopy) [°C]
25
Frequency (NMR Spectro- 500 scopy) [MHz] Kumpulainen, Hanna; Jaervinen, Tomi; Mannila, Anne; Leppaenen, Jukka; Nevalainen, Tapio; Maentylae, Antti; Vepsaelaeinen, Jouko; Rautio, Jarkko; European Journal of Pharmaceutical Sciences; vol. 34; nb. 2-3; (2008); p. 110 - 117, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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4 of 5
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
13C
Solvents (NMR Spectroscopy)
D2O
Temperature (NMR Spectroscopy) [°C]
25
Frequency (NMR Spectro- 125.76 scopy) [MHz] Kumpulainen, Hanna; Jaervinen, Tomi; Mannila, Anne; Leppaenen, Jukka; Nevalainen, Tapio; Maentylae, Antti; Vepsaelaeinen, Jouko; Rautio, Jarkko; European Journal of Pharmaceutical Sciences; vol. 34; nb. 2-3; (2008); p. 110 - 117, View in Reaxys 5 of 5
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
31P
Solvents (NMR Spectroscopy)
D2O
Temperature (NMR Spectroscopy) [°C]
25
Frequency (NMR Spectro- 202.46 scopy) [MHz] Kumpulainen, Hanna; Jaervinen, Tomi; Mannila, Anne; Leppaenen, Jukka; Nevalainen, Tapio; Maentylae, Antti; Vepsaelaeinen, Jouko; Rautio, Jarkko; European Journal of Pharmaceutical Sciences; vol. 34; nb. 2-3; (2008); p. 110 - 117, View in Reaxys IR Spectroscopy (1) 1 of 1
Description (IR Spectroscopy)
Bands; Spectrum
Solvent (IR Spectroscopy)
potassium bromide
Location
Page/Page column 4; 14
Patent; Yichang humanwell pharmaceutical Co., Ltd; Li, Lie; Li, Jie; Fu, Yigang; Wang, Min; Xu, Huabin; Ye, Xia; (15 pag.); CN103172658; (2016); (B) Chinese, View in Reaxys Mass Spectrometry (1) Description (Mass Location Spectrometry) high resolution mass spectrometry (HRMS); spectrum Use (4) Use Pattern
References
supporting informa- Yang, Jun; Yin, Wang; Liu, Jin; Wang, Yu; Zhou, Cheng; Kang, Yi; Zhang, Wen-Sheng; Bition oorganic and Medicinal Chemistry Letters; vol. 23; nb. 6; (2013); p. 1813 - 1816, View in Reaxys
Location
References
Pharmaceuticals
Page/Page column title page; 2
Patent; Shanxi Synthetic Pharmaceutical Co., Ltd.; Jiangsu Tiandi Renhe Pharmaceutical Co., Ltd.; Zhang Qiyuan; (10 pag.); CN106674270; (2017); (A) Chinese, View in Reaxys
monitored anesthesia care (MAC) for adult patients
Page/Page column title page; 2
Patent; Shanxi Synthetic Pharmaceutical Co., Ltd.; Jiangsu Tiandi Renhe Pharmaceutical Co., Ltd.; Zhang Qiyuan; (10 pag.); CN106674270; (2017); (A) Chinese, View in Reaxys
Anesthesia
Patent; WINCH, Peter, D.; WO2007/59019; (2007); (A2) English, View in Reaxys
Sedative
Patent; WINCH, Peter, D.; WO2007/59019; (2007); (A2) English, View in Reaxys
Medchem (112) 1 of 112
Substance Effect
Sedative
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
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Bioassay Details
Bioassay : EXAMPLES; [0034] Patients undergoing elective colonoscopy were intravenously administered a 35 mg/mL sterile aqueous solution of 0-phosphonooxymethyl propofol disodium salt for sedation. The patients refrained from ingesting caffeinated drinks and foods or alcohol for at least 12 hours prior to the
Biological Species/NCBI ID
human
Substance RN
12826505View in Reaxys
Substance Name
5, GPI 15715
Substance Route of Adm.
intravenous administration
Qualitative Results
administration of fentanyl citrate (0.5 - 1.5 μg/kg) followed by title compound (7.5 - 12.5 mg/kg) caused concentration-dependent sedative effect; diagram given
Measurement Parameter
qualitative
Patent; MGI GP, INC.; WO2007/8869; (2007); (A1) English, View in Reaxys 2 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |pharmacokinetics Bioassay : [0080] Venous blood plasma samples taken from the patients of Examples IA and B at several points during and after the procedure were analyzed for concentrations of propofol prodrug and propofol derived from the propofol prodrug, and the obtained values (see Figure 1) were added to a data pool for the
Biological Species/NCBI ID
human
Substance RN
12826505View in Reaxys
Substance Name
5, GPI 15715
Substance Route of Adm.
intravenous administration
Qualitative Results
central volume and clearance of the title compound increased by 1.8% and 1.4%, respectively, per kg of lean body weight over 55 kg; gender and weight were strongly correlated, but there was no independent gender effect; figure
Measurement Parameter
qualitative
Patent; MGI GP, INC.; WO2007/8869; (2007); (A1) English, View in Reaxys 3 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : loss of consciousness; induction of EXAMPLE 1 [50] This example compares the dosedependent pharmacological effects of a propofol prodrug of Formula I, 0-phosphonooxymethyl propofol disodium salt, on rats when administered in a single oral dose to the pharmacological effects observed after an equipotent intravenous infusion. Young adult
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
2363920
Substance Route of Adm.
intragastric administration
Qualitative Results
title compound at 300-400 mg/kg caused loss of consciousness (figures)
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 4 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : loss of consciousness; induction of EXAMPLE 1 [50] This example compares the dosedependent pharmacological effects of a propofol prodrug of Formula I, 0-phosphonooxymethyl propofol disodium salt, on rats when administered in a single oral dose to the pharmacological effects observed after an equipotent intravenous infusion. Young adult
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5/38
2018-06-10 19:48:31
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
2363920
Substance Route of Adm.
intraduodenal administration
Qualitative Results
title compound at high doses caused loss of consciousness (figures)
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 5 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : pharmacokinetics EXAMPLE 1 [50] This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, 0-phosphonooxymethyl propofol disodium salt, on rats when administered in a single oral dose to the pharmacological effects observed after an equipotent intravenous infusion. Young adult
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
2363920
Substance Route of Adm.
intraduodenal administration
Qualitative Results
after administartion of 1-100 mg/kg of title compound Cmax for propofol was 0.00826-5.84 µg/ml and AUCt was 0.389-223 µg x min/ml
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 6 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : pharmacokinetics EXAMPLE 1 [50] This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, 0-phosphonooxymethyl propofol disodium salt, on rats when administered in a single oral dose to the pharmacological effects observed after an equipotent intravenous infusion. Young adult
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
2363920
Substance Route of Adm.
intraduodenal administration
Qualitative Results
after administartion of 20-100 mg/kg of title compound Cmax for propofol was 0.0426-0.526 µg/ml and AUCt was 3.70-73.8 µg x min/ml
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 7 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : pharmacokinetics EXAMPLE 1 [50] This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, 0-phosphonooxymethyl propofol disodium salt, on rats when administered in a single oral dose to the pharmacological effects observed after an equipotent intravenous infusion. Young adult
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
2363920
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
6/38
2018-06-10 19:48:31
Substance Route of Adm.
intravenous administration
Qualitative Results
after administartion of 5 or 50 mg/kg of title compound Cmax for propofol was 0.286 or 2.48 µg/ml and AUCt was 6.94 or 81.8 µg x min/ml
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 8 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : sedation; induction of EXAMPLE 1 [50] This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, 0-phosphonooxymethyl propofol disodium salt, on rats when administered in a single oral dose to the pharmacological effects observed after an equipotent intravenous infusion. Young adult
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
2363920
Substance Route of Adm.
intraduodenal administration
Qualitative Results
title compound at 100-400 mg/kg caused dose-dependent sedated behavior (figures)
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 9 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : sedation; induction of EXAMPLE 1 [50] This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, 0-phosphonooxymethyl propofol disodium salt, on rats when administered in a single oral dose to the pharmacological effects observed after an equipotent intravenous infusion. Young adult
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
2363920
Substance Route of Adm.
intraduodenal administration
Qualitative Results
title compound at 20-400 mg/kg caused dose-dependent sedative effect within five minutes of administration (figures)
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 10 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : sedation; induction of EXAMPLE 1 [50] This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, 0-phosphonooxymethyl propofol disodium salt, on rats when administered in a single oral dose to the pharmacological effects observed after an equipotent intravenous infusion. Young adult
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
2363920
Substance Route of Adm.
intraduodenal administration
Qualitative Results
title compound at 5-40 mg/kg caused dose-dependent sedated/anesthetized state (figure)
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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11 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : pharmacokinetics EXAMPLE 2 [59] In a crossover study aimed at determining the plasma bioavaliablity of propofol after oral or intraduodenal administration of 0-phosphonooxymethyl propofol disodium salt, seven male human volunteers received 400 mg of the test compound dissolved in aqueous solution at a concentration
Biological Species/NCBI ID
human
Substance RN
12826505View in Reaxys
Substance Name
2363920
Substance Route of Adm.
intraduodenal administration
Qualitative Results
0.08-9.0 hours after administartion of 400 mg/kg of title compound appreciable plasma concentrations of propofol were observed
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 12 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : pharmacokinetics EXAMPLE 2 [59] In a crossover study aimed at determining the plasma bioavaliablity of propofol after oral or intraduodenal administration of 0-phosphonooxymethyl propofol disodium salt, seven male human volunteers received 400 mg of the test compound dissolved in aqueous solution at a concentration
Biological Species/NCBI ID
human
Substance RN
12826505View in Reaxys
Substance Name
2363920
Substance Route of Adm.
oral administration
Qualitative Results
0.08-9.0 hours after administartion of 400 mg/kg of title compound appreciable plasma concentrations of propofol were observed
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 13 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : loss of consciousness; induction ofBioassay : EXAMPLE 1 [50] This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, 0-phosphonooxymethyl propofol disodium salt, on rats when administered in a single oral dose to the pharmacological effects observed after an equipotent intravenous infusion. Young adult
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
5, GPI 15715
Substance Route of Adm.
intragastric administration
Qualitative Results
title compound at 300-400 mg/kg caused loss of consciousness (figures)
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 14 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : loss of consciousness; induction ofBioassay : EXAMPLE 1 [50] This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, 0-phosphonooxy-
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
8/38
2018-06-10 19:48:31
methyl propofol disodium salt, on rats when administered in a single oral dose to the pharmacological effects observed after an equipotent intravenous infusion. Young adult Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
5, GPI 15715
Substance Route of Adm.
intraduodenal administration
Qualitative Results
title compound at high doses caused loss of consciousness (figures)
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 15 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : sedation; induction ofBioassay : EXAMPLE 1 [50] This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, 0-phosphonooxymethyl propofol disodium salt, on rats when administered in a single oral dose to the pharmacological effects observed after an equipotent intravenous infusion. Young adult
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
5, GPI 15715
Substance Route of Adm.
intraduodenal administration
Qualitative Results
title compound at 100-400 mg/kg caused dose-dependent sedated behavior (figures)
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 16 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : sedation; induction ofBioassay : EXAMPLE 1 [50] This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, 0-phosphonooxymethyl propofol disodium salt, on rats when administered in a single oral dose to the pharmacological effects observed after an equipotent intravenous infusion. Young adult
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
5, GPI 15715
Substance Route of Adm.
intraduodenal administration
Qualitative Results
title compound at 20-400 mg/kg caused dose-dependent sedative effect within five minutes of administration (figures)
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 17 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : sedation; induction ofBioassay : EXAMPLE 1 [50] This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, 0-phosphonooxymethyl propofol disodium salt, on rats when administered in a single oral dose to the pharmacological effects observed after an equipotent intravenous infusion. Young adult
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
5, GPI 15715
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
9/38
2018-06-10 19:48:31
Substance Route of Adm.
intravenous administration
Qualitative Results
title compound at 5-40 mg/kg caused dose-dependent sedated/anesthetized state (figure)
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 18 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |pharmacokinetics Bioassay : EXAMPLE 1 [50] This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, 0-phosphonooxymethyl propofol disodium salt, on rats when administered in a single oral dose to the pharmacological effects observed after an equipotent intravenous infusion. Young adult
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
5, GPI 15715
Substance Route of Adm.
intraduodenal administration
Qualitative Results
after administartion of 1-100 mg/kg of title compound Cmax for propofol was 0.00826-5.84 µg/ml and AUCt was 0.389-223 µg x min/ml
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 19 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |pharmacokinetics Bioassay : EXAMPLE 1 [50] This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, 0-phosphonooxymethyl propofol disodium salt, on rats when administered in a single oral dose to the pharmacological effects observed after an equipotent intravenous infusion. Young adult
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
5, GPI 15715
Substance Route of Adm.
intraduodenal administration
Qualitative Results
after administartion of 20-100 mg/kg of title compound Cmax for propofol was 0.0426-0.526 µg/ml and AUCt was 3.70-73.8 µg x min/ml
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 20 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |pharmacokinetics Bioassay : EXAMPLE 1 [50] This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, 0-phosphonooxymethyl propofol disodium salt, on rats when administered in a single oral dose to the pharmacological effects observed after an equipotent intravenous infusion. Young adult
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
5, GPI 15715
Substance Route of Adm.
intraduodenal administration
Qualitative Results
after administartion of 5 or 50 mg/kg of title compound Cmax for propofol was 0.286 or 2.48 µg/ml and AUCt was 6.94 or 81.8 µg x min/ml
Measurement Parameter
qualitative
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
10/38
2018-06-10 19:48:31
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 21 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |pharmacokinetics Bioassay : EXAMPLE 2 [59] In a crossover study aimed at determining the plasma bioavaliablity of propofol after oral or intraduodenal administration of 0-phosphonooxymethyl propofol disodium salt, seven male human volunteers received 400 mg of the test compound dissolved in aqueous solution at a concentration
Biological Species/NCBI ID
human
Substance RN
12826505View in Reaxys
Substance Name
5, GPI 15715
Substance Route of Adm.
intraduodenal administration
Qualitative Results
0.08-9.0 hours after administartion of 400 mg/kg of title compound appreciable plasma concentrations of propofol were observed
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 22 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |pharmacokinetics Bioassay : EXAMPLE 2 [59] In a crossover study aimed at determining the plasma bioavaliablity of propofol after oral or intraduodenal administration of 0-phosphonooxymethyl propofol disodium salt, seven male human volunteers received 400 mg of the test compound dissolved in aqueous solution at a concentration
Biological Species/NCBI ID
human
Substance RN
12826505View in Reaxys
Substance Name
5, GPI 15715
Substance Route of Adm.
oral administration
Qualitative Results
0.08-9.0 hours after administartion of 400 mg/kg of title compound appreciable plasma concentrations of propofol were observed
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS INC.; WO2005/58250; (2005); (A2) English, View in Reaxys 23 of 112
Substance Effect
Sedative
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Bioassay : This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, O-phosphonooxymethyl propofol disodium salt, on rats when administered in single subcutaneous injections to the pharmacological effects observed after intravenous infusion. Young adult male Sprague-Dawley
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
5, GPI 15715
Substance Route of Adm.
subcutaneous administration
Qualitative Results
Title compound innduced a rapid (within 5-10 minutes of dosing) dose-dependent onset of sedated behavior, quickly followed by loss of consciousness in the 100, 200, and 300 mg/kg dose groups; loss of consciousness lasted for more than two hours in animals
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS, INC.; WO2006/33911; (2006); (A2) English, View in Reaxys 24 of 112
Bioassay Category
In Vivo (Animal models)
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
11/38
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Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |pharmacokinetics Bioassay : This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, O-phosphonooxymethyl propofol disodium salt, on rats when administered in single subcutaneous injections to the pharmacological effects observed after intravenous infusion. Young adult male Sprague-Dawley
Biological Species/NCBI ID
dog
Substance RN
12826505View in Reaxys
Substance Name
5, GPI 15715
Substance Route of Adm.
subcutaneous administration
Qualitative Results
after administration of 16 mg/kg propofol parameters: AUC(last) = 1322 h*ng/ml, Cmax = 0.39 &mg;/ml, Tmax = 1.0 h
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS, INC.; WO2006/33911; (2006); (A2) English, View in Reaxys 25 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |pharmacokinetics Bioassay : This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, O-phosphonooxymethyl propofol disodium salt, on rats when administered in single subcutaneous injections to the pharmacological effects observed after intravenous infusion. Young adult male Sprague-Dawley
Biological Species/NCBI ID
dog
Substance RN
12826505View in Reaxys
Substance Name
5, GPI 15715
Substance Route of Adm.
intravenous administration
Qualitative Results
after administration of 16 mg/kg propofol parameters: AUC(last) = 1728 h*ng/ml, Cmax = 3.84 &mg;/ml, Tmax = 0.003 h
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS, INC.; WO2006/33911; (2006); (A2) English, View in Reaxys 26 of 112
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |pharmacokinetics Bioassay : This example compares the dose-dependent pharmacological effects of a propofol prodrug of Formula I, O-phosphonooxymethyl propofol disodium salt, on rats when administered in single subcutaneous injections to the pharmacological effects observed after intravenous infusion. Young adult male Sprague-Dawley
Biological Species/NCBI ID
dog
Substance RN
12826505View in Reaxys
Substance Name
5, GPI 15715
Substance Route of Adm.
rectal administration
Qualitative Results
after administration of 16 mg/kg propofol parameters: AUC(last) = 240.9 h*ng/ml, Cmax = 0.16 &mg;/ml, Tmax = 0.50 h
Measurement Parameter
qualitative
Patent; GUILFORD PHARMACEUTICALS, INC.; WO2006/33911; (2006); (A2) English, View in Reaxys 27 of 112
Bioassay Category
Metabolism/Transport
Bioassay Details
Volume of distribution of compound in human was determined
Biological Species/NCBI ID
human
Substance RN
12826505View in Reaxys
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12/38
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Measurement Parameter
Vd (volume of distribution)
Unit
L/kg
Measurement Object
Volume of distribution
Qualitative value
=
Quantitative value
0.11
Gooyit, Major; Lee, Mijoon; Schroeder, Valerie A.; Ikejiri, Masahiro; Suckow, Mark A.; Mobashery, Shahriar; Chang, Mayland; Journal of Medicinal Chemistry; vol. 54; nb. 19; (2011); p. 6676 - 6690, View in Reaxys 28 of 112
Bioassay Category
Metabolism/Transport
Bioassay Details
Volume of distribution of compound in rat was determined
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Measurement Parameter
Vd (volume of distribution)
Unit
L/kg
Measurement Object
Volume of distribution
Qualitative value
=
Quantitative value
0.25
Gooyit, Major; Lee, Mijoon; Schroeder, Valerie A.; Ikejiri, Masahiro; Suckow, Mark A.; Mobashery, Shahriar; Chang, Mayland; Journal of Medicinal Chemistry; vol. 54; nb. 19; (2011); p. 6676 - 6690, View in Reaxys 29 of 112
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
The onset time from the injection of the drug to the disappearance of the righting reflex in rat was measured
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Unit
second
Measurement Object
righting reflex
Qualitative value
=
Quantitative value
2.17
Deviation
0.32
Jun Yang; Wang Yin; Jin Liu; Yu Wang; Cheng Zhou; Yi Kang; Wen-Sheng Zhang; Bioorganic & medicinal chemistry letters; vol. 23; nb. 6; (2013); p. 1813 - 1816, View in Reaxys 30 of 112
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective dose of the compound required to induce systemic convulsions in rat after administration through the tail vein
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Measurement Parameter
ED50
Unit
mg/kg
Measurement Object
Number of convulsions
Qualitative value
=
Quantitative value
34.78
Deviation
4.14
Jun Yang; Wang Yin; Jin Liu; Yu Wang; Cheng Zhou; Yi Kang; Wen-Sheng Zhang; Bioorganic & medicinal chemistry letters; vol. 23; nb. 6; (2013); p. 1813 - 1816, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
13/38
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31 of 112
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Lethal dose of the compound against systemic convulsions in rat after compound administration through the tail vein
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Measurement Parameter
LD50
Unit
mg/kg
Measurement Object
PROTECT TYPICAL CONVULSIONS
Qualitative value
=
Quantitative value
163.11
Deviation
19.71
Jun Yang; Wang Yin; Jin Liu; Yu Wang; Cheng Zhou; Yi Kang; Wen-Sheng Zhang; Bioorganic & medicinal chemistry letters; vol. 23; nb. 6; (2013); p. 1813 - 1816, View in Reaxys 32 of 112
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
The duration time from the disappearance of the righting reflex to the recovery of the righting reflex in rat
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Measurement Parameter
Activity
Unit
minute
Measurement Object
Dt
Qualitative value
=
Quantitative value
31.04
Deviation
7.9
Jun Yang; Wang Yin; Jin Liu; Yu Wang; Cheng Zhou; Yi Kang; Wen-Sheng Zhang; Bioorganic & medicinal chemistry letters; vol. 23; nb. 6; (2013); p. 1813 - 1816, View in Reaxys 33 of 112
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Therapeutic index is ratio of Lethal dose to that of Effective dose required to induce systemic convulsions after compound administration through the tail vein
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Measurement Parameter
qualitative
Measurement Object
Number of convulsions
Qualitative value
Not Published
Jun Yang; Wang Yin; Jin Liu; Yu Wang; Cheng Zhou; Yi Kang; Wen-Sheng Zhang; Bioorganic & medicinal chemistry letters; vol. 23; nb. 6; (2013); p. 1813 - 1816, View in Reaxys 34 of 112
Bioassay Category
Metabolism/Transport
Bioassay Details
Terminal half-life of the compound in human volunteers
Biological Species/NCBI ID
human
Substance RN
12826505View in Reaxys
Measurement Parameter
t1/2
Unit
minute
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
14/38
2018-06-10 19:48:31
Qualitative value
=
Quantitative value
46
Fechner, Joerg; Ihmsen, Harald; Hatterscheid, Dirk; Schiessl, Christine; Vornov, James J.; Burak, Eric; Schwilden, Helmut; Schuettler, Juergen; Anesthesiology; vol. 99; nb. 2; (2003); p. 303 - 313, View in Reaxys 35 of 112
Bioassay Category
Metabolism/Transport
Bioassay Details
Central volume of distribution of the compound in human volunteers
Biological Species/NCBI ID
human
Substance RN
12826505View in Reaxys
Measurement Parameter
Vd (volume of distribution)
Unit
L/kg
Qualitative value
=
Quantitative value
0.071
Fechner, Joerg; Ihmsen, Harald; Hatterscheid, Dirk; Schiessl, Christine; Vornov, James J.; Burak, Eric; Schwilden, Helmut; Schuettler, Juergen; Anesthesiology; vol. 99; nb. 2; (2003); p. 303 - 313, View in Reaxys 36 of 112
Bioassay Category
Metabolism/Transport
Bioassay Details
Clearance of the compound in human volunteers
Biological Species/NCBI ID
human
Substance RN
12826505View in Reaxys
Unit
mL/min/kg
Qualitative value
=
Quantitative value
7
Fechner, Joerg; Ihmsen, Harald; Hatterscheid, Dirk; Schiessl, Christine; Vornov, James J.; Burak, Eric; Schwilden, Helmut; Schuettler, Juergen; Anesthesiology; vol. 99; nb. 2; (2003); p. 303 - 313, View in Reaxys 37 of 112
Substance Effect
General Anaesthesic
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
beagle
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
75 mg/kg
Measurement Parameter
time
Unit
minute
Measurement Object
on-set of loss of righting reflex
Quantitative value
2.1
Qin, Linlin; Ren, Lei; Wan, Songlin; Liu, Guoliang; Luo, Xinfeng; Liu, Zhenhong; Li, Fangqiong; Yu, Yan; Liu, Jianyu; Wei, Yonggang; Journal of Medicinal Chemistry; vol. 60; nb. 9; (2017); p. 3606 - 3617, View in Reaxys 38 of 112
Substance Effect
General Anaesthesic
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
minipig
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
22.5 mg/kg
Measurement Parameter
time
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
15/38
2018-06-10 19:48:31
Unit
minute
Measurement Object
on-set of loss of righting reflex
Quantitative value
1.6
Qin, Linlin; Ren, Lei; Wan, Songlin; Liu, Guoliang; Luo, Xinfeng; Liu, Zhenhong; Li, Fangqiong; Yu, Yan; Liu, Jianyu; Wei, Yonggang; Journal of Medicinal Chemistry; vol. 60; nb. 9; (2017); p. 3606 - 3617, View in Reaxys 39 of 112
Substance Effect
General Anaesthesic
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
beagle
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
75 mg/kg
Measurement Parameter
time
Unit
minute
Measurement Object
duration of loss righting reflex
Quantitative value
80.4
Qin, Linlin; Ren, Lei; Wan, Songlin; Liu, Guoliang; Luo, Xinfeng; Liu, Zhenhong; Li, Fangqiong; Yu, Yan; Liu, Jianyu; Wei, Yonggang; Journal of Medicinal Chemistry; vol. 60; nb. 9; (2017); p. 3606 - 3617, View in Reaxys 40 of 112
Substance Effect
General Anaesthesic
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
minipig
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
22.5 mg/kg
Measurement Parameter
time
Unit
minute
Measurement Object
duration of loss righting reflex
Quantitative value
72.6
Qin, Linlin; Ren, Lei; Wan, Songlin; Liu, Guoliang; Luo, Xinfeng; Liu, Zhenhong; Li, Fangqiong; Yu, Yan; Liu, Jianyu; Wei, Yonggang; Journal of Medicinal Chemistry; vol. 60; nb. 9; (2017); p. 3606 - 3617, View in Reaxys 41 of 112
Substance Effect
General Anaesthesic
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
beagle
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
75 mg/kg
Measurement Parameter
time
Unit
minute
Measurement Object
Total recovery from loss of the righting reflex
Quantitative value
7.3
Qin, Linlin; Ren, Lei; Wan, Songlin; Liu, Guoliang; Luo, Xinfeng; Liu, Zhenhong; Li, Fangqiong; Yu, Yan; Liu, Jianyu; Wei, Yonggang; Journal of Medicinal Chemistry; vol. 60; nb. 9; (2017); p. 3606 - 3617, View in Reaxys 42 of 112
Substance Effect
General Anaesthesic
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
16/38
2018-06-10 19:48:31
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
minipig
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
22.5 mg/kg
Measurement Parameter
time
Unit
minute
Measurement Object
Total recovery from loss of the righting reflex
Quantitative value
6
Qin, Linlin; Ren, Lei; Wan, Songlin; Liu, Guoliang; Luo, Xinfeng; Liu, Zhenhong; Li, Fangqiong; Yu, Yan; Liu, Jianyu; Wei, Yonggang; Journal of Medicinal Chemistry; vol. 60; nb. 9; (2017); p. 3606 - 3617, View in Reaxys 43 of 112
Substance Effect
General Anaesthesic
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
mouse
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Measurement Parameter
ED50
Unit
mg/kg
Measurement Object
50% animals to loss righting reflex
Quantitative value
94.97
Qin, Linlin; Ren, Lei; Wan, Songlin; Liu, Guoliang; Luo, Xinfeng; Liu, Zhenhong; Li, Fangqiong; Yu, Yan; Liu, Jianyu; Wei, Yonggang; Journal of Medicinal Chemistry; vol. 60; nb. 9; (2017); p. 3606 - 3617, View in Reaxys 44 of 112
Substance Effect
Toxic
Bioassay Category
Toxicity/Safety Pharmacology
Biological Species/NCBI ID
mouse
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
220
Qin, Linlin; Ren, Lei; Wan, Songlin; Liu, Guoliang; Luo, Xinfeng; Liu, Zhenhong; Li, Fangqiong; Yu, Yan; Liu, Jianyu; Wei, Yonggang; Journal of Medicinal Chemistry; vol. 60; nb. 9; (2017); p. 3606 - 3617, View in Reaxys 45 of 112
Substance Effect
General Anaesthesic
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Measurement Parameter
ED50
Unit
mg/kg
Measurement Object
50% animals to loss righting reflex
Quantitative value
40.98
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
17/38
2018-06-10 19:48:31
Qin, Linlin; Ren, Lei; Wan, Songlin; Liu, Guoliang; Luo, Xinfeng; Liu, Zhenhong; Li, Fangqiong; Yu, Yan; Liu, Jianyu; Wei, Yonggang; Journal of Medicinal Chemistry; vol. 60; nb. 9; (2017); p. 3606 - 3617, View in Reaxys 46 of 112
Substance Effect
Toxic
Bioassay Category
Toxicity/Safety Pharmacology
Biological Species/NCBI ID
rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
189
Qin, Linlin; Ren, Lei; Wan, Songlin; Liu, Guoliang; Luo, Xinfeng; Liu, Zhenhong; Li, Fangqiong; Yu, Yan; Liu, Jianyu; Wei, Yonggang; Journal of Medicinal Chemistry; vol. 60; nb. 9; (2017); p. 3606 - 3617, View in Reaxys 47 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
t1/2 el
Unit
h
Quantitative value
2.32
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 48 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
30 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
t1/2 el
Unit
h
Quantitative value
2.85
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 49 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
oral administration
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
18/38
2018-06-10 19:48:31
Measurement Parameter
t1/2 el
Unit
h
Quantitative value
4.13
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 50 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
20 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
t1/2 el
Unit
h
Quantitative value
4.66
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 51 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
F (drug bioavailability)
Unit
%
Quantitative value
141
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 52 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
20 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
F (drug bioavailability)
Unit
%
Quantitative value
22.7
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
19/38
2018-06-10 19:48:31
53 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
30 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
F (drug bioavailability)
Unit
%
Quantitative value
47.3
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 54 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
F (drug bioavailability)
Unit
%
Quantitative value
70.5
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 55 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
5 mg/kg
Substance Route of Adm.
intravenous drug administration
Measurement Parameter
AUC (0-inf)
Unit
μg*h/ml
Quantitative value
0.14
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 56 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
20 mg/kg
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
20/38
2018-06-10 19:48:31
Substance Route of Adm.
oral administration
Measurement Parameter
AUC (0-inf)
Unit
μg*h/ml
Quantitative value
0.13
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 57 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
30 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
AUC (0-inf)
Unit
μg*h/ml
Quantitative value
0.398
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 58 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
AUC (0-inf)
Unit
μg*h/ml
Quantitative value
3.95
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 59 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
AUC (0-inf)
Unit
μg*h/ml
Quantitative value
1.96
Metabolite RN
1866484
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
21/38
2018-06-10 19:48:31
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 60 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
Cmax
Unit
μg/ml
Quantitative value
3.74
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 61 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
Cmax
Unit
μg/ml
Quantitative value
9.23
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 62 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
5 mg/kg
Substance Route of Adm.
intravenous drug administration
Measurement Parameter
Cmax
Unit
μg/ml
Quantitative value
16.3
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 63 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
30 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
Cmax
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
22/38
2018-06-10 19:48:31
Unit
μg/ml
Quantitative value
0.17
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 64 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
20 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
Cmax
Unit
μg/ml
Quantitative value
0.23
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 65 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
30 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
AUC (0-6 h)
Unit
μg*h/ml
Quantitative value
0.044
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 66 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
20 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
AUC (0-6 h)
Unit
μg*h/ml
Quantitative value
0.05
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 67 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
5 mg/kg
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
23/38
2018-06-10 19:48:31
Substance Route of Adm.
intravenous drug administration
Measurement Parameter
AUC (0-6 h)
Unit
μg*h/ml
Quantitative value
3.15
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 68 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
AUC (0-6 h)
Unit
μg*h/ml
Quantitative value
0.644
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 69 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
AUC (0-6 h)
Unit
μg*h/ml
Quantitative value
2.16
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 70 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
30 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
t1/2 el
Unit
h
Quantitative value
0.21
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 71 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
24/38
2018-06-10 19:48:31
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
t1/2 el
Unit
h
Quantitative value
0.23
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 72 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
t1/2 el
Unit
h
Quantitative value
0.49
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 73 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
20 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
t1/2 el
Unit
h
Quantitative value
0.19
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 74 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
5 mg/kg
Substance Route of Adm.
intravenous drug administration
Measurement Parameter
t1/2 el
Unit
h
Quantitative value
0.49
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 75 of 112
Bioassay Category
Pharmacokinetic
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
25/38
2018-06-10 19:48:31
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
5 mg/kg
Substance Route of Adm.
intravenous drug administration
Measurement Parameter
Vd (volume of distribution)
Unit
l/kg
Quantitative value
1.02
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 76 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
5 mg/kg
Substance Route of Adm.
intravenous drug administration
Measurement Parameter
CL (drug clearance)
Unit
l/h/kg
Quantitative value
1.38
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 77 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
30 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
F (drug bioavailability)
Unit
%
Quantitative value
0.264
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 78 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
20 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
F (drug bioavailability)
Unit
%
Quantitative value
0.448
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
26/38
2018-06-10 19:48:31
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 79 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
F (drug bioavailability)
Unit
%
Quantitative value
1.03
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 80 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
F (drug bioavailability)
Unit
%
Quantitative value
3.46
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 81 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
30 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
AUC (0-inf)
Unit
μg*h/ml
Quantitative value
0.05
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 82 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
20 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
AUC (0-inf)
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
27/38
2018-06-10 19:48:31
Unit
μg*h/ml
Quantitative value
0.06
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 83 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
5 mg/kg
Substance Route of Adm.
intravenous drug administration
Measurement Parameter
AUC (0-inf)
Unit
μg*h/ml
Quantitative value
3.15
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 84 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
AUC (0-inf)
Unit
μg*h/ml
Quantitative value
0.65
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 85 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
AUC (0-inf)
Unit
μg*h/ml
Quantitative value
2.18
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 86 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
20 mg/kg
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
28/38
2018-06-10 19:48:31
Substance Route of Adm.
oral administration
Measurement Parameter
Cmax
Unit
μg/ml
Quantitative value
0.04
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 87 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
Cmax
Unit
μg/ml
Quantitative value
0.53
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 88 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
Cmax
Unit
μg/ml
Quantitative value
5.84
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 89 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
30 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
Cmax
Unit
μg/ml
Quantitative value
1.27
Metabolite RN
1866484
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
29/38
2018-06-10 19:48:31
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 90 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
5 mg/kg
Substance Route of Adm.
intravenous drug administration
Measurement Parameter
Cmax
Unit
μg/ml
Quantitative value
0.29
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 91 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
5 mg/kg
Substance Route of Adm.
intravenous drug administration
Measurement Parameter
AUC (0-6 h)
Unit
μg*h/ml
Quantitative value
0.12
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 92 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
20 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
AUC (0-6 h)
Unit
μg*h/ml
Quantitative value
0.06
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 93 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
30/38
2018-06-10 19:48:31
Substance Dose
30 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
AUC (0-6 h)
Unit
μg*h/ml
Quantitative value
0.353
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 94 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
AUC (0-6 h)
Unit
μg*h/ml
Quantitative value
1.21
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 95 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
AUC (0-6 h)
Unit
μg*h/ml
Quantitative value
3.57
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 96 of 112
Substance Effect
Sedative
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
10 - 40 mg/kg
Substance Route of Adm.
intravenous drug administration
Measurement Parameter
% increase
Qualitative value
Active
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
31/38
2018-06-10 19:48:31
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 97 of 112
Substance Effect
Sedative
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 - 200 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
% increase
Qualitative value
Moderate
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 98 of 112
Substance Effect
Sedative
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
300 - 400 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
qualitative
Measurement Object
Loss of consciousness
Qualitative value
Active
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 99 of 112
Substance Effect
Sedative
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
100 - 400 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Measurement Parameter
qualitative
Measurement Object
Loss of consciousness
Qualitative value
Active
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 100 of 112
Substance Effect
Analgesic
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
32/38
2018-06-10 19:48:31
Substance Dose
75 - 100 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
% decrease
Measurement Object
withdrawal latency, thermal hyperalgesia at hindpaw
Qualitative value
Active
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 101 of 112
Substance Effect
Analgesic
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
50 mg/kg
Substance Route of Adm.
oral administration
Measurement Parameter
% decrease
Measurement Object
withdrawal latency, thermal hyperalgesia at hindpaw
Qualitative value
Not active
Measurement pX
1
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 102 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Healthy
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
400 mg/kg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Single
Measurement Parameter
tmax
Unit
h
Quantitative value
0.08
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 103 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Healthy
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
400 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Substance Dosing Regimen
Single
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Measurement Parameter
tmax
Unit
h
Quantitative value
0.17
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 104 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Healthy
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
400 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Substance Dosing Regimen
Single
Measurement Parameter
tmax
Unit
h
Quantitative value
0.17
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 105 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Healthy
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
400 mg/kg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Single
Measurement Parameter
tmax
Unit
h
Quantitative value
0.33
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 106 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Healthy
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
400 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Substance Dosing Regimen
Single
Measurement Parameter
t1/2 el
Unit
h
Quantitative value
0.28
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 107 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Healthy
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
400 mg/kg
Substance Route of Adm.
intravenous drug administration
Substance Dosing Regimen
Single
Measurement Parameter
t1/2 el
Unit
h
Quantitative value
0.28
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 108 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Healthy
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
400 mg/kg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Single
Measurement Parameter
t1/2 el
Unit
h
Quantitative value
0.32
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 109 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Healthy
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
400 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Substance Dosing Regimen
Single
Measurement Parameter
F (drug bioavailability)
Unit
%
Quantitative value
0.1
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 110 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Healthy
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
400 mg/kg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Single
Measurement Parameter
F (drug bioavailability)
Unit
%
Quantitative value
1
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 111 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Healthy
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
400 mg/kg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Single
Measurement Parameter
F (drug bioavailability)
Unit
%
Quantitative value
30
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys 112 of 112
Bioassay Category
Pharmacokinetic
Biological Species/NCBI ID
human
Population State
Healthy
Substance RN
12826505View in Reaxys
Substance Name
fospropofol disodium
Substance Dose
400 mg/kg
Substance Route of Adm.
intraduodenal drug administration
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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2018-06-10 19:48:31
Substance Dosing Regimen
Single
Measurement Parameter
F (drug bioavailability)
Unit
%
Quantitative value
37
Metabolite RN
1866484
Patent; THE JOHNS HOPKINS UNIVERSITY; SLUSHER, Barbara; RAIS, Rana; VORNOV, James; (78 pag.); WO2017/205632; (2017); (A1) English, View in Reaxys
Reaxys ID 25844484 View in Reaxys
2/3 O–
Linear Structure Formula: C13H19O5P(2-)*Na(1+) Molecular Formula: C13H19O5P*Na Molecular Weight: 309.254 InChI Key: FVLUXVLPXDIGAK-UHFFFAOYSA-L Note:
O– P O O Na +
O
Druglikeness (1) 1 of 1
LogP
2.524
H Bond Donors
0
H Bond Acceptors
4
Rotatable Bonds
6
TPSA
91.46
Lipinski Number
4
Veber Number
2
Bioassay Category
Pharmacokinetic
Bioassay Details
In vivo time taken to reach maximum plasma concentration of compound in rat after intavenous administration of dose at 40 mg/kg
Biological Species/NCBI ID
rat
Substance RN
25844484View in Reaxys
Substance Route of Adm.
intravenous administration
Measurement Parameter
tmax
Unit
minute
Measurement Object
Tmax
Qualitative value
=
Quantitative value
3.7
Deviation
0.2
Medchem (2) 1 of 2
Kumpulainen, Hanna; Jaervinen, Tomi; Mannila, Anne; Leppaenen, Jukka; Nevalainen, Tapio; Maentylae, Antti; Vepsaelaeinen, Jouko; Rautio, Jarkko; European Journal of Pharmaceutical Sciences; vol. 34; nb. 2-3; (2008); p. 110 - 117, View in Reaxys 2 of 2
Bioassay Category
Pharmacokinetic
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2018-06-10 19:48:31
Bioassay Details
In vivo maximum plasma concentration of compound in rat after intavenous administration of dose at 40 mg/kg
Biological Species/NCBI ID
rat
Substance RN
25844484View in Reaxys
Substance Route of Adm.
intravenous administration
Measurement Parameter
Cmax
Unit
µg/mL
Measurement Object
Maximum plasma concentration of compound in rat
Qualitative value
=
Quantitative value
7.1
Deviation
1.6
Kumpulainen, Hanna; Jaervinen, Tomi; Mannila, Anne; Leppaenen, Jukka; Nevalainen, Tapio; Maentylae, Antti; Vepsaelaeinen, Jouko; Rautio, Jarkko; European Journal of Pharmaceutical Sciences; vol. 34; nb. 2-3; (2008); p. 110 - 117, View in Reaxys
Reaxys ID 29966792 View in Reaxys 2
Na +
-1
3/3
H 2O
O–
O–
Linear Structure Formula: C13H19O5P(2-)*2Na(1+)*xH2O Molecular Formula: C13H19O5P*(x)H2O*2Na InChI Key: PSFIXYJJRKTRHC-UHFFFAOYSA-L Note:
P O
O
O
Substance Label (1) Label References 2
Patent; Yichang humanwell pharmaceutical Co., Ltd; Li, Lie; Li, Jie; Fu, Yigang; Wang, Min; Xu, Huabin; Ye, Xia; (15 pag.); CN103172658; (2016); (B) Chinese, View in Reaxys
Druglikeness (1) 1 of 1
LogP
2.057
H Bond Donors
1
H Bond Acceptors
5
Rotatable Bonds
6
TPSA
91.46
Lipinski Number
4
Veber Number
2
Crystal Phase (1) Description (Crystal Phase) Interplanar spacing Space Group (1) Location Page/Page column 2; 4; 8; 9
Location
References
Page/Page column 2; 4; 8; 9
Patent; Yichang humanwell pharmaceutical Co., Ltd; Li, Lie; Li, Jie; Fu, Yigang; Wang, Min; Xu, Huabin; Ye, Xia; (15 pag.); CN103172658; (2016); (B) Chinese, View in Reaxys
Comment (Space Group)
References
Method = Powder X-ray diffraction
Patent; Yichang humanwell pharmaceutical Co., Ltd; Li, Lie; Li, Jie; Fu, Yigang; Wang, Min; Xu, Huabin; Ye, Xia; (15 pag.); CN103172658; (2016); (B) Chinese, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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