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爱维莫潘

爱维莫潘用途

Alvimopan(LY 246736; ADL 8-2698)二水合物是新型的口服外周阿片样受体(PAM-OR)拮抗剂,IC50为1.7 nM。

爱维莫潘名称

[ CAS 号 ]:
170098-38-1

[ 中文名 ]:
爱维莫潘二水合物

[ 英文名 ]:
Alvimopan

[中文别名 ]:

爱维莫潘杂质

[英文别名 ]:

Alvimopan dihydrate
Alvimopan
Alvimopan (USAN)
Adl 8-2698
Alvimopan anhydrous
UNII-677C126AET
Alvimopan hydrate
Entereg
Alvimopan (dihydrate)

爱维莫潘生物活性

[ 描述 ]:

Alvimopan(LY 246736; ADL 8-2698)二水合物是新型的口服外周阿片样受体(PAM-OR)拮抗剂,IC50为1.7 nM。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体

信号通路 >> 神经信号通路 >> 阿片受体

研究领域 >> 神经疾病

[参考文献]

[1]. NCBI BioAssay: 325959

[2]. Cassel JA, et al. [(3)H]Alvimopan binding to the micro opioid receptor: comparative binding kinetics of opioid antagonists. Eur J Pharmacol. 2005 Sep 27;520(1-3):29-36.

[3]. Viscusi ER, et al. Alvimopan, a peripherally acting mu-opioid receptor antagonist, compared with placebo in postoperative ileus after major abdominal surgery: results of a randomized, double-blind, controlled study. Surg Endosc. 2006 Jan;20(1):64-70.

[4]. Fukuda H, et al. The selective mu opioid receptor antagonist, alvimopan, improves delayed GI transit of postoperative ileus in rats. Brain Res. 2006 Aug 2;1102(1):63-70.

[5]. Delaney CP, et al. Phase III trial of alvimopan, a novel, peripherally acting, mu opioid antagonist, for postoperative ileus after major abdominal surgery. Dis Colon Rectum. 2005 Jun;48(6):1114-25; discussion 1125-6; author reply 1127-9.

[相关活性小分子]

爱维莫潘物理化学性质

[ 密度 ]:
1.166g/cm3

[ 沸点 ]:
684.1ºC at 760mmHg

[ 熔点 ]:
210-213ºC

[ 分子式 ]:
C₂₅H₃₆N₂O₆

[ 分子量 ]:
460.563

[ 闪点 ]:
367.5ºC

[ 精确质量 ]:
460.257324

[ PSA ]:
108.33000

[ LogP ]:
3.25160

[ 外观性状 ]:
粉末

[ 蒸汽压 ]:
1.18E-19mmHg at 25°C

[ 折射率 ]:
1.572

[ 储存条件 ]:
-20℃

爱维莫潘毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MC0595275

CHEMICAL NAME :: Glycine, N-(2-((4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl )methyl)-1-oxo-3-phen ylpropyl)-,dihydrate, (3R-(1(S*),3-alpha,4-alpha))-

CAS REGISTRY NUMBER :: 170098-38-1

LAST UPDATED :: 199606

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C25-H32-N2-O4.2H2-O

MOLECULAR WEIGHT :: 460.63

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 19,1078,1994

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >20 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 19,1078,1994

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 19,1078,1994