普瑞巴林

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产品名称: 普瑞巴林

药理药效:普瑞巴林是一种新型γ-氨基丁酸(GABA)受体激动剂,能阻断电压依赖性钙通道,减少神经递质的释放,临床主要用于治疗外周神经痛以及辅助性治疗局限性部分癫痫发作。

别名: C1-1008

化学名称: (3S)-3-氨甲基-5-甲基己酸

美国化学文摘登录号: [ 148553-50-8 ]

分子式: C8H17NO2

分子量: 159.23

物化性质: 白色结晶性粉末

熔点 (oC) 184 - 186

Monograph Number: 7813

Title: Pregabalin

CAS Registry Number: 148553-50-8

CAS Name: (3S)-3-(Aminomethyl)-5-methylhexanoic acid

Additional Names: (S)-(+)-4-amino-3-(2-methylpropyl)butanoic acid; (S)-(+)-3-isobutyl-g-aminobutyric acid

Manufacturers' Codes: CI-1008; PD-144723

Molecular Formula: C8H17NO2

Molecular Weight: 159.23.

Percent Composition: C 60.34%, H 10.76%, N 8.80%, O 20.10%

Literature References: GABA analog. Prepn of racemate: R. Andruszkiewicz, R. B. Silverman, Synthesis 1989, 953. Enantioselective synthesis: P. Yuen et al., Bioorg. Med. Chem. Lett. 4, 823 (1994). Manufacturing process: M. S. Hoekstra et al., Org. Process Res. Dev. 1, 26 (1997). HPLC determn in biological fluids: B. L. Windsor, L. L. Radulovic, J. Chromatog. B 674, 143 (1995). Anticonvulsive activity: C. P. Taylor et al., Epilepsy Res. 14, 11 (1993). Activity in models of neuropathic pain: M. J. Field et al., Pain 80, 391 (1999).

Properties: White crystalline solid, mp 186-188? [a]D23 +10.52?(c = 1.06 in water).

Melting point: mp 186-188°

Optical Rotation: [a]D23 +10.52?(c = 1.06 in water)

Therap-Cat: Anticonvulsant.

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