普瑞巴林

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產(chǎn)品名稱: 普瑞巴林

藥理藥效：普瑞巴林是一種新型γ-氨基丁酸(GABA)受體激動(dòng)劑,能阻斷電壓依賴性鈣通道,減少神經(jīng)遞質(zhì)的釋放,臨床主要用于治療外周神經(jīng)痛以及輔助性治療局限性部分癲癇發(fā)作。

別名: C1-1008

化學(xué)名稱: (3S)-3-氨甲基-5-甲基己酸

美國(guó)化學(xué)文摘登錄號(hào): ［ 148553-50-8 ］

分子式: C8H17NO2

分子量: 159.23

物化性質(zhì)： 白色結(jié)晶性粉末

熔點(diǎn) (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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