普瑞巴林
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產品名稱: 普瑞巴林
藥理藥效:普瑞巴林是一種新型γ-氨基丁酸(GABA)受體激動劑,能阻斷電壓依賴性鈣通道,減少神經遞質的釋放,臨床主要用於治療外周神經痛以及輔助性治療局限性部分癲癇發作。
別名: C1-1008
美國化學文摘登錄號: [ 148553-50-8 ]
分子式: C8H17NO2
分子量: 159.23
物化性質: 白色結晶性粉末
熔點 (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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