化合物简介
CI-988 (PD-134,308) is a drug which acts as a cholecystokinin antagonist, selective for the CCKB subtype. In animal studies it showed anxiolytic effects and potentiated the analgesic action of both morphine and endogenous opioid peptides, as well as preventing the development of tolerance to opioids and reducing symptoms of withdrawal. Consequently, it was hoped that it might have clinical applications for the treatment of pain and anxiety in humans, but trial results were disappointing with only minimal therapeutic effects observed even at high doses. The reason for the failure of CI-988 and other CCKB antagonists in humans despite their apparent promise in pre-clinical animal studies is unclear, although poor pharmacokinetic properties of the currently available drugs are a possible explanation, and CCKB antagonists are still being researched for possible uses as adjuvants to boost the activity of other drugs.
基本信息
中文名称
3-[[(1R)-2-[[(2R)-2-(2-金刚烷基氧基羰基氨基)-3-(1H-吲哚-3-基)-2-甲基-丙酰]氨基]-1-苯基-乙基]氨基甲酰]丙酸
英文名称
4-[[(1R)-2-[[(2R)-2-(2-adamantyloxycarbonylamino)-3-(1H-indol-3-yl)-2-methylpropanoyl]amino]-1-phenylethyl]amino]-4-oxobutanoic acid
中文别名
英文别名
CI 988
CAS号
130332-27-3
分子式
C35H42N4O6
分子量
614.731
精确质量
614.31
PSA
149.62
LOGP
6.0312
编号系统
UNII
2637PDX9SI
物化性质
密度
1.32g/cm3
沸点
949.6ºC at 760mmHg
折射率
1.647
蒸汽压
0mmHg at 25°C
合成路线
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