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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
4-[[(1R)-2-[[(2R)-2-(2-adamantyloxycarbonylamino)-3-(1H-indol-3-yl)-2-methylpropanoyl]amino]-1-phenylethyl]amino]-4-oxobutanoic acid
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
CAS：130332-27-3
中文别名：
英文别名：CI 988;
分子式：C35H42N4O6
分子量：614.731
精确质量：614.31
Psa：149.62
Logp：6.0312
中文别名：
英文别名：CI 988;
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
沸点：949.6ºC at 760mmHg
折射率：1.647
蒸汽压：0mmHg at 25°C
安全信息
生产方法及用途
合成路线
上游原料
下游产品
图谱
Predict 1H proton NMR
