化合物简介
Cebranopadol (GRT-6005) is a novel opioid analgesic of the benzenoid class which is currently under development internationally by Grünenthal, a German pharmaceutical company, and its partner Depomed, a pharmaceutical company in the United States, for the treatment of a variety of different acute and chronic pain states. As of November 2014, it is in phase III clinical trials. Cebranopadol is unique in its mechanism of action as an opioid, binding to and activating all four of the opioid receptors; it acts as a full agonist of the nociceptin receptor (Ki = 0.9 nM; EC50 = 13.0; IA = 89%), μ-opioid receptor (Ki = 0.7 nM; EC50 = 1.2; IA = 104%), and δ-opioid receptor (Ki = 18 nM; EC50 = 110; IA = 105%), and as a partial agonist of the κ-opioid receptor (Ki = 2.6 nM; EC50 = 17; IA = 67%). The ED50 values of 0.5-5.6µg/kg when introduced IV & 25.1µg/kg after oral administration.
基本信息
中文名称
Cebranopadol
英文名称
6-fluoro-N,N-dimethyl-1'-phenylspiro[4,9-dihydro-3H-pyrano[3,4-b]indole-1,4'-cyclohexane]-1'-amine
中文别名
英文别名
(1r,4r)-6\'-fluoro-N,N-dimethyl-4-phenyl-4\',9\'-dihydro-3\'H-spiro[cyclohexane-1,1\'-pyrano[3,4-b]indole]-4-amine、Cebranopadol、Cebranopadol (USAN/INN)、(1r,4r)-6\'-fluoro-N,N-dimethyl-4-phenyl-4\',9\'-dihydro-3\'H-spiro[cyclohexane-1,1\'-pyrano[3,4-b]indol]-4-amine
CAS号
863513-91-1
分子式
C24H27FN2O
分子量
378.482
精确质量
378.211
PSA
28.26
LOGP
5.1061
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