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.

CAS：863513-91-1
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;
分子式：C24H27FN2O
分子量：378.482
精确质量：378.211
Psa：28.26
Logp：5.1061

密度：1.2±0.1g/cm3
沸点：547.5±50.0°Cat760mmHg
闪点：284.9±30.1°C
蒸汽压：0.0±1.5mmHgat25°C
折射率：1.644
储存条件：2-8℃