CAY10508 is a potent and selective inverse agonist for the central cannabinoid (CB1) receptor with therapeutic potential for treating obesity and drug dependence, lacking psychotropic effects. It exhibits a Ki value of 243 nM and an EC50 of 195 nM. At a concentration of 10 µM, CAY10508 displaces [3H]-CP-55,940 with 100% efficacy at the CB1 receptor and 35% at the peripheral cannabinoid (CB2) receptor. Its inverse agonist activity at the CB1 receptor was confirmed through a [35S]-GTPgammaS binding assay.
Molekulargewicht:
486.2
CAS Nummer:
[878533-35-8]
Formel:
C21H14Br2N2O2
Target-Kategorie:
Others|||Cannabinoid Receptor
T84518
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