A CB1 inverse agonist
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Central cannabinoid (CB1) receptor antagonists and inverse agonists exhibit therapeutic potential for obesity and drug dependence, while being devoid of psychotropic effects. CAY10508 is a potent and selective central cannabinoid (CB1) receptor inverse agonist with a Ki value of 243 nM and an EC50 of 195 nM. A 10 µM concentration of CAY10508 resulted in 100% and 35% displacement of [3H]-CP-55,940 at the CB1 and peripheral cannabinoid (CB2) receptors, respectively. A [35S]-GTPγS binding assay revealed the inverse agonist properties of CAY10508 at the CB1 receptor.
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