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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 K_i 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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An imidazolidine-2,-4-dione derivative that is an effective and selective inverse agonist of CB cannabinoid receptor

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