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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.

1,3-Bis(4-bromophenyl)-5-phenyl-2,4-imidazolidinedione is a central cannabinoid (CB1) receptor antagonist and inverse agonist. It may be a potential therapeutic agent for treating obesity and drug dependence.

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

hCB₁: 195 nM (EC₅₀); hCB₁: 243 nM (Ki)

[1] GIULIO G. MUCCIOLI. Synthesis and Activity of 1,3,5-Triphenylimidazolidine-2,4-diones and 1,3,5-Triphenyl-2-thioxoimidazolidin-4-ones: Characterization of New CB1 Cannabinoid Receptor Inverse Agonists/Antagonists[J]. Journal of Medicinal Chemistry, 2006, 49 3: 872-882. DOI: 10.1021/jm050484f