Rimonabant is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.

AM251 is a potent CB1 receptor antagonist (IC50 = 8 nM, Ki = 7.49 nM) that displays 306-fold selectivity over CB2 receptors and also a potent GPR55 agonist (EC50 = 39 nM).

Otenabant HCl is a recently discovered selective, high affinity, competitive CB1 receptor antagonist with Ki of 0.7 nM.