Cannabinoids (CBs) and their synthetic analogs produce biochemical and pharmacological effects by interacting with the central CB and peripheral CB receptors. The CB receptor has emerged as a pharmacotherapeutic target for treating osteoporosis, as well as for eliciting antinociceptive effects in various models of pain. 4-Quinolone-3-carboxamide CB ligand is a selective, high-affinity ligand of the CB receptor, displaying a K value of 0.6 nM (K >10,000 nM for CB) in vitro. At a dose of 6 mg/kg, 4-quinolone-3-carboxamide CB ligand exhibits antinociceptive activity in a formalin test of nocifensive response in mice. This analgesic affect is not significantly reversed by the CB antagonist AM630 , which suggests 4-quinolone-3-carboxamide CB ligand may behave as an inverse agonist.