Antidote to cannabinoid intoxication: the CB₁ receptor inverse agonist, AM251, reverses hypothermic effects of the CB₁ receptor agonist, CB‐13, in mice

BACKGROUND AND PURPOSE: receptor antagonism could reverse physical cannabimimetic effects. EXPERIMENTAL APPROACH: receptor antagonist/inverse agonist AM251 (N-(piperidin-1-yl)-5-(4-iodophenyl)-1-(2, 4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide) was administered 20 min after the injection of CB-13 and its effects on the cannabimimetic responses were assessed. KEY RESULTS: receptor antagonist/inverse agonist. There was also a subjective reversal of visually evident sedation. CONCLUSIONS AND IMPLICATIONS: Cannabinoid receptor antagonists have been widely used and so may provide an acceptable single-dose antidote to cannabinoid intoxication. This use may save human life, where the life-threatening effects are mediated by cannabinoid receptors and not off-target influences of the synthetic cannabinoids or non-cannabinoids within the recreational drug mixture.