(−)-WIN 55,212-3 is an aminoalkylindole derivative which acts as a competitive neutral antagonist of the human cannabinoid CB receptor, blocking both the stimulating action of CP 55,940 (pA = 6.1) and the inverse agonism of SR 144528 (pEC = 5.3). (−)-WIN 55,212-3 neither antagonizes nor mimics the effects of Δ-THC on rat cerebellar membranes, which presumably express the CB receptor. (−)-WIN 55,212-3 also weakly antagonizes the melatonin MT and muscarinic M receptors but has no effect on several other G protein-coupled receptors.
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