Nalmefene (hydrochloride)

A µ- and kappa-opioid receptor antagonist (Kis = 0.91 and 1.03 nM, respectively, in CHO membranes expressing the human receptors), selective for µ- and kappa-opioid receptors over delta-opioid receptors (Ki = 13.26 nM in CHO membranes expressing the human receptors), decreases self-administration of alcohol in non-alcohol- and alcohol-dependent rats, reduces food and water intake and body weight in obese and lean rats at 25 mg/kg per day, inhibits morphine-induced scratching behavior and increases in the latency to tail withdrawal in a warm water tail withdrawal assay in rhesus monkeys at 32 µg/kg. Formulation: A solid. InChI: InChI=1S/C21H25NO3.ClH/c1-12-6-7-21(24)16-10-14-4-5-15(23)18-17(14)20(21,19(12)25-18)8-9-22(16)11-13-2-3-13,/h4-5,13,16,19,23-24H,1-3,6-11H2,1H/t16-,19+,20+,21-,/m1./s1. InChIKey: GYWMRGWFQPSQLK-OPHZJPRHSA-N. SMILES: O[C@]12[C@]3(CCN(CC4CC4)[C@@H]2C5)[C@](OC6=C3C5=CC=C6O)([H])C(CC1)=C.Cl