Moperone

Moperone is a dopamine D₂, D₃, and D₄ receptor antagonist (K_is = 0.7, 14, and 27 nM, respectively, in NIH3T3 cells expressing the human receptors).¹ It also inhibits E. electricus acetylcholinesterase (AChE; K_i = 120 µM) and is a histamine H₁ receptor inverse agonist (IC₅₀ = 794 nM for the human receptor).^2,3 Intraocular administration of moperone (0.5% w/v) induces ocular hypotension in normotensive rabbits.⁴ Formulations containing moperone have been used in the treatment of schizophrenia, psychosis, epilepsy, and alcohol withdrawal syndrome.

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1. Burstein, E.S., Ma, J., Wong, S., et al. Intrinsic efficacy of antipsychotics at human D₂, D₃, and D₄ dopamine receptors: Identification of the clozapine metabolite N-desmethylclozapine as a D₂/D₃ partial agonist. J. Pharmacol. Exp. Ther. 315(3), 1278-1287 (2005).

2. Michalek, H. Inhibition of cholinesterase and acetylcholinesterase in vitro by butyrophenone neuroleptics. Biochem. Pharmacol. 22(9), 1067-1074 (1973).

3. Bakker, R.A., Nicholas, M.W., Smith, T.T., et al. In vitro pharmacology of clinically used central nervous system-active drugs as inverse H1 receptor agonists. J. Pharmacol. Exp. Ther. 322(1), 172-179 (2007).

4. Chiou, G.C.Y., Li, B.H.P., and Chiou, F.Y. Effects of dopamine antagonists injected through vortex veins on intraocular pressure. J. Ocul. Pharmacol. 5(4), 281-291 (1989).