Ocaperidone

Ocaperidone is an atypical antipsychotic that binds to dopamine D₂ receptors (K_i = 0.75 nM), α₁-adrenergic receptors (α₁-ARs; K_i = 0.46 nM), and the serotonin (5-HT) receptor subtype 5-HT₂ (K_i = 0.14 nM).¹ It is selective for these receptors over a panel of 26 additional receptors, transporters, channels, and enzymes but does bind to α₂-ARs, 5-HT_1A, 5-HT_1D, and the histamine H₁ receptor (K_is = 5.4, 6.8, 9.6, and 1.6 nM, respectively). Ocaperidone increases the levels of homovanillic acid (Item No. 27307) and 3,4-dihydroxyphenylacetic acid (DOPAC; Item No. 24912) in the striatum, nucleus accumbens, tuberculum olfactorium, and frontal cortex in rats in a dose-dependent manner. It inhibits apomorphine-induced stereotypy and cocaine- or amphetamine-induced agitation (ED₅₀s = 0.018, 0.042, and 0.014 mg/kg, respectively) and tryptamine-induced clonic seizures and mescaline-induced head twitches (ED₅₀s = 0.021 and 0.037 mg/kg, respectively) in rats.² Ocaperidone decreases locomotor activity and food intake (ED₅₀s = 0.024 and 0.074 mg/kg, respectively) and induces catalepsy, palpebral ptosis, and hypotonia (ED₅₀s = 0.39, 1.34, and 5.37 mg/kg, respectively) in rats. It also inhibits LSD-induced drug discrimination, ovalbumin and histamine-induced skin sensitization, acetic acid-induced writhing, and xylazine-induced loss of the righting reflex in rats (ED₅₀s = 0.021, 1.18, 1.34, and 5.37 mg/kg, respectively).

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1. Leysen, J.E., Janssen, P.M., Gommeren, W., et al. In vitro and in vivo receptor binding and effects on monoamine turnover in rat brain regions of the novel antipsychotics risperidone and ocaperidone. Mol. Pharmacol. 41(3), 494-508 (1992).

2. Megens, A.A.H.P., Awouters, F.H., Meert, T.F., et al. Pharmacological profile of the new potent neuroleptic ocaperidone (R 79,598). 260(1), 146-159 (1992).