Ocaperidone

Ocaperidone is an atypical antipsychotic that binds to dopamine D2 receptors (Ki = 0. nM), alpha1-adrenergic receptors (alpha1-ARs, Ki = 0. nM), and the serotonin (5-HT) receptor subtype 5-HT2 (Ki = 0. nM). It is selective for these receptors over a panel of 26 additional receptors, transporters, channels, and enzymes but does bind to alpha2-ARs, 5-HT1A, 5-HT1D, and the histamine H1 receptor (Kis = 5. 6. 9. and 1. nM, respectively). Ocaperidone increases the levels of homovanillic acid (Cay-27307) and 3,4-dihydroxyphenylacetic acid (DOPAC, Cay-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. 0. and 0. mg/kg, respectively) and tryptamine-induced clonic seizures and mescaline-induced head twitches (ED50s = 0. and 0. mg/kg, respectively) in rats. Ocaperidone decreases locomotor activity and food intake (ED50s = 0. and 0. mg/kg, respectively) and induces catalepsy, palpebral ptosis, and hypotonia (ED50s = 0. 1. and 5. 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. 1. 1. and 5. mg/kg, respectively).. Solulibility: Chloroform: Soluble: = 10 mg/ml: DMSO: Slightly soluble: 0.1-1 mg/ml.