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Perospirone is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT2 and 5-HT1A and the dopamine D2 receptor (Kis = 0.61, 2.9, and 1.4 nM, respectively, in rat brain membranes).1 It is selective for these receptors over the dopamine D1 and α1- and α2-adrenergic receptors (Kis = 41, 17, and 408 nM, respectively) and a panel of six other receptors (Kis = >1,000 nM for all). Perospirone inhibits clonic seizures induced by tryptamine (Item No. 20995) and reduces hyperactivity induced by methamphetamine in rats and climbing behavior induced by apomorphine in mice (ED50s = 1.4, 2.2, and 3.5 mg/kg, respectively) but does not induce catalepsy in rats or mice.2 Formulations containing perospirone have been used in the treatment of schizophrenia and acute bipolar mania.
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1. Binding profile of SM-
2. Pharmacological actions of SM-