Cayman Sertindole

Sertindole is an atypical antipsychotic that binds to dopamine D₂ receptors and the serotonin (5-HT) receptor subtypes 5-HT_1D, 5-HT_2A, and 5-HT_2C (K_ds = 2.7, 20, 0.14, and 6 nM, respectively). It also binds to histamine H₁ and α₁- and α₂-adrenergic receptors (K_ds = 320, 3.9, and 190 nM, respectively). In vivo, sertindole (10 mg/kg) increases extracellular dopamine, acetylcholine (ACh), and glutamate levels in the medial prefrontal cortex in conscious rats. Sertindole (2.5 mg/kg) reverses ketamine-induced impairments in the extradimensional shift stage of the attentional set-shifting task (ASST) in rats. It reverses phencyclidine (PCP)-induced selective reversal learning deficits in rats and subchronic PCP-induced deficits in the novel object recognition task in mice. Sertindole (0.02-0.32 mg/kg) also prevents accuracy deficits and anticipatory over-responding in the 5-choice serial reaction time task (5CSRTT) induced by the NMDA receptor antagonist (R)-CPP (Item No. ) in rats. Formulations containing sertindole have been used in the treatment of schizophrenia.

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