Sertindole (Lu 23-174)

An atypical antipsychotic

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10mg

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Background

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).¹ 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.² Sertindole (2.5 mg/kg) reverses ketamine-induced impairments in the extradimensional shift stage of the attentional set-shifting task (ASST) in rats.³ It reverses phencyclidine (PCP)-induced selective reversal learning deficits in rats and subchronic PCP-induced deficits in the novel object recognition task in mice.⁴ 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 in rats.⁵ Formulations containing sertindole have been used in the treatment of schizophrenia.

1.Richelson, E., and Souder, T.Binding of antipsychotic drugs to human brain receptors: Focus on newer generation compoundsLife Sci.68(1)29-39(2000) 2.M?rk, A., Witten, L.M., and Arnt, J.Effect of sertindole on extracellular dopamine, acetylcholine, and glutamate in the medial prefrontal cortex of conscious rats: A comparison with risperidone and exploration of mechanisms involvedPsychopharmacol. (Berl)206(1)39-49(2009) 3.Nikiforuk, A., and Popik, P.Effects of quetiapine and sertindole on subchronic ketamine-induced deficits in attentional set-shifting in ratsPsychopharmacol. (Berl)220(1)65-74(2012) 4.Idris, N., Neill, J., Grayson, B., et al.Sertindole improves sub-chronic PCP-induced reversal learning and episodic memory deficits in rodents: Involvement of 5-HT6 and 5-HT 2A receptor mechanismsPsychopharmacol. (Berl)208(1)23-36(2010) 5.Carli, M., Calcagno, E., Mainini, E., et al.Sertindole restores attentional performance and suppresses glutamate release induced by the NMDA receptor antagonist CPPPsychopharmacol. (Berl)214(3)625-637(2011)