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Perlapine is an atypical neuroleptic that blocks dopamine and serotonin (5-HT) receptors (Kis = 60, 30, and 30 nM for D2, D4, and 5-HT2A, respectively).1 Perlapine is also an agonist for hM3Dq, a designer receptor exclusively activated by designer drugs (DREADDs) derived from the human muscarinic acetylcholine M3 receptor that activates neuronal firing.2 Perlapine displays >10,000-fold selectivity for hM3Dq over hM3.2
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1. Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors. Neuropsychopharmacology 16(2), 93-110 (1997).
2. The first structure-