Perlapine exhibits antipsychotic activity and blocks dopamine and serotonin receptors. Perlapine is also a novel agonist of hM3Dq, a designer receptor exclusively activated by designer drugs (DREADD).
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). Perlapine is also an agonist for hM3Dq, a designer receptor exclusively activated by designer drugs (DREADD) derived from the human muscarinic acetylcholine M3 receptor that activates neuronal firing. Perlapine displays >10,000-fold selectivity for hM3Dq over hM3.
