Perlapine, sold under the brand names Hypnodine and Pipnodine, is a hypnotic and sedative of the tricyclic group which is marketed in Japan.[1] It acts primarily as a potent antihistamine,[2] and also has anticholinergic,[2] antiserotonergic,[3] antiadrenergic, and some antidopaminergic activity.[3][4][5][6] The drug has relatively weak affinity for the dopamine D2 receptor (IC50 = 1,803 nM) and, in accordance, is said to be ineffective as an antipsychotic.[6][7] However, it retains higher affinity for the dopamine D1 receptor (IC50 = 198 nM).[6] Its IC50 values are 19 nM for the α1-adrenergic receptor, 4,945 nM for the α2-adrenergic receptor, and 70 nM for the serotonin 5-HT2A receptor.[6] Perlapine is closely related to clotiapine, clozapine, fluperlapine, loxapine, and tilozepine.[6]
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Trade names | Hypnodine, Pipnodine |
Other names | AW-14233; HF-2333; MP-11; PLP 100-127; 6-(4-Methyl-1-piperazinyl)morphanthridine |
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ECHA InfoCard | 100.241.831 |
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Formula | C19H21N3 |
Molar mass | 291.398 g·mol−1 |
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Perlapine has been suggested as a potential ligand for certain DREADDs.[8][9]