fluperlapine

Fluperlapine is a morphanthridine derivative classified as an atypical antipsychotic with additional antidepressant and sedative effects[1][4][5]. It is structurally and pharmacologically similar to clozapine and belongs to the dibenzazepine class[1][5][7]. Fluperlapine acts as an antagonist at serotonin receptors (notably 5-HT2A, 5-HT2C, 5-HT6, 5-HT7), dopamine receptors (D1, D2, D3, D4), and muscarinic acetylcholine receptors (M1, M2, M3, M4, M5)[1][9][10]. Compared to typical neuroleptics, it shows weaker and shorter-acting affinity for dopaminergic systems, which has been proposed to underlie its lower incidence of extrapyramidal symptoms[3][4]. Despite demonstrating efficacy for schizophrenia, psychosis associated with Parkinson’s disease, depressive symptoms, and dystonia, it was never marketed, likely due to risk of agranulocytosis analogous to clozapine[1][7]. It was primarily developed and studied by Novartis. Fluperlapine’s development for schizophrenia reached Phase 3 trials before discontinuation[7][9]. Its binding profile supports its clinical effects, including potent antagonism of several serotonin and muscarinic receptors, and modest antagonism of dopamine receptors[1][9].

Other names

fluoroperlapinefluperlapine