Melperone


Melperone, Buronil, Eunerpan ) is an atypical antipsychotic of the butyrophenone chemical class, making it structurally related to the typical antipsychotic haloperidol. It first entered clinical use in 1960s.

Marketing and indications

It has been tried in treatment-resistant cases of schizophrenia with some success. It has also been reported effective in the treatment of L-DOPA and other forms of psychosis in Parkinson's disease. It is also known to possess anxiolytic properties. It is marketed in the following countries:
Melperone is reported to produce significantly less weight gain than clozapine and approximately as much weight gain as typical antipsychotics. It is also purported to produce around as much prolactin secretion as clozapine. It is also purported to produce sedative effects and QT interval prolongation. It is also known to produce less extrapyramidal side effects than the first-generation antipsychotic, thiothixene. It can also produce dry mouth.
;Other common adverse effects include
;Rare adverse effects include
;Unknown frequency adverse effects include
Melperone is reported to be a CYP2D6 inhibitor.

Pharmacology

Melperone binds to the dopamine D2 receptor, just like all other clinically utilized antipsychotics, but it does so with a very low affinity and hence may be liable to rapidly dissociate from the D2 receptor hence potentially giving it the profile of an atypical antipsychotic.
ReceptorKi
5-HT1A2,200
5-HT1D3,400
5-HT2A230
5-HT2C2,100
5-HT61,254
5-HT7578
α1180
α2150
M1>10,000
M22,400
M3>10,000
M44,400
M5>10,000
D2194
D3347
D4555
H1580

Synthesis

For the last step of the synthesis the sidechain 4-Chloro-4'-Fluorobutyrophenone is attached to
4-Methylpiperidine .