It has been tried in treatment-resistant cases of schizophrenia with some (albeit limited) success.[4][5][6][7] It has also been reported effective in the treatment ofL-DOPA and other forms of psychosis inParkinson's disease[8] (although a multicentre, double-blind, placebo-controlled study conducted in 2012 failed to support these findings[9]). It is also known to possess anxiolytic properties.[10] It is marketed in the following countries:[3][11]
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.[23]
For the last step of the synthesis the sidechain 4-Chloro-4'-Fluorobutyrophenone [3874-54-2] (1) is attached to 4-Methylpiperidine (4-Pipecoline) [626-58-4] (2).
^abcBorgström L, Larsson H, Molander L (1982). "Pharmacokinetics of parenteral and oral melperone in man".European Journal of Clinical Pharmacology.23 (2):173–6.doi:10.1007/BF00545974.PMID7140807.S2CID36697288.
^abcdProduct Information: Eunerpan(R), Melperonhydrochlorid (Report). Knoll Deutschland GmbH, Ludwigshafen. 1995.
^abMelperone Hydrochloride. The Royal Pharmaceutical Society of Great Britain. 30 January 2013. Archived fromthe original on 14 January 2021. Retrieved3 November 2013.{{cite book}}:|work= ignored (help)
^Sumiyoshi T, Meltzer HY, Jayathilake K (2004). "Melperone, an atypical antipsychotic drug, in the treatment of schizophrenia: dose-response analysis on effectiveness and tolerability, and efficacy for treatment-resistant schizophrenia and cognitive function".International Clinical Psychopharmacology.19 (3): 184.doi:10.1097/00004850-200405000-00039.
^Barbato L, Monge A, Stocchi F, Nordera G. Melperone in the treatment of iatrogenic psychosis in Parkinson's disease. Funct Neurol. 1996 Aug;11(4):201–7.
^Bobo WV, Jayathilake K, Lee MA, Meltzer HY (April 2010). "Changes in weight and body mass index during treatment with melperone, clozapine and typical neuroleptics".Psychiatry Research.176 (2–3):114–9.doi:10.1016/j.psychres.2009.03.026.PMID20199813.S2CID25366120.
^Bobo WV, Jayathilake K, Lee MA, Meltzer HY (July 2009). "Melperone, an aytpical antipsychotic drug with clozapine-like effect on plasma prolactin: contrast with typical neuroleptics".Human Psychopharmacology.24 (5):415–22.doi:10.1002/hup.1036.PMID19551763.S2CID25812368.
^Molander L, Borgström L (1983). "Sedative effects and prolactin response to single oral doses of melperone".Psychopharmacology.79 (2–3):142–7.doi:10.1007/bf00427801.PMID6133301.S2CID392818.
^Molander L, Birkhed D (1981). "Effect of single oral doses of various neuroleptic drugs on salivary secretion rate, pH, and buffer capacity in healthy subjects".Psychopharmacology.75 (2):114–8.doi:10.1007/bf00432171.PMID6119724.S2CID780924.
^abcKirkegaard A, Kirkegaard G, Geismar L, Christensen I (1981). "Additional studies on side effects of melperone in long-term therapy for 1 to 15 years in psychiatric patients".Arzneimittel-Forschung.31 (4):737–40.PMID6113835.
^abcChristensen I, Geismar L, Kirkegaard A, Kirkegaard G (May 1986). "Additional studies on side effects of melperone in long-term therapy for 1-20 years in psychiatric patients".Arzneimittel-Forschung.36 (5):855–60.PMID2873821.
^Köhnke MD, Lutz U, Wiatr G, Schwärzler F, Weller B, Schott K, Buchkremer G (April 2006). "Cytochrome P450 2D6 dependent metabolization of risperidone is inhibited by melperone".European Journal of Clinical Pharmacology.62 (4):333–4.doi:10.1007/s00228-006-0098-y.PMID16534635.S2CID13168439.
^Grözinger M, Dragicevic A, Hiemke C, Shams M, Müller MJ, Härtter S (January 2003). "Melperone is an inhibitor of the CYP2D6 catalyzed O-demethylation of venlafaxine".Pharmacopsychiatry.36 (1):3–6.doi:10.1055/s-2003-38084.PMID12649767.S2CID260242201.
^Roth BL, Driscol J."PDSP Ki Database".Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Archived fromthe original on 2013-11-08. Retrieved2013-10-14.
^BE651144 idem Erik Harry Hernestam Sven, et al.GB 1029220 (1966 to Ferrosan); CA, 63, 13244c
^Leyva-Pérez, Antonio; Cabrero-Antonino, Jose R.; Rubio-Marqués, Paula; Al-Resayes, Saud I.; Corma, Avelino (2014). "Synthesis of the ortho/meta/para Isomers of Relevant Pharmaceutical Compounds by Coupling a Sonogashira Reaction with a Regioselective Hydration". ACS Catalysis. 4 (3): 722–731. doi:10.1021/cs401075z.
Clinical trial numberNCT00125138 for "Melperone (an Anti-Psychotic) in Patients With Psychosis Associated With Parkinson's Disease" atClinicalTrials.gov
