Melperone
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Melperone
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CAS No:
3575-80-2
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Formula:
C16H22FNO
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Chemical Name:
Melperone
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Synonyms:
1-Butanone,1-(4-fluorophenyl)-4-(4-methyl-1-piperidinyl)-;Butyrophenone,4′-fluoro-4-(4-methylpiperidino)-;1-(4-Fluorophenyl)-4-(4-methyl-1-piperidinyl)-1-butanone;4′-Fluoro-4-(4-methylpiperidino)butyrophenone;γ-(4-Methylpiperidino)-p-fluorobutyrophenone;Methylperone;4-Fluoro-γ-(4-methylpiperidino)butyrophenone;Buronil;FG 5111;Melperone;Flubuperone;Buronon
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CAS No:
Description
Melperone, a butyrophenone, is an antipsychotic drug used for sleep induction which is frequently prescribed in psychiatric setting[1]. Melperone has been used for a variety of indications, including the treatment of schizophrenia, but also for agitation in the elderly[2].
1-(4-fluorophenyl)-4-(4-methyl-1-piperidinyl)-1-butanone is an aromatic ketone.|Melperone is an atypical antipsychotic of the butyrophenone chemical class, making it structurally related to the typical antipsychotic haloperidol. Melperone has been used for a span of greater than 30 years in the European Union. It has been well established in the treatment of confusion, anxiety, restlessness (particularly in the elderly) and schizophrenia as It is known to be well-tolerated with an excellent safety profile. Recently, it has been studied as a treatment of psychosis related to Parkinson's disease.
Characteristics
20.3
3.45840
1.046g/cm3
<25 °C
122.5 °C
181.3ºC
163.5 Ų [M+H]+ [CCS Type: TW, Method: Major Mix IMS/Tof Calibration Kit (Waters)]
Safety Information
P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P312, P304+P340, P305+P351+P338, P312, P322, P330, P337+P313, P363, P501
H302
Toxicity
An overdose of Melperone may result in cardiac arrhythmias.
Melperone has a bioavailability of 50-70%.
Drug Information
For the treatment of schizophrenia, sleep, disorders, agitation and mentally confused states.
Melperone has been demonstrated to produce an antipsychotic effect at doses that cause minimal extrapyramidal symptoms frequently associated with more traditional antipsychotics.
Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus. (See all compounds classified as Antipsychotic Agents.)
Oral doses are rapidly absorbed (Tmax 1.5–3.0 hours post oral ingestion).|Excreted mainly in the urine, with small amounts of unchanged drug.
Mainly hepatic.
Approximately 3-4 hours after oral administration. After intramuscular injection, the half-life has been found to be approximately 6 hours.
Melperone demonstrates antagonist activity at D2 dopaminergic and 5HT2A serotonergic receptors. It has a weak affinity to D2 receptors and possesses less risk of inducing dopamine receptor supersensitivity after both acute and chronic administration. In addition, the ratio of dopamine D4/D2 occupancy for melperone has been shown to resemble the binding profile of clozapine.
Buronil