Melperone hydrochloride Chemical Properties

Melting point:

209-211℃

storage temp. 

Inert atmosphere,Store in freezer, under -20°C

solubility 

Chloroform (Slightly), Methanol (Slightly), Water (Slightly)

form 

Solid

color 

White to Light Brown

Safety Information

Toxicity

LD50 in rats, mice (mg/kg): 330, 230 orally; 40, 35 i.v. (Christensen)

Melperone hydrochloride Usage And Synthesis

Chemical Properties

White Solid

Originator

Eunerpan,Nordmark,W. Germany,1965

Uses

Melperone Hydrochloride is an atypical antipsychotic drug.

Uses

Melperone hydrochloride is a neuroleptic butyrophenone. Melperone is also an antiarrhythmic agent. Melperone is an effective atypical antipsychotic drug used in the treatment of schizophrenia.

Manufacturing Process

A solution or dispersion consisting of 20.1 g (0.1 mol) of γ-chloro-pfluorobutyrophenone, 19.8 g (0.2 mol) of 4-methylpiperidine and 0.1 g of potassium iodide in 150 ml toluene is heated in a sealed glass tube for 15 hours at 100°C to 110°C. The potassium iodide and the 4-methylpiperidine hydrochloride formed in the reaction are separated by filtration and the solvent removed from the filtrate by evaporation in vacuum on a steam bath. The residue is distilled and the fraction obtained at 120°C to 125°C and at a pressure lower than 0.1 mm Hg is collected. The base is dissolved in ether and the 4-fluoro-γ-(4-methylpiperidino)-butyrophenone precipitated as the hydrochloride. The reaction product is purified by recrystallization in ethanol/ether.
Yield 22.0 g (73% of theory). MP 209°C to 211°C.

Therapeutic Function

Neuroleptic

Biological Activity

Atypical neuroleptic; 5-HT 2A /D 2 receptor antagonist (K i values are 120 and 180 nM respectively). Causes an increase in dopamine levels in the medial prefrontal cortex (mPFC) and nucleus accumbens and an increase in ACh in the mPFC. Also binds adrenergic α 1 and α 2 receptors (K i values are 180 and 150 nM respectively).

Safety Profile

Poison by ingestion, subcutaneous, and intravenous routes. Experimental teratogenic effects. A neuroleptic drug used to treat anxiety and confusion. When heated to decomposition it emits very toxic fumes of F-, NOx, and HCl.

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