1. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease
  2. 5-HT Receptor Dopamine Receptor Adrenergic Receptor Cytochrome P450
  3. Melperone hydrochloride

Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values ​​of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly.

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Melperone hydrochloride Chemical Structure

Melperone hydrochloride Chemical Structure

CAS No. : 1622-79-3

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Based on 1 publication(s) in Google Scholar

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Description

Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values ​​of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly[1][2][3][4].

IC50 & Target[2][4]

Human D2 Receptor

180 nM (Kd)

α1-adrenergic receptor

180 nM (Kd)

α2-adrenergic receptor

150 nM (Kd)

CYP2D6

 

In Vivo

Melperone (2 mg/kg/day; drinking water; changed in lightproof drinking bottles twice a week; for 21 days) hydrochloride increases basal, but not D-Amphetamine-induced, extracellular dopamine levels in the rat nucleus accumbens[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley albino rats (180-200 g) was administered subcutaneously with D-Amphetamine sulfate (1.0 mg/kg)[1]
Dosage: 2 mg/kg/day
Administration: Drinking water; changed in lightproof drinking bottles twice a week; for 21 days
Result: Increased basal extracellular DA and enhanced D-Amphetamine-induced DA release in the striatum.
Molecular Weight

299.81

Formula

C16H23ClFNO

CAS No.
SMILES

O=C(C1=CC=C(F)C=C1)CCCN2CCC(C)CC2.Cl

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Melperone hydrochloride
Cat. No.:
HY-103109
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