Melperone hydrochloride

Name: Melperone hydrochloride
Brand: Tocris Bioscience
SKU: 2495

Tocris Bioscience a Bio-Techne Brand

Catalog # 2495

Citations (1)

COA / SDS

Discontinued Product

2495 has been discontinued. View all 5-HT2A Receptor Antagonists products.

Key Product Details

Description:	5-HT_2A antagonist; also D₂ antagonist; neuroleptic
Chemical Name:	1-(4-Fluorophenyl)-4-(4-methyl-1-piperidinyl)-1-butanone hydrochloride
Purity:	≥99% (HPLC)
Molecular Weight:	299.81

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Biological Activity for Melperone hydrochloride

Melperone hydrochloride is an atypical neuroleptic; 5-HT_2A/D₂ 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 α₁ and α₂ receptors (K_i values are 180 and 150 nM respectively).

Technical Data for Melperone hydrochloride

M. Wt	299.81
Formula	C₁₆H₂₂FNO.HCl
Storage	Desiccate at RT
Purity	≥99% (HPLC)
CAS Number	1622-79-3
PubChem ID	15386
InChi Key	MQHYXXIJLKFQGY-UHFFFAOYSA-N
Smiles	Cl.CC1CCN(CCCC(=O)C2=CC=C(F)C=C2)CC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Melperone hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	29.98	100
	DMSO	29.98	100

Preparing Stock Solutions for Melperone hydrochloride

The following data is based on the product molecular weight 299.81.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.34 mL	16.68 mL	33.35 mL
5 mM	0.67 mL	3.34 mL	6.67 mL
10 mM	0.33 mL	1.67 mL	3.34 mL
50 mM	0.07 mL	0.33 mL	0.67 mL

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References for Melperone hydrochloride

References are publications that support the biological activity of the product.

Uhr P-glycoprotein is a factor in the uptake of dextromethorphan, but not of melperone, into mouse brain: evidence for an overlap in substrate specificity between P-gp and CYP2D6. J.Psychopharmacol.
Ichikawa Atypical antipsychotic drugs, quetiapine, iloperidone, and melperone, preferentially increase DA and acetylcholine release in rat medial prefrontal cortex: role of 5-HT_1A receptor agonism. Brain Res. 2002 PMID: 12445705
Seeman Atypical neuroleptics have low affinity for DA D₂ receptors or are selective for D₄ receptors. Neuropsychopharmacology. 1997 PMID: 9015795

Citations for Melperone hydrochloride (1)

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Citations are publications that use Bio-Techne products. Selected citations for Melperone hydrochloride include:

Hacker et al. (2015) Substrate-Dependent Inhibition of the Human Organic Cation Transporter OCT2: A Comparison of MetF. with Experimental Substrates. Brain Res. 10:e0136451
PMID: 26327616

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