Melperone

Melperone is a butyrophenone with atypical antipsychotic properties. Melperone 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 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 is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly[1][2][3][4].

Product Specifications

CAS Number

[3575-80-2]

UNSPSC

12352005

Hazard Statement

H302, H312, H319, H332

Target

5-HT Receptor; Adrenergic Receptor; Cytochrome P450; Dopamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Metabolic Enzyme/Protease; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/melperone.html

Purity

99.84

Solubility

DMSO : 41.67 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C16H22FNO

Molecular Weight

263.35

Precautions

H302, H312, H319, H332

References & Citations

[1]Hefner G, et al. Melperone but not bisoprolol or metoprolol is a clinically relevant inhibitor of CYP2D6: evidence from a therapeutic drug monitoring survey. J Neural Transm (Vienna) . 2015 Nov;122 (11) :1609-17.|[2]Bobo WV, et al. Melperone, an aytpical antipsychotic drug with clozapine-like effect on plasma prolactin: contrast with typical neuroleptics. Hum Psychopharmacol. 2009 Jul;24 (5) :415-22.|[3]Ichikawa J, et al. The effect of chronic atypical antipsychotic drugs and haloperidol on amphetamine-induced dopamine release in vivo. Brain Res. 1992 Mar 6;574 (1-2) :98-104. |[4]Richelson E, et al. Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68 (1) :29-39.