Melperone-d4 (hydrochloride)

Melperone-d4 hydrochloride is the deuterium labeled Melperone hydrochloride (HY-103109) [1]. 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[2][3][4][5].

Product Specifications

CAS Number

[1219798-80-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

5-HT Receptor; Adrenergic Receptor; Cytochrome P450; Dopamine Receptor; Isotope-Labeled Compounds

Type

Isotope-Labeled Compounds

Related Pathways

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

Field of Research

Neurological Disease

Purity

99.84

Solubility

DMSO : 20 mg/mL (ultrasonic; warming)

Smiles

CC(CC1([2H])[2H])CC([2H])([2H])N1CCCC(C2=CC=C(C=C2)F)=O.Cl

Molecular Formula

C16H19D4ClFNO

Molecular Weight

303.84

Precautions

H302, H315, H319, H335

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]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.|[3]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.|[4]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. |[5]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.