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Melperone

CAT: 0804-HY-B2169-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-B2169-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
5-HT1 Receptor;5-HT2 Receptor; CYP2D6; D2 Receptor; α adrenergic receptor

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