Melperone-d4 hydrochloride
Based on 1 Customer Validation
Melperone-d4 hydrochloride is the deuterium labeled Melperone hydrochloride (HY-103109). 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.
For research use only. We do not sell to patients.
- Purity: 99.84%
- CAS No.: 1219798-80-7
- Formula: C16H19D4ClFNO
- Molecular Weight:303.84
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All 5-HT Receptor Isoforms
MoreAll Dopamine Receptor Isoforms
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Biological Activity
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Human D2 Receptor 180 nM (Kd) |
5-HT1A Receptor |
5-HT1D Receptor |
5-HT2A Receptor |
5-HT2C Receptor |
α1-adrenergic receptor 180 nM (Kd) |
α2-adrenergic receptor 150 nM (Kd) |
CYP2D6 |
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 1219798-80-7
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Unlabeled Cas 3575-80-2
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Appearance Solid
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Molecular Weight 303.84
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Formula C16H19D4ClFNO
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Color White to off-white
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SMILES
CC(CC1([2H])[2H])CC([2H])([2H])N1CCCC(C2=CC=C(C=C2)F)=O.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 20 mg/mL (65.82 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief]
[2]. 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. [Content Brief]
[3]. 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. [Content Brief]
[4]. 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. [Content Brief]
[5]. 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2912 mL | 16.4560 mL | 32.9121 mL | 82.2801 mL |
| 5 mM | 0.6582 mL | 3.2912 mL | 6.5824 mL | 16.4560 mL | |
| 10 mM | 0.3291 mL | 1.6456 mL | 3.2912 mL | 8.2280 mL | |
| 15 mM | 0.2194 mL | 1.0971 mL | 2.1941 mL | 5.4853 mL | |
| 20 mM | 0.1646 mL | 0.8228 mL | 1.6456 mL | 4.1140 mL | |
| 25 mM | 0.1316 mL | 0.6582 mL | 1.3165 mL | 3.2912 mL | |
| 30 mM | 0.1097 mL | 0.5485 mL | 1.0971 mL | 2.7427 mL | |
| 40 mM | 0.0823 mL | 0.4114 mL | 0.8228 mL | 2.0570 mL | |
| 50 mM | 0.0658 mL | 0.3291 mL | 0.6582 mL | 1.6456 mL | |
| 60 mM | 0.0549 mL | 0.2743 mL | 0.5485 mL | 1.3713 mL |
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