Melperone hydrochloride
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.
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- CAS No.: 1622-79-3
- Formule: C16H23ClFNO
- Masse moléculaire:299.81
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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5-HT1A Receptor |
5-HT1D Receptor |
5-HT2A Receptor |
5-HT2C Receptor |
Human D2 Receptor 180 nM (Kd) |
α1-adrenergic receptor 180 nM (Kd) |
α2-adrenergic receptor 150 nM (Kd) |
CYP2D6 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley albino rats (180-200 g) was administered subcutaneously with D-Amphetamine sulfate (1.0 mg/kg)[1]
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Dosage:2 mg/kg/day
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Administration:Drinking water; changed in lightproof drinking bottles twice a week; for 21 days
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Result:Increased basal extracellular DA and enhanced D-Amphetamine-induced DA release in the striatum.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1622-79-3
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Masse moléculaire 299.81
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Formule C16H23ClFNO
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SMILES
O=C(C1=CC=C(F)C=C1)CCCN2CCC(C)CC2.Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvant et solubilité
DMSO : 50 mg/mL (166.77 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
Références
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3354 mL | 16.6772 mL | 33.3545 mL | 83.3861 mL |
| 5 mM | 0.6671 mL | 3.3354 mL | 6.6709 mL | 16.6772 mL | |
| 10 mM | 0.3335 mL | 1.6677 mL | 3.3354 mL | 8.3386 mL | |
| 15 mM | 0.2224 mL | 1.1118 mL | 2.2236 mL | 5.5591 mL | |
| 20 mM | 0.1668 mL | 0.8339 mL | 1.6677 mL | 4.1693 mL | |
| 25 mM | 0.1334 mL | 0.6671 mL | 1.3342 mL | 3.3354 mL | |
| 30 mM | 0.1112 mL | 0.5559 mL | 1.1118 mL | 2.7795 mL | |
| 40 mM | 0.0834 mL | 0.4169 mL | 0.8339 mL | 2.0847 mL | |
| 50 mM | 0.0667 mL | 0.3335 mL | 0.6671 mL | 1.6677 mL | |
| 60 mM | 0.0556 mL | 0.2780 mL | 0.5559 mL | 1.3898 mL | |
| 80 mM | 0.0417 mL | 0.2085 mL | 0.4169 mL | 1.0423 mL | |
| 100 mM | 0.0334 mL | 0.1668 mL | 0.3335 mL | 0.8339 mL |
Melperone hydrochloride Related Classifications
HY-103109 Related Classifications
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