Napamezole hydrochloride
Based on 1 Customer Validation
Napamezole hydrochloride is an orally active α-2 adrenergic receptor antagonist and serotonin (5-HT Receptor) reuptake inhibitor, with Ki values of 28 nM and 93 nM for rat α-2 and α-1 adrenergic receptors, respectively. Napamezole hydrochloride can be used for the research of depression.
For research use only. We do not sell to patients.
- Purity: 98.97%
- CAS No.: 87495-33-8
- Formula: C14H17ClN2
- Molecular Weight:248.75
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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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Biological Activity
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α2-adrenergic receptor 28 nM (Ki) |
α1-adrenergic receptor 93 nM (Ki) |
5-HT Receptor |
Napamezole (hydrochloride) inhibits [3H]Clonidine binding to rat brain alpha-2 adrenergic receptors with a Ki of 28 nM and inhibits [3H]Prazosin binding to rat brain alpha-1 adrenergic receptors with a Ki of 93 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Napamezole (30 mg/kg; p.o.) enhances the conversion rate of norepinephrine in the rat brain, confirming its in vivo α-2 adrenergic receptor blocking activity[1].
Napamezole (≥ 1 mg/kg, i.v.) enhances the firing activity of locus coeruleus neurons in rats and reverses the inhibitory effect of Clonidine on this firing activity, indicating that it exhibits in vivo α2-adrenergic receptor blocking activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 87495-33-8
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Appearance Solid
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Molecular Weight 248.75
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Formula C14H17ClN2
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Color Yellow to orange
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SMILES
C1(CC2=CC3=C(CC2)C=CC=C3)=NCCN1.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 31.25 mg/mL (125.63 mM; Need ultrasonic; 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 (stored under nitrogen). 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 (stored under nitrogen). 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 (274 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]. Perrone MH, et al. In vivo assessment of napamezole, an alpha-2 adrenoceptor antagonist and monoamine re-uptake inhibitor. J Pharmacol Exp Ther. 1990;254(2):476-483. [Content Brief]
[2]. Perrone MH, et al. Napamezole, an alpha-2 adrenergic receptor antagonist and monoamine uptake inhibitor in vitro. J Pharmacol Exp Ther. 1990;254(2):471-475. [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 (stored under nitrogen). 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 | 4.0201 mL | 20.1005 mL | 40.2010 mL | 100.5025 mL |
| 5 mM | 0.8040 mL | 4.0201 mL | 8.0402 mL | 20.1005 mL | |
| 10 mM | 0.4020 mL | 2.0101 mL | 4.0201 mL | 10.0503 mL | |
| 15 mM | 0.2680 mL | 1.3400 mL | 2.6801 mL | 6.7002 mL | |
| 20 mM | 0.2010 mL | 1.0050 mL | 2.0101 mL | 5.0251 mL | |
| 25 mM | 0.1608 mL | 0.8040 mL | 1.6080 mL | 4.0201 mL | |
| 30 mM | 0.1340 mL | 0.6700 mL | 1.3400 mL | 3.3501 mL | |
| 40 mM | 0.1005 mL | 0.5025 mL | 1.0050 mL | 2.5126 mL | |
| 50 mM | 0.0804 mL | 0.4020 mL | 0.8040 mL | 2.0101 mL | |
| 60 mM | 0.0670 mL | 0.3350 mL | 0.6700 mL | 1.6750 mL | |
| 80 mM | 0.0503 mL | 0.2513 mL | 0.5025 mL | 1.2563 mL | |
| 100 mM | 0.0402 mL | 0.2010 mL | 0.4020 mL | 1.0050 mL |
Napamezole hydrochloride Related Classifications
Cat. No.: HY-W982195
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- Napamezole
- 87495-33-8
- Adrenergic Receptor
- 5-HT Receptor
- rat alpha-1 adrenergic receptor
- rat vas deferens
- rat brain alpha-2 adrenergic receptor
- locus coeruleus neuronal firing
- alpha-2 adrenergic receptor
- norepinephrine turnover
- 5-hydroxytryptamine re-uptake inhibitor
- rat alpha-2 adrenergic receptor
- monoamine re-uptake
- antinociception
- Inhibitor
- inhibitor
- inhibit