Napamezole hydrochloride

Name: Napamezole hydrochloride
Brand: MedChemExpress
SKU: HY-W982195
Rating: 4.5 (0 reviews)

Cat. No.: HY-W982195 Purity: 98.97%: Data Sheet
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Napamezole hydrochloride is an orally active α-2 adrenergic receptor antagonist and serotonin (5-HT Receptor) reuptake inhibitor, with K_i 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.

Napamezole hydrochloride Chemical Structure

CAS No. : 87495-33-8

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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•Related Screening Libraries:

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View All Adrenergic Receptor Isoform Specific Products:

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α adrenergic receptor β adrenergic receptor

View All 5-HT Receptor Isoform Specific Products:

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5-HT Receptor 5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[2]^[1]

α2-adrenergic receptor

28 nM (Ki)

α1-adrenergic receptor

93 nM (Ki)

5-HT Receptor

In Vitro

Napamezole (hydrochloride) inhibits [³H]Clonidine binding to rat brain alpha-2 adrenergic receptors with a K_i of 28 nM and inhibits [³H]Prazosin binding to rat brain alpha-1 adrenergic receptors with a K_i of 93 nM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Napamezole (p.o.; s.c.) antagonizes clonidine-induced analgesia in mice, with an ED₅₀ of 36 mg/kg via intragastric administration and 3 mg/kg via subcutaneous injection, indicating that it exhibits in vivo α₂-adrenergic receptor blocking activity^[1].
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.

Molecular Weight

248.75

Formula

C₁₄H₁₇ClN₂

CAS No.

87495-33-8

Appearance

Solid

Color

Yellow to orange

SMILES

C1(CC2=CC3=C(CC2)C=CC=C3)=NCCN1.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.0201 mL	20.1005 mL	40.2010 mL
5 mM	0.8040 mL	4.0201 mL	8.0402 mL
10 mM	0.4020 mL	2.0101 mL	4.0201 mL

View the 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.

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.97%

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Data Sheet (274 KB) SDS (393 KB)

COA (249 KB)

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

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