2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor 5-HT Receptor
  4. Napamezole (hydrochloride)

Napamezole hydrochloride 是一种口服有效的 α-2 肾上腺素能受体 (α2-adrenoceptor) 拮抗剂和 5-羟色胺 (5-HT Receptor) 再摄取抑制剂，对大鼠 α-2 和 α-1 肾上腺素能受体的 Ki 分别为 28 nM 和 93 nM。Napamezole hydrochloride 可用于研究抑郁症。

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Napamezole (hydrochloride)

Napamezole (hydrochloride) Chemical Structure

CAS No. : 87495-33-8

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规格 价格 是否有货 数量
5 mg ￥336
询价
10 mg ￥532
询价
25 mg ￥952
询价
50 mg ￥1512
询价
100 mg ￥2450
询价
200 mg   询价  
500 mg   询价  

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Napamezole (hydrochloride) 相关抗体

Top Publications Citing Use of Products

查看 Adrenergic Receptor 亚型特异性产品:

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α adrenergic receptor β adrenergic receptor

查看 5-HT Receptor 亚型特异性产品:

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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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1][2].

IC50 & Target[2][1]

α2-adrenergic receptor

28 nM (Ki)

α1-adrenergic receptor

93 nM (Ki)

5-HT Receptor

 

体外研究
(In Vitro)

Napamezole (hydrochloride) 可抑制 [3H]Clonidine 与大鼠脑 α-2 肾上腺素能受体的结合，其 Ki 为 28 nM；还可抑制 [3H]Prazosin 与大鼠脑 α-1 肾上腺素能受体的结合，其 Ki 为 93 nM[2]。

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

Napamezole (hydrochloride) 相关抗体:
体内研究
(In Vivo)

Napamezole (口服；皮下注射) 可拮抗可乐定诱导的小鼠镇痛作用，其口服给药的 ED50 为 36 mg/kg，皮下注射给药的 ED50 为 3 mg/kg，表明其具有体内 α-2 肾上腺素能受体阻断活性[1]。
Napamezole (30 mg/kg；口服) 可增强大鼠脑内去甲肾上腺素的转换率，证实了其体内 α-2 肾上腺素能受体阻断活性[1]。
Napamezole (≥ 1 mg/kg，静脉注射) 可增强大鼠蓝斑神经元的放电活动，还能逆转 Clonidine 对该放电活动的抑制效应，表明其具有体内 α2 肾上腺素能受体阻断活性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

248.75

Formula

C14H17ClN2
CAS 号
性状

固体

颜色

Yellow to orange

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, stored under nitrogen

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

纯度 & 产品资料
参考文献

Napamezole (hydrochloride) 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Napamezole (hydrochloride)87495-33-8Adrenergic Receptor5-HT ReceptorBeta ReceptorSerotonin Receptor5-hydroxytryptamine Receptorrat alpha-1 adrenergic receptorrat vas deferensrat brain alpha-2 adrenergic receptorlocus coeruleus neuronal firingalpha-2 adrenergic receptornorepinephrine turnover5-hydroxytryptamine re-uptake inhibitorrat alpha-2 adrenergic receptormonoamine re-uptakeantinociceptionInhibitorinhibitorinhibit

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