2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein Immunology/Inflammation
  3. nAChR Histamine Receptor
  4. Mecamylamine

Mecamylamine 是一种具有口服活性，非选择性，非竞争性的 nAChR 拮抗剂。Mecamylamine 也是一种神经节阻滞剂，可穿过血脑屏障。Mecamylamine 可用于神经疾病，高血压，抗抑郁的研究。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 Mecamylamine hydrochloride 通常具有更好的水溶性和稳定性。

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Mecamylamine

Mecamylamine Chemical Structure

CAS No. : 60-40-2

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Mecamylamine 的其他形式现货产品:

Customer Review

Other Forms of Mecamylamine:

Mecamylamine 相关抗体

Top Publications Citing Use of Products

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Mecamylamine is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine is also a ganglionic blocker. Mecamylamine can across the blood-brain barrier. Mecamylamine can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area[1][2][5].

IC50 & Target

nAChR[1], histamine receptor[2]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Oocyte IC50
1.8 μM
Compound: 5, mecamylamine
Ability to block activation of acetylcholine-stimulated currents in human alpha-7 homomers expressed in oocytes
Ability to block activation of acetylcholine-stimulated currents in human alpha-7 homomers expressed in oocytes
[PMID: 9435889]
PC-12 EC50
0.2 μM
Compound: 5, mecamylamine
Compound was evaluated for functional potency and efficacy at rat Nicotinic acetylcholine receptor in PC12 cells (ganglionic)
Compound was evaluated for functional potency and efficacy at rat Nicotinic acetylcholine receptor in PC12 cells (ganglionic)
[PMID: 9435889]
TE-671 EC50
30 μM
Compound: 5, mecamylamine
Compound was evaluated for functional potencies and efficacies at human muscle type Nicotinic acetylcholine receptor in TE671 cells
Compound was evaluated for functional potencies and efficacies at human muscle type Nicotinic acetylcholine receptor in TE671 cells
[PMID: 9435889]
体外研究
(In Vitro)

Mecamylamine (0.5-9 μM, bath administered) increases the firing frequency of identified 5-HT DRN (dorsal raphe nucleus) neurons[1].
Mecamylamine (0.5-9 μM, bath administered) increases the glutamatergic and decreases the GABAergic input of 5-HT DRN neurons[1].
Mecamylamine (1 mM, 5 min) blocks the histamine receptor and the histamine-induced contractions in helically cut strips of rabbit aorta[2].
Mecamylamine (10 μM,48 h) attenuates the effect of nicotine’s action of neuroprotection[3].
Mecamylamine (1-100 nM, 30 min) dose-dependently attenuates endothelial tube formation in HDMVECs[4].

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

Mecamylamine 相关抗体:

Western Blot Analysis[3]

Cell Line: SCG neurons
Concentration: 10 μM
Incubation Time: 48 h
Result: Reduced the nicotine-facilitated increase in ERK1/2.
体内研究
(In Vivo)

Mecamylamine (subcutaneous pumps, 50 mg/kg/day, 2 days) inhibits choroidal neovascularization (CNV) in CNV mice model[4].
Mecamylamine (intraperitoneal injection, 0.5-1 mg/kg) has antidepressant-like effects in both the TST (tail suspension test) and FST (forced swim test) in C57BL/6J mice, which are dependent on both β2 and α7 subunits[5].

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

Animal Model: Choroidal neovascularization (CNV) mice model[1]
Dosage: 50 mg/kg/day, 2 days
Administration: Subcutaneous pumps implanted beneath the skin of the back, 200 μL and mean pumping rate of 0.5 μL/h.
Result: Suppressed the development of CNV at Bruch’s membrane rupture sites in the absence of nicotine.
Animal Model: C57BL/6J mice[5]
Dosage: 0.5-1 mg/kg
Administration: Intraperitoneal injection
Result: Had no effect in β2 knockout mice and α7 knockout mice, but decreased immobility time in wildtype littermates in the FST.
Clinical Trial
分子量

167.29

Formula

C11H21N
CAS 号
性状

固体

颜色

White to off-white

中文名称

美加明
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料

纯度: ≥90.0%

COA (290 KB)

产品使用指南 (1538 KB)
参考文献

Mecamylamine 相关分类

  • 摩尔计算器

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The molarity calculator equation

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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:

Mecamylamine60-40-2美加明nAChRHistamine ReceptorNicotinic acetylcholine receptorsNeuropsychiatricganglionichypertensionblood-brain barriervoltage-dependentneuronantidepressantvascularizationCNVFSTTSTtail suspensionforced swimInhibitorinhibitorinhibit

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