Mecamylamine hydrochloride 是一种具有口服活性，非选择性，非竞争性的nAChR拮抗剂。Mecamylamine hydrochloride 也是一种神经节阻滞剂，可穿过血脑屏障。Mecamylamine hydrochloride 可用于神经疾病，高血压，抗抑郁的研究。
| 生物活性 | Mecamylamine hydrochloride is an orally active, nonselective, noncompetitivenAChRantagonist. Mecamylamine hydrochloride is also a ganglionic blocker. Mecamylamine hydrochloride can across the blood-brain barrier. Mecamylamine hydrochloride can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area[1][2][5]. |
| IC50& Target | nAChR[1], histamine receptor[2] |
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].
Western Blot Analysis[3] | Cell Line: | SCG neurons | | Concentration: | 10 μM | | Incubation Time: | 48 h | | Result: | Reduced the nicotine-facilitated increase in ERK1/2. |
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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].
| 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 100 mg/mL(490.80 mM;Need ultrasonic) DMSO : 31.25 mg/mL(153.37 mM;Need ultrasonic) 配制储备液 | 1 mM | 4.9080 mL | 24.5399 mL | 49.0798 mL | | 5 mM | 0.9816 mL | 4.9080 mL | 9.8160 mL | | 10 mM | 0.4908 mL | 2.4540 mL | 4.9080 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (10.21 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (10.21 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (10.21 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (10.21 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (10.21 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (10.21 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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