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。
| 生物活性 | Mecamylamine is an orally active, nonselective, noncompetitivenAChRantagonist. 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] |
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 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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