Mecamylamine hydrochloride
(Synonyms: 盐酸美加明) 目录号 : GC10329
Mecamylamine hydrochloride是一种非选择性、非竞争性的烟碱型乙酰胆碱受体（nAChR）拮抗剂，能够阻断多种不同的nAChR亚型，如α3β4、α4β2、α3β2，其IC50值分别为640nM、2.5µM、3.6µM。
Cas No.:826-39-1
Sample solution is provided at 25 µL, 10mM.
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Mecamylamine hydrochloride is a non-selective, non-competitive nicotinic acetylcholine receptor (nAChR) antagonist that can block various nAChR subtypes, such as α3β4, α4β2, and α3β2 receptors, with IC50 values of 640nM, 2.5µM, and 3.6µM respectively[1]. Mecamylamine hydrochloride can inhibit acetylcholine in autonomic ganglia, thereby reducing blood pressure[2], and also has antidepressant functions[3]. Mecamylamine hydrochloride can also improve symptoms of diabetes[4].
In vitro, pre-treatment of SH-SY5Y neuroblastoma cells with Mecamylamine hydrochloride (10µM) for 1h, followed by stimulation with Nicotine (100µM) for 48h, significantly inhibited nicotine-induced cell proliferation and blocked the increase in BDNF secretion and TrkB receptor surface density induced by Nicotine[5]. Pre-treatment of GLC-8 small cell lung cancer cells with Mecamylamine hydrochloride (1µM) for 10min, followed by stimulation with Nicotine (100nM) for 5min, completely blocked the increase in nicotine-induced extracellular signal-regulated kinase (MAP kinase) activity[6].
In vivo, Mecamylamine hydrochloride (50mg/kg/day) was continuously administered via subcutaneously implanted osmotic pumps and used to treat mouse models of choroidal neovascularization for 2 weeks. Mecamylamine hydrochloride significantly inhibited Matrigel-induced and ocular endothelial cell tube formation in mice[7]. Pre-treatment of diabetic C57BL/6 mice with Mecamylamine hydrochloride (2mg/kg) via intraperitoneal injection for 3 weeks restored the mice's sensitivity to glucose and effectively reduced their hyperglycemia[8].
References:
[1] Kumar P, Scholze P, Fronius M, et al. Nicotine stimulates ion transport via metabotropic β4 subunit containing nicotinic ACh receptors. Br J Pharmacol. 2020 Dec;177(24):5595-5608.
[2] Shytle RD, Penny E, Silver AA, et al. Mecamylamine (Inversine): an old antihypertensive with new research directions. J Hum Hypertens. 2002 Jul;16(7):453-7.
[3] Lippiello PM, Beaver JS, Gatto GJ, et al. TC-5214 (S-(+)-mecamylamine): a neuronal nicotinic receptor modulator with antidepressant activity. CNS Neurosci Ther. 2008 Winter;14(4):266-77.
[4] Campochiaro PA, Shah SM, Hafiz G, et al. Topical mecamylamine for diabetic macular edema. Am J Ophthalmol. 2010 May;149(5):839-51.e1.
[5] Serres F, Carney SL. Nicotine regulates SH-SY5Y neuroblastoma cell proliferation through the release of brain-derived neurotrophic factor. Brain Res. 2006 Jul 26;1101(1):36-42.
[6] Cattaneo MG, D'atri F, Vicentini LM. Mechanisms of mitogen-activated protein kinase activation by nicotine in small-cell lung carcinoma cells. Biochem J. 1997 Dec 1;328 ( Pt 2)(Pt 2):499-503.
[7] Kiuchi K, Matsuoka M, Wu JC, et al. Mecamylamine suppresses Basal and nicotine-stimulated choroidal neovascularization. Invest Ophthalmol Vis Sci. 2008 Apr;49(4):1705-11.
[8] Fernández-Cabezudo MJ, George JA, Bashir G, et al. Involvement of Acetylcholine Receptors in Cholinergic Pathway-Mediated Protection Against Autoimmune Diabetes. Front Immunol. 2019 May 15;10:1038.
Mecamylamine hydrochloride是一种非选择性、非竞争性的烟碱型乙酰胆碱受体（nAChR）拮抗剂，能够阻断多种不同的nAChR亚型，如α3β4、α4β2、α3β2，其IC50值分别为640nM、2.5µM、3.6µM[1]。Mecamylamine hydrochloride可以抑制自主神经节中的乙酰胆碱，从而降低血压[2]，以及发挥抗抑郁的功能[3]。Mecamylamine hydrochloride还可改善糖尿病的症状[4]。
在体外，Mecamylamine hydrochloride（10μM）预处理SH-SY5Y神经母细胞瘤细胞1h，随后以尼古丁（100μM）刺激48 h，Mecamylamine hydrochloride显著抑制尼古丁诱导的细胞增殖，同时阻断尼古丁对BDNF分泌和TrkB受体细胞表面密度的增加[5]。Mecamylamine hydrochloride（1μM）预处理GLC-8小细胞肺癌细胞10min，随后以尼古丁（100nM）刺激5min，Mecamylamine hydrochloride完全阻断尼古丁诱导的细胞外信号调节激酶（MAP激酶）活性的增加[6]。
在体内，Mecamylamine hydrochloride（50mg/kg/天）通过皮下植入的渗透泵持续给药，用于处理脉络膜新生血管形成的小鼠模型2周。Mecamylamine hydrochloride显著抑制了小鼠的基质胶和眼内皮细胞管形成[7]。Mecamylamine hydrochloride（2mg/kg）通过腹腔注射预处理糖尿病C57BL/6小鼠3周后，Mecamylamine hydrochloride恢复了小鼠对于葡萄糖的敏感性，并且可有效降低小鼠的高血糖[8]。
| Cell experiment [1]: | |
Cell lines | SH-SY5Y neuroblastoma cells (human neuronal cell line) |
Preparation Method | SH-SY5Y cells were grown in a 1:1 mixture of Eagle's minimal essential medium–F12 medium, containing fetal calf serum (10%), glutamine (2mM), penicillin (50U/ml), and streptomycin (50µg/ml) at 37°C, 5% CO₂. Cells were subcultured at a 1:10 ratio, left to attach for 2 days, and treated with retinoic acid (10µM) for an additional 5 days. Cells were preincubated for 1h with Mecamylamine hydrochloride (10µM) before the addition of Nicotine (100µM) for 48h. |
Reaction Conditions | 100μM; 48 hours |
Applications | Mecamylamine hydrochloride significantly prevented the enhanced [14C]-thymidine incorporation induced by Nicotine. Additionally, Mecamylamine hydrochloride prevented the Nicotine-induced increase in TrkB receptors on the SH-SY5Y cell surface. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | Mice were given nicotine in their drinking water (100µg/ml) and had implantation of an osmotic pump that released Mecamylamine hydrochloride (50mg/kg/day) subcutaneously. Mice were sacrificed 14 days after laser-induced rupture of Bruch's membrane for choroidal neovascularization (CNV) analysis. |
Dosage form | 50mg/kg/d; subcutaneous pump |
Applications | Mecamylamine hydrochloride blocked the nicotine-induced increase in CNV lesion size and suppressed CNV formation in the absence of nicotine. |
References: | |
| Cas No. | 826-39-1 | SDF | |
| 别名 | 盐酸美加明 | ||
| 化学名 | (1R,2S,4S)-N,2,3,3-tetramethylbicyclo[2.2.1]heptan-2-amine hydrochloride | ||
| Canonical SMILES | CC([C@@H]1C[C@H]2CC1)(C)[C@@]2(C)NC.Cl | ||
| 分子式 | C11H21N.HCl | 分子量 | 203.75 |
| 溶解度 | ≥ 20.4mg/mL in Ethanol | 储存条件 | Store at 2-8°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.908 mL | 24.5399 mL | 49.0798 mL |
| 5 mM | 981.6 μL | 4.908 mL | 9.816 mL |
| 10 mM | 490.8 μL | 2.454 mL | 4.908 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
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2.
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Quality Control & SDS
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- Purity: >98.00%
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