Mecamylamine hydrochloride (Synonyms: Inversine) |
| Catalog No.GC10329 |
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.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| Synonyms | Inversine | ||
| Chemical Name | (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 | ||
| Formula | C11H21N.HCl | M.Wt | 203.75 |
| Solubility | ≥ 20.4mg/mL in Ethanol | Storage | Store at 2-8°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
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