(±)-Epibatidine (hydrochloride)
An agonist of α4β2 subunit-containing nAChRs
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包装价格促销价数量
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1mg￥1337.001070.00- +
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5mg￥5012.004010.00- +
- 货号: ajcx20868
- CAS: 162885-01-0
- 别名: CMI 545 dihydrochloride
- 分子式: C11H13ClN2.2HCl
- 分子量: 281.6
- 纯度: ＞98%
- 溶解度: DMSO: soluble
- 储存: Store at -20°C
- 库存: 现货
Background
(±)-Epibatidine is an alkaloid that has been found in Ecuadoran poison frog (E. tricolor) skin extracts and an agonist of α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs; Ki = 43 pM).1,2 It is selective for α4β2 subunit-containing nAChRs over α7 nAChRs (Ki = 230 nM).1 (±)-Epibatidine enhances 86Rb+ flux in IMR-32 cells (EC50 = 7 nM) and induces dopamine release from rat striatal slices (EC50 = 0.4 nM), effects that can be reduced by the nAChR antagonist mecamylamine . In vivo, (±)-epibatidine induces analgesia in the hot plate test and the Straub-tail response in mice (ED50s = 0.005 and 0.02 mg/kg, respectively).2
1.Sullivan, J.P., Decker, M.W., Brioni, J.D., et al.(+/-)-Epibatidine elicits a diversity of in vitro and in vivo effects mediated by nicotinic acetylcholine receptorsJ. Pharmacol. Exp. Ther.271(2)624-631(1994) 2.Spande, T.F., Garraffo, H.M., Edwards, M.W., et al.Epibatidine: A novel (chloropyridyl)azabicycloheptane with potent analgesic activity from an Ecuadoran poison frogJ. Am. Chem. Soc.114(9)3475-3478(1992)
