α7-containing neuronal nicotinic receptors antagonist
CAS：351344-10-0
分子式：C37H50N2O10.C6H8O7
分子量：874.93
纯度：98%
存储：Store at -20°C

Background:

Methyllycaconitine (MLA) is an antagonist of α7-containing neuronal nicotinic acetylcholine receptors (nAChRs; Ki = 1.4 nM).[1],[2] It is less effective at other nAChRs.[3],[4] MLA is used to selectively evaluate the role of α7-containing nAChRs in signaling pathways.[5],[6]
Reference:
[1]. Kalappa, B.I., Sun, F., Johnson, S.R., et al. A positive allosteric modulator of α7 nAChRs augments neuroprotective effects of endogenous nicotinic agonists in cerebral ischaemia. Brit.J.Pharmacol. 169, 1862-1878 (2013).
[2]. Ward, J.M., Cockcroft, V.B., Lunt, G.G., et al. Methyllycaconitine: A selective probe for neuronal α-bungarotoxin binding sites. FEBS Lett. 270(1-2), 45-48 (1990).
[3]. Eaton, J.B., Peng, J.H., Schroeder, K.M., et al. Characterization of human α4β 2-nicotinic acetylcholine receptors stably and heterologously expressed in native nicotinic receptor-null SH-EP1 human epithelial cells. Mol. Pharmacol. 64(6), 1283-1294 (2003).
[4]. Grinevich, V.P., Letchworth, S.R., Lindenberger, K.A., et al. Heterologous expression of human α6β4β3α5 nicotinic acetylcholine receptors: Binding properties consistent with their natural expression require quaternary subunit assembly including the α5 subunit. J. Pharm. Exp. Ther. 312(2), 619-626 (2005).
[5]. Fan, B.-S., Zhang, E.-H., Wu, M., et al. Activation of α7 nicotinic acetylcholine receptor decreases on-site mortality in crush syndrome through insulin signaling-Na/K-ATPase pathway. Front. Pharmacol. 7, 79 (2016).
[6]. Liu, L., Yu, J., Zhang, B., et al. Alpha7 nicotinic acetylcholine receptor is required for amyloid pathology in brain endothelial cells induced by Glycoprotein 120, methamphetamine and nicotine. Sci. Rep. 7, 40467 (2017).