Bradanicline 是一种高度选择性的 α7 烟碱乙酰胆碱受体 (nAChR) 激动剂 (对人 α7 nAChR 的 EC50=17 nM; Ki= 1.4 nM)。Bradanicline 可用于研究认知障碍。
货号:ajcx36894
CAS:639489-84-2
分子式:C22H23N3O2
分子量：361.44
溶解度:DMSO : 25 mg/mL (69.17 mM; ultrasonic and warming and heat to 60°C)
纯度：98%
存储：Store at -20°C
库存： 现货

Background:

Bradanicline is a highly selective α7 nicotinic acetylcholine receptor (nAChR) agonist (humanα7 nAChR: EC50=17 nM; Ki= 1.4 nM). Bradanicline is used for the research of cognitive disorders[1][2].

Bradanicline is more than a thousand-fold separation between the affinities for the α7 and α4β2 receptor subtypes and has no detectable effects on muscle or ganglionic nicotinic receptor subtypes, indicating a marked selectivity for the central nervous system over the peripheral nervous system[1].

Bradanicline (0.1-1 mg/kg) shows efficacy in animal models of the positive and negative symptoms and cognitive dysfunction of schizophrenia[2].

[1]. Mazurov AA, et al. Discovery of (2S,3R)-N-[2-(pyridin-3-ylmethyl)-1-azabicyclo[2.2.2]oct-3-yl]benzo[b]furan-2-carboxamide (TC-5619), a selective α7 nicotinic acetylcholine receptor agonist, for the treatment of cognitive disorders. J Med Chem. 2012;55(22):9793-9809. [2]. Hauser TA, et al. TC-5619: an alpha7 neuronal nicotinic receptor-selective agonist that demonstrates efficacy in animal models of the positive and negative symptoms and cognitive dysfunction of schizophrenia. Biochem Pharmacol. 2009;78(7):803-812.