Pozanicline hydrochloride 是一种口服生物可利用的烟碱乙酰胆碱受体 (nAChR) 激动剂,与 [3H] 金雀花碱位点结合的 Ki 值为 16.7 nM。它是一种 α4β2 选择性 nAChR 激动剂,可与大鼠脑 α4β2 nAChR 结合,Ki 为 17 nM,而与 α7 nAChR 的结合不显著。
产品描述
Pozanicline hydrochloride is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [3H]cytisine sites[1]. Pozanicline hydrochloride is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant[2].
体外活性
Pozanicline hydrochloride is a partial agonist at α4β2 nAChR. Moreover, one α6β2 nAChR subtype is particularly sensitive to Pozanicline with an EC50 of 0.11 μM[2]. Pozanicline hydrochloride shows high selectivity for α6β2 and α4α5β2 nAChR subtypes[3].
体内活性
Pozanicline hydrochloride (0.3 mg/kg and 0.6 mg/kg) reverses nicotine withdrawal-induced deficits in contextual fear conditioning[3].
Cas No.
T16563L
分子式
C11H17ClN2O
分子量
228.72
别名
Pozanicline hydrochloride
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years