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Pozanicline dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pozanicline dihydrochloride图片
CAS NO:161416-61-1
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Pozanicline dihydrochloride (ABT-089 dihydrochloride) 是一种具有口服活性的烟碱型乙酰胆碱受体 (nAChR) 激动剂,与 [3H] 胱氨酸位点结合,Ki 为 16.7 nM。Pozanicline dihydrochloride 是一种 α4β2 选择性 nAChR 激动剂,与大鼠脑 α4β2 nAChR 结合,Ki 为 17 nM,而与 α7nAChR 的结合力很弱。
Cas No.161416-61-1
别名ABT-089 dihydrochloride
Canonical SMILES[H]Cl.[H]Cl.CC(N=CC=C1)=C1OC[C@@H]2CCCN2
分子式C11H18Cl2N2O
分子量265.18
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [3H]cytisine sites[1]. Pozanicline 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].

Pozanicline (ABT-089) 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 (ABT-089) shows high selectivity for α6β2 and α4α5β2 nAChR subtypes[3].

Pozanicline (ABT-089; 0.3 mg/kg and 0.6 mg/kg) reverses nicotine withdrawal-induced deficits in contextual fear conditioning[3]. Animal Model: Adult male C57BL6/J mice at 8-12 weeks of age[3].

[1]. Lin NH, et al. Structure-activity studies on 2-methyl-3-(2(S)-pyrrolidinylmethoxy) pyridine (ABT-089): an orally bioavailable 3-pyridyl ether nicotinic acetylcholine receptor ligand with cognition-enhancing properties. J Med Chem. 1997 Jan 31;40(3):385-90. [2]. Marks MJ, et al. Selectivity of ABT-089 for α4β2 and α6β2 nicotinic acetylcholine receptors in brain. Biochem Pharmacol. 2009 Oct 1;78(7):795-802. [3]. Yildirim E, et al. ABT-089, but not ABT-107, ameliorates nicotine withdrawal-induced cognitive deficits in C57BL6/J mice. Behav Pharmacol. 2015 Apr;26(3):241-8.