Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a K i of 16.7 nM for binding to [H]cytisine sites. Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a K i of 17 nM while binding to α7 nAChR is insignificant.
性状
Solid
体外研究(In Vitro)
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. Pozanicline (ABT-089) shows high selectivity for α6β2 and α4α5β2 nAChR subtypes. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Pozanicline (ABT-089; 0.3 mg/kg and 0.6 mg/kg) reverses nicotine withdrawal-induced deficits in contextual fear conditioning. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Adult m
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: H2O : 100 mg/mL (377.10 mM; Need ultrasonic)配制储备液