PeptideDB

Pozanicline dihydrochloride

CAS: 161416-61-1 F: C11H18Cl2N2O W: 265.18

Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR)
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Bioactivity 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].
Invitro 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].
In Vivo Pozanicline (ABT-089; 0.3 mg/kg and 0.6 mg/kg) reverses nicotine withdrawal-induced deficits in contextual fear conditioning[3]. Animal Model:
Name Pozanicline dihydrochloride
CAS 161416-61-1
Formula C11H18Cl2N2O
Molar Mass 265.18
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Reference [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.