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Pozanicline dihydrochloride

Catalog No. T12525 CAS 161416-61-1

Synonyms: ABT-089 dihydrochloride

Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable agonist of nicotinic acetylcholine receptor (nAChR) (Ki = 16.7 nM)

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Pozanicline dihydrochloride Chemical Structure

Pozanicline dihydrochloride, CAS 161416-61-1

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable agonist of nicotinic acetylcholine receptor (nAChR) (Ki = 16.7 nM)
Targets&IC50	α4β2 nAChR:17 nM(Ki,rat brain), nAChR:16.7 nM(Ki), α6β2 nAChR:0.11 μM(EC50)
In vitro	Pozanicline is a partial agonist at α4β2 nAChR. Moreover, one α6β2 nAChR subtype is particularly sensitive to Pozanicline (EC50 of 0.11 μM)[2]. Pozanicline shows high selectivity for α6β2 and α4α5β2 nAChR subtypes[3].
In vivo	ABT-089, a partial agonist of α4β2*, and ABT-107, an α7 nicotinic acetylcholine receptor agonist, for amelioration of cognitive deficits induced by withdrawal from chronic nicotine in mice.?Mice underwent chronic nicotine administration (12.6 mg/kg/day or saline for 12 days), followed by 24 h of withdrawal.?At the end of withdrawal, mice received 0.3 or 0.6 mg/kg ABT-089 or 0.3 mg/kg ABT-107 (doses were determined through initial dose-response experiments and prior studies) and were trained and tested for CFC.?Nicotine withdrawal produced deficits in CFC that were reversed by acute ABT-089, but not ABT-107.?Cued conditioning was not affected.?modulation of hippocampal learning and memory using ABT-089 may be an effective component of novel therapeutic strategies for nicotine addiction[3].

Synonyms	ABT-089 dihydrochloride
Molecular Weight	265.18
Formula	C11H18Cl2N2O
CAS No.	161416-61-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 100 mg/mL (377.10 mM)

References and Literature

1. 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. 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. 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.

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Keywords

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