Description
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. 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.
Product information
CAS Number: 161416-61-1
Molecular Weight: 265.18
Formula: C11H18Cl2N2O
Synonym:
ABT-089 dihydrochloride
Chemical Name: 2-methyl-3-{[(2S)-pyrrolidin-2-yl]methoxy}pyridine; bis(chlorohydrogen)
Smiles: Cl.Cl.CC1=NC=CC=C1OC[C@@H]1CCCN1
InChiKey: UGVSESCRKJTJAK-XRIOVQLTSA-N
InChi: InChI=1S/C11H16N2O.2ClH/c1-9-11(5-3-6-12-9)14-8-10-4-2-7-13-10;;/h3,5-6,10,13H,2,4,7-8H2,1H3;2*1H/t10-;;/m0../s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
In Vivo:
Pozanicline (ABT-089; 0.3 mg/kg and 0.6 mg/kg) reverses nicotine withdrawal-induced deficits in contextual fear conditioning.
References:
- 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.
- 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.
- 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.
Products are for research use only. Not for human use.
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