Pozanicline dihydrochloride 是口服有效的烟碱型乙酰胆碱受体激动剂，与 [3H] 胱氨酸位点结合，Ki为 16.7 nM，对 α4β2 nAChR 的选择性高于α7nAChR。

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

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].

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].

161416-61-1

C11H18Cl2N2O

265.18

ABT-089 dihydrochloride

H2O:100 mg/mL (377.10 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years