Pozanicline dihydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Pozanicline diHClide 是一种口服生物可利用的烟碱型乙酰胆碱受体 (nAChR) 激动剂 (Ki = 16.7 nM)。

Pozanicline dihydrochloride is an orally bioavailable agonist of nicotinic acetylcholine receptor (nAChR) (Ki = 16.7 nM)(In Vitro):Pozanicline dihydrochloride is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR (Ki = 17 nM) while binding to α7 nAChR is insignificant. Moreover, one α6β2 nAChR subtype is particularly sensitive to Pozanicline dihydrochloride(EC50 = 0.11 μM).(In Vivo):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 Pozanicline dihydrochloride and were trained and tested for CFC.?Nicotine withdrawal produced deficits in CFC that were reversed by acute Pozanicline dihydrochloride.?Cued conditioning was not affected.?Modulation of hippocampal learning and memory using Pozanicline dihydrochloride may be an effective component of novel therapeutic strategies for nicotine addiction.

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.

Pozanicline (ABT-089; 0.3 mg/kg and 0.6 mg/kg) reverses nicotine withdrawal-induced deficits in contextual fear conditioning. Animal Model:Adult male C57BL6/J mice at 8-12 weeks of age.Dosage:0.3 mg/kg and 0.6 mg/kg Administration:Treated 5 min before training and testing for contextual fear conditioning Result:A dose of0.3 mg/kg and 0.6 mg/kg ameliorated nicotine withdrawal-induced cognitive deficits in contextual fear conditioning.

ABT-089 dihydrochloride

Cell Cycle/DNA Damage

AChR

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161416-61-1

265.18

C11H18Cl2N2O

>98% (HPLC)

In Vitro:?H2O : 100 mg/mL (377.10 mM)

Cl.Cl.Cc1ncccc1OC[C@@H]1CCCN1

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(-20℃)

With Ice Pack

≥ 2 years