Pozanicline dihydrochloride (Synonyms: ABT-089 dihydrochloride)
目录号: PL07658 纯度: ≥97%
CAS No. :161416-61-1
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中文名称
Pozanicline dihydrochloride
中文别名
ABT 089 dihydrochloride
英文名称
Pozanicline dihydrochloride
英文别名
ABT 089 dihydrochloride;2-methyl-3-(2-(S)-pyrrolidinylmethoxy)pyridine dihydrochloride;Pozanicline dihydrochloride;Pozanicline (dihydrochloride);Pozanicline hydrochloride;(S)-3-(2-pyrrolidinylmethoxy)-2-picoline dihydrochloride;(S)-3-(2-pyrrolidinylmethoxy)-2-picoline 2HCl;2-Methyl-3-[(2S)-pyrrolidinylmethoxy]pyridine dihydrochloride;2-Methyl-3-[(2S)-2-pyrrolidinylmethoxy]-pyridineDihydrochloride;(S)-2-M;ABT-089 dihydrochloride
Cas No.
161416-61-1
分子式
C11H18Cl2N2O
分子量
265.18
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Pozanicline dihydrochloride (ABT-089 dihydrochloride) 是一种具有口服活性的烟碱型乙酰胆碱受体 (nAChR) 激动剂,与 [3H] 胱氨酸位点结合,Ki 为 16.7 nM。Pozanicline dihydrochloride 是一种 α4β2 选择性 nAChR 激动剂,与大鼠脑 α4β2 nAChR 结合,Ki 为 17 nM,而与 α7nAChR 的结合力很弱。
生物活性
Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a K i of 16.7 nM for binding to [H]cytisine sites. Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a K i of 17 nM while binding to α7 nAChR is insignificant.
性状
Solid
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Pozanicline (ABT-089; 0.3 mg/kg and 0.6 mg/kg) reverses nicotine withdrawal-induced deficits in contextual fear conditioning. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Adult m
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: H2O : 100 mg/mL (377.10 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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