161416-61-1
中文名稱
Pyridine, 2-methyl-3-[(2S)-2-pyrrolidinylmethoxy]-, dihydrochloride
英文名稱
Pyridine, 2-methyl-3-[(2S)-2-pyrrolidinylmethoxy]-, dihydrochloride
CAS
161416-61-1
分子式
C11H16N2O.2ClH
分子量
265.179
MOL 文件
161416-61-1.mol
更新日期
2023/03/20 15:41:23
161416-61-1 結(jié)構(gòu)式
基本信息
中文別名
POZANICLINE DIHYDROCHLORIDE 英文別名
ABT 089 dihydrochloridePozanicline dihydrochloride
ABT 089 dihydrochloride (ABT089
2-Methyl-3-[(2S)-pyrrolidinylmethoxy]pyridine dihydrochloride
Pyridine, 2-methyl-3-[(2S)-2-pyrrolidinylmethoxy]-, dihydrochloride
物理化學(xué)性質(zhì)
儲(chǔ)存條件2-8°C
溶解度溶于二甲基亞砜
形態(tài)粉末
顏色白色至米色
旋光性 (optical activity)[α]/D +20 to +30°, c = 1 in methanol
常見(jiàn)問(wèn)題列表
生物活性
Pozanicline dihydrochloride (ABT-089 dihydrochloride) 是一種具有口服活性的煙堿型乙酰膽堿受體 (nAChR) 激動(dòng)劑，與 [3H] 胱氨酸位點(diǎn)結(jié)合，Ki 為 16.7 nM。Pozanicline dihydrochloride 是一種 α4β2 選擇性 nAChR 激動(dòng)劑，與大鼠腦 α4β2 nAChR 結(jié)合，Ki 為 17 nM，而與 α7nAChR 的結(jié)合力很弱。體外研究
Pozanicline (ABT-089) is a partial agonist at α4β2 nAChR. Moreover, one α6β2 nAChR subtype is particularly sensitive to Pozanicline with an EC
50
of 0.11 μM.
Pozanicline (ABT-089) shows high selectivity for α6β2 and α4α5β2 nAChR subtypes.
體內(nèi)研究
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 of 0.3 mg/kg and 0.6 mg/kg ameliorated nicotine withdrawal-induced cognitive deficits in contextual fear conditioning. |