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1431628-22-6

中文名稱 (S)-UFR2709
英文名稱 2-Pyrrolidinemethanol, 1-methyl-, 2-benzoate, (2S)-
CAS 1431628-22-6
分子式 C13H17NO2
分子量 219.28
MOL 文件 1431628-22-6.mol
1431628-22-6 結(jié)構(gòu)式 1431628-22-6 結(jié)構(gòu)式

基本信息

英文別名
(S)-UFR2709
2-Pyrrolidinemethanol, 1-methyl-, 2-benzoate, (2S)-
(2S)?-1-?Methyl-?2-?pyrrolidinemethanol 2-?Benzoate
Benzoic acid [(2S)-1-methylpyrrolidine-2-yl]methyl ester

物理化學(xué)性質(zhì)

沸點(diǎn)304.4±15.0 °C(Predicted)
密度1.079±0.06 g/cm3(Predicted)
酸度系數(shù)(pKa)9.47±0.40(Predicted)

常見問(wèn)題列表

生物活性
(S)-UFR2709 是一種競(jìng)爭(zhēng)性的 nAChR 拮抗劑,并顯示出較強(qiáng)的親和力,對(duì) α4β2 nAChR 的親和力比對(duì)α7 nAChR 的高。(S)-UFR2709 在偏好酒精的老鼠中減少焦慮,并且可以減少其酒精攝入和對(duì)酒精偏好。(S)-UFR2709 是抗焦慮試劑,可用于研究尼古丁成癮。
體外研究

Brain nicotinic acetylcholine receptors (nAChRs) is a heterogeneous family of pentameric acetylcholine-gated cation channels, which is a molecular target for the treatment of alcohol abuse and dependence.

體內(nèi)研究

(S)-UFR2709 (50-100 μg/ml; 3 min and then maintained for another 5 min in a holding tank before testing the swimming behaviour in the test tank for a period of 5 min) produces a decrease in the bottom dwelling for NTT test, and UFR2709 induces a significant and dose-dependent decrease in bottom dwelling time to 52.9 and 87.0 s, respectively at 50 and 100 μg/ml.(S)-UFR2709 (50-100 μg/ml) decreases nicotine-evoked mRNA expression of α4 nACh receptor subunit, but UFR2709 has less effect on α4 nACh receptor subunit in the brain of adult zebrafish.(S)-UFR2709 (intraperitoneal?injection; 1-10 mg/kg; daily; 17 days) reduces ethanol consumption and ethanol preference and increased water consumption in a dose-dependent manner. The most effective dose of UFR2709 is 2.5 mg/kg, it induces a 56% reduction in alcohol consumption.?(S)-UFR2709 does not affect the weight or locomotor activity of the rats.

Animal Model: High-alcohol-drinking UChB rats
Dosage: 10 mg/kg, 5 mg/kg, 2.5 mg/kg, or 1 mg/kg
Administration: Intraperitoneal?injection; 1-10 mg/kg; daily; 17 days
Result: Did not affect the weight or locomotor activity and reduced ethanol consumption and preference.
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