(S)-UFR2709
- CAS号:1431628-22-6
- 英文名:2-Pyrrolidinemethanol, 1-methyl-, 2-benzoate, (2S)-
- 中文名:(S)-UFR2709
- CBNumber:CB08310530
- 分子式:C13H17NO2
- 分子量:219.28
- MOL File:1431628-22-6.mol
- 沸点 :304.4±15.0 °C(Predicted)
- 密度 :1.079±0.06 g/cm3(Predicted)
- 酸度系数(pKa) :9.47±0.40(Predicted)
(S)-UFR2709性质、用途与生产工艺
- 生物活性 (S)-UFR2709 是一种竞争性的 nAChR 拮抗剂，并显示出较强的亲和力，对 α4β2 nAChR 的亲和力比对α7 nAChR 的高。(S)-UFR2709 在偏好酒精的老鼠中减少焦虑，并且可以减少其酒精摄入和对酒精偏好。(S)-UFR2709 是抗焦虑试剂，可用于研究尼古丁成瘾。
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体外研究
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.
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体内研究
(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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