生物活性 | (S)-UFR2709 (hydrochloride) is a competitivenAChRantagonist and displays higher affinity for α4β2nAChRs than for α7nAChRs. (S)-UFR2709 (hydrochloride) decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 (hydrochloride) acts as an anxiolytic agent and can be used for the study of nicotine addiction[1][2]. | ||||||||||||||||
体外研究 (In Vitro) | 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[1]. | ||||||||||||||||
体内研究 (In Vivo) | (S)-UFR2709 (hydrochloride) (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[2].(S)-UFR2709 (hydrochloride) (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[2].(S)-UFR2709 (hydrochloride) (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 (hydrochloride) does not affect the weight or locomotor activity of the rats[1].
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分子量 | 255.74 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C13H18ClNO2 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) | ||||||||||||||||
溶解性数据 | In Vitro: H2O : 100 mg/mL(391.02 mM;Need ultrasonic) DMSO : 50 mg/mL(195.51 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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