产品描述
(S)-UFR2709 (hydrochloride) is a competitive nAChR antagonist and displays higher affinity for α4β2 nAChRs than for α7 nAChRs. (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].
体外活性
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].
体内活性
(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]. Animal Model: High-alcohol-drinking UChB rats[1]
别名
(S)-UFR2709 hydrochloride;(S)-UFR2709 hydrochloride
储存和溶解度
DMSO:50 mg/mL (195.51 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years