| Description |
(S)-UFR2709 is a competitive nAChR antagonist and displays higher affinity for α4β2 nAChRs than for α7 nAChRs. (S)-UFR2709 decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 acts as an anxiolytic agent and can be used for the study of nicotine addiction[1][2].
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| Related Catalog |
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| 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].
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| In Vivo |
(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[2]. (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[2]. (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[1]. Animal Model: High-alcohol-drinking UChB rats[1] 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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| References |
[1]. Gabriel Quiroz, et al. UFR2709, a Nicotinic Acetylcholine Receptor Antagonist, Decreases Ethanol Intake in Alcohol-Preferring Rats. Front Pharmacol. 2019 Dec 3;10:1429. [2]. Franco Viscarra, et al. Nicotinic Antagonist UFR2709 Inhibits Nicotine Reward and Decreases Anxiety in Zebrafish. Molecules. 2020 Jun 30;25(13):2998.
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