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(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]. | [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]. | 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. |
| [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. DOI:10.3389/fphar.2019.01429
[2] Franco Viscarra, et al. Nicotinic Antagonist UFR2709 Inhibits Nicotine Reward and Decreases Anxiety in Zebrafish. Molecules. 2020 Jun 30;25(13):2998. DOI:10.3390/molecules25132998 |
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