(S)-UFR2709
(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.
For research use only. We do not sell to patients.
- CAS No.: 1431628-22-6
- Formula: C13H17NO2
- Molecular Weight:219.28
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Oocyte | IC50 |
2.5 μM
Compound: 1
|
Antagonist activity at (alpha4beta2)2beta2 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay
Antagonist activity at (alpha4beta2)2beta2 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay
|
[PMID: 23561269] |
| Oocyte | IC50 |
313 μM
Compound: 1
|
Antagonist activity at (alpha4beta2)2alpha4 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay
Antagonist activity at (alpha4beta2)2alpha4 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay
|
[PMID: 23561269] |
| Oocyte | IC50 |
52.3 μM
Compound: 1
|
Antagonist activity at (alpha4beta2)2alpha5 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay
Antagonist activity at (alpha4beta2)2alpha5 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay
|
[PMID: 23561269] |
| SH-SY5Y | IC50 |
13.4 μM
Compound: 1
|
Displacement of [125I]alpha-bungarotoxin from human alpha7 nAChR overexpressed in human SH-SY5Y cells after 120 mins by liquid scintillation spectrometric analysis
Displacement of [125I]alpha-bungarotoxin from human alpha7 nAChR overexpressed in human SH-SY5Y cells after 120 mins by liquid scintillation spectrometric analysis
|
[PMID: 23561269] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:High-alcohol-drinking UChB rats[1]
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Dosage:10 mg/kg, 5 mg/kg, 2.5 mg/kg, or 1 mg/kg
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Administration:Intraperitoneal injection; 1-10 mg/kg; daily; 17 days
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Result:Did not affect the weight or locomotor activity and reduced ethanol consumption and preference.
Chemical Information
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CAS No. 1431628-22-6
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Molecular Weight 219.28
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Formula C13H17NO2
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SMILES
O=C(C1=CC=CC=C1)OC[C@H](CCC2)N2C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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. [Content Brief]
[2]. Franco Viscarra, et al. Nicotinic Antagonist UFR2709 Inhibits Nicotine Reward and Decreases Anxiety in Zebrafish. Molecules. 2020 Jun 30;25(13):2998. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)