1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. nAChR
  3. (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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form ((S)-UFR2709 hydrochloride) usually boasts enhanced water solubility and stability.

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(S)-UFR2709

(S)-UFR2709 Estructura química

No. CAS : 1431628-22-6

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Descripciòn

(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].

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

(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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Peso molecular

219.28

Fòrmula

C13H17NO2

No. CAS
SMILES

O=C(C1=CC=CC=C1)OC[C@H](CCC2)N2C

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

Nombre del producto:
(S)-UFR2709
Cat. No.:
HY-137231A
Cantidad:
MCE Japan Authorized Agent: