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ln Vitro |
A molecular target for the treatment of alcohol misuse and dependence is the brain's nicotinic acetylcholine receptors (nAChRs), a diverse family of pentameric acetylcholine-gated cation channels[1].
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ln Vivo |
UFR2709 significantly and dose-dependently reduces bottom dwelling time to 52.9 and 87.0 s, respectively, at 50 and 100 μg/ml. (S)-UFR2709 (50-100 μg/ml; 3 min and then maintained for another 5 min in a holding tank before testing the swimming behavior in the test tank for a period of 5 min) also results in a decrease in bottom dwelling for the NTT test[2]. (S)-UFR2709 (50-100 μg/ml) reduces the α4 nACh receptor subunit's nicotine-evoked mRNA expression; however, UFR2709 has less of an impact on the subunit in the adult zebrafish brain[2]. In a dose-dependent manner, (S)-UFR2709 (intraperitoneal injection; 1–10 mg/kg; daily; 17 days) decreases ethanol consumption and preference while increasing water consumption. UFR2709's most potent dosage is 2.5 mg/kg, which results in a 56% decrease in alcohol intake. The rats' weight and level of locomotor activity are unaffected by (S)-UFR2709[1].
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Animal Protocol |
Animal/Disease Models: High-alcohol-drinking UChB rats[1]
Doses: 10 mg/kg, 5 mg/kg, 2.5 mg/kg, or 1 mg/kg Route of Administration: intraperitoneal (ip) injection; 1-10 mg/kg; daily; 17 days Experimental Results: Did not affect the weight or locomotor activity and decreased 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.
[2]. Franco Viscarra, et al. Nicotinic Antagonist UFR2709 Inhibits Nicotine Reward and Decreases Anxiety in Zebrafish. Molecules. 2020 Jun 30;25(13):2998. |
Molecular Formula |
C13H17NO2
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Molecular Weight |
219.28
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CAS # |
1431628-22-6
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Related CAS # |
(S)-UFR2709 hydrochloride;2934318-93-9
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SMILES |
O(C(C1C=CC=CC=1)=O)C[C@@H]1CCCN1C
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.5604 mL | 22.8019 mL | 45.6038 mL | |
5 mM | 0.9121 mL | 4.5604 mL | 9.1208 mL | |
10 mM | 0.4560 mL | 2.2802 mL | 4.5604 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.