SR 57227A
Based on 1 publication(s) in Google Scholar
SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.
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- Pureza: 99.86%
- No. CAS: 77145-61-0
- Fòrmula: C10H15Cl2N3
- Peso molecular:248.15
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) SR 57227A
MoreVer todos los productos específicos de isoformas 5-HT Receptor
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Actividad biológica
SR 57227A binds to 5-HT3 receptors labelled with [3H]S-zacopride with an affinity (Ki) of 115 nM in rat cerebral cortex, 150 nM in NG 108-15 cell membranes and 103 nM in whole NG 108-15 cell[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In the forced swimming test, SR 57227A dose-dependently reduces the duration of immobility in rats after i.p. administration. (ED50=7.6 mg/kg i.p. in rats.) SR 57227A is also active in both species after oral administration. In a time-course study in mice, SR 57227A (20 mg/kg p.o.) produces a significant effect lasting 6 hours. SR 57227A (1 and 3 mg/kg i.p.) reduces the elevation of the escape failures in the learned helplessness model in rats by 50-60% on the last two days of the avoidance task, and reduces isolation-induced aggressivity in mice by 50 to 85%, an effect which is antagonised by Zacopride (1 mg/kg i.p.)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 77145-61-0
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Appearance Solid
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Peso molecular 248.15
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Fòrmula C10H15Cl2N3
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Color Off-white to light yellow
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SMILES
ClC1=NC(N2CCC(N)CC2)=CC=C1.[H]Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
Disfunction of dorsal raphe nucleus-hippocampus serotonergic-HTR3 transmission results in anxiety phenotype of Neuroplastin 65-deficient mice. [Abstract]2024 Jul;45(7):1393-1405. PMID: 38528118
Solvente y solubilidad
H2O : 33.33 mg/mL (134.31 mM; Need ultrasonic)
DMSO : 8.33 mg/mL (33.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 10 mg/mL (40.30 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Poncelet M, et al, Le Fur G. Antidepressant-like effects of SR 57227A, a 5-HT3 receptor agonist, in rodents. J Neural Transm Gen Sect. 1995;102(2):83‐90. [Content Brief]
[2]. Bachy A, et al. SR 57227A: a potent and selective agonist at central and peripheral 5-HT3 receptors in vitro and in vivo. Eur J Pharmacol. 1993;237(2-3):299‐309. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 4.0298 mL | 20.1491 mL | 40.2982 mL | 100.7455 mL |
| 5 mM | 0.8060 mL | 4.0298 mL | 8.0596 mL | 20.1491 mL | |
| 10 mM | 0.4030 mL | 2.0149 mL | 4.0298 mL | 10.0746 mL | |
| 15 mM | 0.2687 mL | 1.3433 mL | 2.6865 mL | 6.7164 mL | |
| 20 mM | 0.2015 mL | 1.0075 mL | 2.0149 mL | 5.0373 mL | |
| 25 mM | 0.1612 mL | 0.8060 mL | 1.6119 mL | 4.0298 mL | |
| 30 mM | 0.1343 mL | 0.6716 mL | 1.3433 mL | 3.3582 mL | |
| H2O | 40 mM | 0.1007 mL | 0.5037 mL | 1.0075 mL | 2.5186 mL |
| 50 mM | 0.0806 mL | 0.4030 mL | 0.8060 mL | 2.0149 mL | |
| 60 mM | 0.0672 mL | 0.3358 mL | 0.6716 mL | 1.6791 mL | |
| 80 mM | 0.0504 mL | 0.2519 mL | 0.5037 mL | 1.2593 mL | |
| 100 mM | 0.0403 mL | 0.2015 mL | 0.4030 mL | 1.0075 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
SR 57227A Related Classifications
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