| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
SR 57227A targets the serotonin 5-HT3 receptor. It is a potent and selective 5-HT3 receptor agonist. The compound shows 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. By activating 5-HT3 receptors, the compound enhances serotonin-mediated signaling, making it a valuable pharmacological tool for studying serotonergic pathways.
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| ln Vitro |
With an affinity (Ki) of 115 nM in rat cerebral cortex, 150 nM in NG 108-15 cell membranes, and 103 nM in the entire NG 108-15 cell, SR 57227A binds to 5-HT3 receptors tagged with [3H]S-zacopride[1].
In vitro, SR 57227A acts as a potent and selective 5-HT3 receptor agonist. Its activity is typically assessed by measuring its ability to induce ion flux or calcium influx in cells expressing 5-HT3 receptors. The compound shows affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites. It is an inhibitor of NMDA receptor-mediated responses in rat cortical pyramidal cells. Standard in vitro assays include receptor binding studies using radiolabeled ligands such as [3H]-GR65630 and functional assays measuring ion flux or calcium influx. |
| ln Vivo |
In the forced swimming test, SR 57227A (1–30 mg/kg; ip) reduces immobility time in a dose-dependent manner; its ED50 value is 14.2 mg/kg[2]. SR 57227A dose-dependently shortens the rats' period of immobility following intraperitoneal injection in the forced swimming test. Following oral dosing, SR 57227A is also active in both species (ED50=7.6 mg/kg ip in rats). In a mouse time-course investigation, SR 57227A (20 mg/kg po) has a noteworthy 6-hour duration of effect. In the final two days of the avoidance task, SR 57227A (1 and 3 mg/kg ip) decreases the elevation of escape failures in the learned helplessness paradigm in rats by 50–60%. It also lessens isolation-induced aggressivity in mice by 50–85%, an effect that is countered by Zacopride (1 mg/kg ip)[2].
In vivo, SR 57227A is orally active and has antidepressant effects. As a blood-brain barrier penetrant 5-HT3 receptor agonist, it is suitable for systemic administration in animal models. By activating 5-HT3 receptors, the compound enhances serotonin-mediated signaling, making it useful for studying mechanisms underlying mood regulation, nociception, emesis, and cognitive processes. However, comprehensive in vivo efficacy data from published literature are limited. |
| Enzyme Assay |
For non-cell-based receptor binding assays, SR 57227A can be evaluated using membrane preparations from rat cortical membranes or NG 108-15 cells. Radioligand binding displacement experiments are performed using a suitable radiolabeled ligand such as [3H]-GR65630. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand at room temperature for 60-90 minutes. Bound radioligand is separated from free by rapid filtration through glass fiber filters. Non-specific binding is determined in the presence of excess unlabeled MDL-72222. IC50 values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing 5-HT3 receptors (e.g., NG 108-15 cells) are cultured in appropriate media. For functional assays, calcium influx is measured using fluorescent calcium indicators such as Fluo-4 AM. Cells are loaded with the dye and treated with various concentrations of SR 57227A. Fluorescence intensity is measured using a fluorescence plate reader. The increase in calcium signal compared to control wells indicates agonist activity. EC50 values are calculated from dose-response curves. For NMDA receptor assays, patch-clamp electrophysiology is performed on rat cortical pyramidal cells to assess the compound's effects on NMDA receptor-mediated responses.
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| Animal Protocol |
For in vivo animal studies, SR 57227A can be administered to rodents via oral gavage or intraperitoneal injection. In models of depression (e.g., forced swim test, tail suspension test), behavioral responses are assessed following compound administration. In models of mood regulation, nociception, and emesis, appropriate behavioral and physiological parameters are evaluated. Dosing regimens vary depending on the specific model and desired exposure levels. Blood and tissue samples may be collected for pharmacokinetic analysis.
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| ADME/Pharmacokinetics |
SR 57227A has a molecular weight of 233.14 and a molecular formula of C10H13ClN2·HCl. It is a potent, orally active and selective 5-HT3 receptor agonist. The compound is supplied as a research-grade compound. It should be stored at -20°C for long-term stability. It is soluble in DMSO and can be formulated for both in vitro and in vivo administration. It is for research use only and is not intended for human consumption.
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| Toxicity/Toxicokinetics |
The toxicity profile of SR 57227A has not been extensively reported. As a 5-HT3 receptor agonist, potential adverse effects may include modulation of serotonergic signaling, which could affect gastrointestinal function, emesis, and mood. The compound is for research use only and is not intended for human consumption. Standard toxicological evaluation would include acute and repeated-dose toxicity studies.
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| References | |
| Additional Infomation |
SR 57227A (CAS 77145-61-0) is a potent, orally active and selective 5-HT3 receptor agonist with the ability to cross the blood-brain barrier. It 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. SR 57227A has antidepressant effects and is an inhibitor of NMDA receptor-mediated responses in rat cortical pyramidal cells. It is available for research purposes only.
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| Molecular Formula |
C10H15CL2N3
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| Molecular Weight |
248.15
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| Exact Mass |
247.064
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| CAS # |
77145-61-0
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| PubChem CID |
131746
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| Appearance |
Off-white to light yellow solid powder
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| Boiling Point |
367.6ºC at 760 mmHg
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| Flash Point |
176.1ºC
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| LogP |
3.229
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
15
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| Complexity |
180
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CN(CCC1N)C2=NC(=CC=C2)Cl.Cl
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| InChi Key |
FUMINTAAUJUVMP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H14ClN3.ClH/c11-9-2-1-3-10(13-9)14-6-4-8(12)5-7-14;/h1-3,8H,4-7,12H2;1H
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| Chemical Name |
1-(6-chloropyridin-2-yl)piperidin-4-amine;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: 33.33 mg/mL (134.31 mM)
DMSO: 8.33 mg/mL (33.57 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (40.30 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0298 mL | 20.1491 mL | 40.2982 mL | |
| 5 mM | 0.8060 mL | 4.0298 mL | 8.0596 mL | |
| 10 mM | 0.4030 mL | 2.0149 mL | 4.0298 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.
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