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SR 57227A

Catalog No. T23394   CAS 77145-61-0
Synonyms: SR 57227 hydrochloride

SR 57227A (SR 57227 hydrochloride) is a potent, orally active and selective 5-HT3 receptor agonist. It with 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 or their membranes. Anti-depressant effects.

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SR 57227A Chemical Structure
SR 57227A, CAS 77145-61-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 31.00
2 mg In stock $ 44.00
5 mg In stock $ 72.00
10 mg In stock $ 113.00
25 mg In stock $ 213.00
50 mg In stock $ 369.00
100 mg In stock $ 549.00
500 mg In stock $ 1,190.00
1 mL * 10 mM (in DMSO) In stock $ 75.00
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Purity: 99.93%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SR 57227A (SR 57227 hydrochloride) is a potent, orally active and selective 5-HT3 receptor agonist. It with 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 or their membranes. Anti-depressant effects.
In vivo Seizure latency was significantly prolonged by a 5-HT3 receptor agonist SR 57227 in a dose-dependent manner.?Seizure score and mortality were also decreased by SR 57227 in PTZ-treated mice.?Furthermore, these anticonvulsant effects of SR 57227 were inhibited by a 5-HT3 receptor antagonist ondansetron.?However, ondansetron alone had no effect on seizure latency, seizure score or mortality at different doses.?Immunohistochemical studies have also shown that c-Fos expression was significantly increased in hippocampus (dentate gyrus, CA1, CA3 and CA4) of PTZ-treated mice.?Furthermore, c-Fos expression was significantly inhibited by ondansetron in mice treated with PTZ and SR 57227.?An ELISA study showed that SR 57227 attenuated the PTZ-induced inhibitory effects of GABA levels in hippocampus and cortex, and the attenuated effects of SR 57227 were antagonized by ondansetron in hippocampus but not cortex.?Activation of 5-HT3 receptor by SR 57227, which plays an important role on the control of seizure induced by PTZ, may be related to GABA activity in hippocampus.?Therefore, 5-HT3 receptor subtype is a potential target for the treatment of epilepsy[1].
Synonyms SR 57227 hydrochloride
Molecular Weight 248.15
Formula C10H14ClN3·HCl
CAS No. 77145-61-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 8.33 mg/mL (33.57 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Li B , Liang W , Sun Z , et al. The Anticonvulsant Effects of SR 57227 on Pentylenetetrazole-Induced Seizure in Mice[J]. Plos One, 2014, 9(4):e93158. 2. Li B , Shao D , Luo Y , et al. Role of 5-HT3 receptor on food intake in fed and fasted mice.[J]. Plos One, 2014, 10(3):e0121473.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library GPCR Compound Library Membrane Protein-targeted Compound Library Anti-Cancer Compound Library Bioactive Compound Library Angiogenesis related Compound Library Bioactive Compounds Library Max Orally Active Compound Library NO PAINS Compound Library CNS-Penetrant Compound Library

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Keywords

SR 57227A 77145-61-0 GPCR/G Protein Neuroscience 5-HT Receptor SR 57227 Hydrochloride immobility barrier Serotonin Receptor cell brain Inhibitor SR 57227 hydrochloride 5-hydroxytryptamine Receptor anti-depressant inhibit blood SR57227 Hydrochloride SR-57227 Hydrochloride NG 108-15 inhibitor

 

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