1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. SR 57227A

SR 57227A 

Cat. No.: HY-102064
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5-HT3 receptor

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.

For research use only. We do not sell to patients.

SR 57227A Chemical Structure

SR 57227A Chemical Structure

CAS No. : 77145-61-0

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Description

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[1][2].

In Vitro

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].

In Vivo

SR 57227A (1-30 mg/kg; i.p.) dose-dependently reduces immobility time in the forced swimming test with an ED50 value for this effect of 14.2 mg/kg[2].
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].

Molecular Weight

248.15

Formula

C₁₀H₁₅Cl₂N₃

CAS No.

77145-61-0

SMILES

ClC1=NC(N2CCC(N)CC2)=CC=C1.[H]Cl

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Storage

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

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Keywords:

SR 57227A5-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorbloodbrainbarrieranti-depressantNG 108-15cellimmobilityInhibitorinhibitorinhibit

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SR 57227A
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