SR 57227A hydrochloride - CAS 77145-61-0
Category: Inhibitor
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5-HT Receptor
SR 57227 hydrochloride is a selective and high affinity 5-HT3 receptor agonist. SR 57227 exhibits anti-depressant like effects and decreases isolation-induced aggressive behavior in rat model.
Brife Description:
5-HT3 receptor agonist
≥99% by HPLC
Off-White to Pale Orange Solid
SR 57227A hydrochloride; SR57227A hydrochloride; SR-57227A hydrochloride; 1-(6-Chloro-2-pyridinyl)-4-piperidinamine hydrochloride; 4-amino-1-(6-chloro-2-pyridyl)-piperidine hydrochloride
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1.Bidirectional allosteric modulation of strychnine-sensitive glycine receptors by tropeines and 5-HT3 serotonin receptor ligands.
Maksay G Neuropharmacology. 1998 Dec;37(12):1633-41.
Specific binding of [3H]strychnine was studied on membranes prepared from rat spinal cord. Several antagonists and agonists of 5-HT3 receptors and tropane derivatives displaced [3H]strychnine binding with micromolar potencies. In the presence of 10 microM glycine a high affinity (nanomolar) component of displacement was also observed for the tropeines zatosetron, bemesetron and tropisetron. The displacing potency of glycine was also enhanced by these agents which are therefore termed glycine-positive. In contrast, atropine, SR 57227A, m-chlorophenylbiguanide, metoclopramide and granisetron are termed glycine-negative, because they decreased the displacing potency of glycine while glycine decreased the displacing potencies of atropine and metoclopramide. The dissociation of [3H]strychnine binding was accelerated in the presence of m-chlorophenylbiguanide, SR 57227A, atropine and zatosetron with a concentration dependence (EC50 values and Hill slopes) similar to their displacing effects. This demonstrates that the displacement of strychnine binding is associated with allosteric interactions between different binding sites. Structure-activity analysis revealed that the tropeine structure is essential for high affinity binding, and its substitutions (in scopolamine and cocaine) or its replacement (in ondansetron and metoclopramide) strongly decrease the potency and/or efficacy of allosteric modulation.
2.Contribution of Hippocampal 5-HT
Wu ZM;Yang LH;Cui R;Ni GL;Wu FT;Liang Y Cell Mol Neurobiol. 2017 May;37(4):595-606. doi: 10.1007/s10571-016-0395-7. Epub 2016 Jun 21.
One of the hypotheses about the pathogenesis of posttraumatic stress disorder (PTSD) is the dysfunction of serotonin (5-HT) neurotransmission. While certain 5-HT receptor subtypes are likely critical for the symptoms of PTSD, few studies have examined the role of 5-HT;3; receptor in the development of PTSD, even though 5-HT;3; receptor is critical for contextual fear extinction and anxiety-like behavior. Therefore, we hypothesized that stimulation of 5-HT;3; receptor in the dorsal hippocampus (DH) could prevent hippocampal autophagy and the development of PTSD-like behavior in animals. To this end, we infused SR57227, selective 5-HT;3; agonist, into the DH after a single prolonged stress (SPS) treatment in rats. Three weeks later, we evaluated the effects of this pharmacological treatment on anxiety-related behaviors and extinction of contextual fear memory. We also accessed hippocampal autophagy and the expression of 5-HT;3A; subunit, Beclin-1, LC3-I, and LC3-II in the DH. We found that SPS treatment did not alter anxiety-related behaviors but prolonged the extinction of contextual fear memory, and such a behavioral phenomenon was correlated with increased hippocampal autophagy, decreased 5-HT;3A; expression, and increased expression of Beclin-1 and LC3-II/LC3-I ratio in the DH.
3.Serotonin3 receptor agonists attenuate glutamate-induced firing in rat hippocampal CA1 pyramidal cells.
Zhang JY;Zeise ML;Wang RY Neuropharmacology. 1994 Mar-Apr;33(3-4):483-91.
The techniques of extracellular single cell recording and microiontophoresis were used to study the effect of 5-HT3 receptor agonists on glutamate-activated firing of CA1 hippocampal pyramidal cells. Iontophoretic application of 5-HT3 receptor agonists 2-methyl-5-HT and SR 57227A produced a current (dose)-dependent suppression of the firing of CA1 pyramidal cells; SR 57227A was more effective than 2-methyl-5-HT. The suppressant action of 2-methyl-5-HT and SR 57227A had a slow onset and showed little or no desensitization. This effect was markedly attenuated or completely blocked by the 5-HT3 receptor antagonist BRL 46470A but not by the nonspecific 5-HT1 and 5-HT2 receptor antagonist metergoline or by the 5-HT1A antagonist WAY 100478. Intravenous administration of SR 57227A was effective in reducing the firing rate of CA1 pyramidal cells and this effect was prevented by BRL 46470A administered either i.v. or iontophoretically. Iontophoresis of 2-methyl-5-HT also diminished CA1 postsynaptic field potentials evoked by electrical stimulation of the Schaffer collaterals. Again, BRL 46470A but not metergoline prevented the suppressant action of 2-methyl-5-HT. Taken together, our results indicate that activation of 5-HT3-like receptors in the hippocampal CA1 region effectively reduces the efficacy of glutamatergic neurotransmission.
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CAS 77145-61-0 SR 57227A hydrochloride

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