SR 57227 hydrochloride
Modify Date: 2024-01-31 11:18:54
SR 57227 hydrochloride structure
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Common Name | SR 57227 hydrochloride | ||
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| CAS Number | 77145-61-0 | Molecular Weight | 248.15200 | |
| Density | N/A | Boiling Point | 367.6ºC at 760 mmHg | |
| Molecular Formula | C10H15Cl2N3 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 176.1ºC | |
| Symbol |
GHS06 |
Signal Word | Danger | |
Use of SR 57227 hydrochlorideSR 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]. |
| Name | 1-(6-chloropyridin-2-yl)piperidin-4-amine,hydrochloride |
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| Synonym | More Synonyms |
| 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]. |
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| Related Catalog | |
| 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]. |
| References |
| Boiling Point | 367.6ºC at 760 mmHg |
|---|---|
| Molecular Formula | C10H15Cl2N3 |
| Molecular Weight | 248.15200 |
| Flash Point | 176.1ºC |
| Exact Mass | 247.06400 |
| PSA | 42.15000 |
| LogP | 3.22980 |
| Symbol |
GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H301-H315-H319-H335 |
| Precautionary Statements | P261-P301 + P310-P305 + P351 + P338 |
| Personal Protective Equipment | Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges |
| Hazard Codes | T |
| Risk Phrases | R25;R36/37/38 |
| Safety Phrases | S26;S45 |
| RIDADR | UN2811 6.1/PG 3 |
| RTECS | TM3465250 |
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The pyramidal neurons in the medial prefrontal cortex show decreased response to 5-hydroxytryptamine-3 receptor stimulation in a rodent model of Parkinson's disease.
Brain Res. 1384 , 69-79, (2011) In the present study, effect of SR 57227A, a selective 5-hydroxytryptamine-3 (5-HT(3)) receptor agonist, on the firing activity of pyramidal neurons in the medial prefrontal cortex (mPFC) was studied ... |
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Discriminative stimulus effects of 5.6 mg/kg pregnanolone in DBA/2J and C57BL/6J inbred mice.
Alcohol 37(1) , 35-45, (2005) Neurosteroids represent a class of endogenous compounds that exert rapid, nongenomic effects through neurotransmitter receptor systems such as gamma-aminobutyric acid(A) (GABA(A)). Two neurosteroids, ... |
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SR 57227A: a potent and selective agonist at central and peripheral 5-HT3 receptors in vitro and in vivo.
Eur. J. Pharmacol. 237 , 299, (1993) SR 57227A (4-amino-(6-chloro-2-pyridyl)-1 piperidine hydrochloride) is a novel compound with high affinity and selectivity for the 5-HT3 receptor. The compound had affinities (IC50) varying between 2.... |
| MFCD01756430 |
| sr 57,227a |