77145-61-0
77145-61-0 structure
- Name: SR 57227 hydrochloride
- Chemical Name: 1-(6-chloropyridin-2-yl)piperidin-4-amine,hydrochloride
- CAS Number: 77145-61-0
- Molecular Formula: C10H15Cl2N3
- Molecular Weight: 248.15200
- Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
- Create Date: 2018-12-10 11:55:17
- Modify Date: 2024-01-31 11:18:54
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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].
| Name | 1-(6-chloropyridin-2-yl)piperidin-4-amine,hydrochloride |
|---|---|
| Synonyms |
MFCD01756430
sr 57,227a |
| 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]. |
|---|---|
| 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 |