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
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	Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
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	[1]. Poncelet M, et al, Le Fur G. Antidepressant-like effects of SR 57227A, a 5-HT3 receptor agonist, in rodents. J Neural Transm Gen Sect. 1995;102(2):83‐90. [2]. Bachy A, et al. SR 57227A: a potent and selective agonist at central and peripheral 5-HT3 receptors in vitro and in vivo. Eur J Pharmacol. 1993;237(2-3):299‐309.

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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