SR 57227A is an orally bioactive selective agonist of the 5-HT3 receptor that penetrates the BBB (blood-brain barrier). The affinity (IC50) of SR 57227A to the 5-HT3 receptor binding site on rat cortical membrane and whole NG 108-15 cells or their membranes is 2.8~250 nM. Has antidepressant effects.

Physicochemical Properties

Molecular Formula	C10H15CL2N3
Molecular Weight	248.15
Exact Mass	247.064
CAS #	77145-61-0
PubChem CID	131746
Appearance	Off-white to light yellow solid powder
Boiling Point	367.6ºC at 760 mmHg
Flash Point	176.1ºC
LogP	3.229
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	1
Heavy Atom Count	15
Complexity	180
Defined Atom Stereocenter Count	0
InChi Key	FUMINTAAUJUVMP-UHFFFAOYSA-N
InChi Code	InChI=1S/C10H14ClN3.ClH/c11-9-2-1-3-10(13-9)14-6-4-8(12)5-7-14;/h1-3,8H,4-7,12H2;1H
Chemical Name	1-(6-chloropyridin-2-yl)piperidin-4-amine;hydrochloride
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	With an affinity (Ki) of 115 nM in rat cerebral cortex, 150 nM in NG 108-15 cell membranes, and 103 nM in the entire NG 108-15 cell, SR 57227A binds to 5-HT3 receptors tagged with [3H]S-zacopride[1].
ln Vivo	In the forced swimming test, SR 57227A (1–30 mg/kg; ip) reduces immobility time in a dose-dependent manner; its ED50 value is 14.2 mg/kg[2]. SR 57227A dose-dependently shortens the rats' period of immobility following intraperitoneal injection in the forced swimming test. Following oral dosing, SR 57227A is also active in both species (ED50=7.6 mg/kg ip in rats). In a mouse time-course investigation, SR 57227A (20 mg/kg po) has a noteworthy 6-hour duration of effect. In the final two days of the avoidance task, SR 57227A (1 and 3 mg/kg ip) decreases the elevation of escape failures in the learned helplessness paradigm in rats by 50–60%. It also lessens isolation-induced aggressivity in mice by 50–85%, an effect that is countered by Zacopride (1 mg/kg ip)[2].
References	[1]. 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]. 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.

Solubility Data

Solubility (In Vitro)	H2O: 33.33 mg/mL (134.31 mM) DMSO: 8.33 mg/mL (33.57 mM)
Solubility (In Vivo)	Solubility in Formulation 1: 10 mg/mL (40.30 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	4.0298 mL	20.1491 mL	40.2982 mL
	5 mM	0.8060 mL	4.0298 mL	8.0596 mL
	10 mM	0.4030 mL	2.0149 mL	4.0298 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.