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SR 57227 hydrochloride

Potent, selective 5-HT3 agonist CAS# 77145-61-0

SR 57227 hydrochloride

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Chemical structure

SR 57227 hydrochloride

3D structure

Chemical Properties of SR 57227 hydrochloride

Cas No. 77145-61-0 SDF Download SDF
PubChem ID 131746 Appearance Powder
Formula C10H15Cl2N3 M.Wt 248.15
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 50 mM in water and to 100 mM in DMSO
Chemical Name 1-(6-chloropyridin-2-yl)piperidin-4-amine;hydrochloride
SMILES C1CN(CCC1N)C2=NC(=CC=C2)Cl.Cl
Standard InChIKey FUMINTAAUJUVMP-UHFFFAOYSA-N
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of SR 57227 hydrochloride

DescriptionA high affinity, selective 5-HT3 receptor agonist, active in vivo and CNS penetrant.

SR 57227 hydrochloride Dilution Calculator

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SR 57227 hydrochloride Molarity Calculator

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Preparing Stock Solutions of SR 57227 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 4.0298 mL 20.1491 mL 40.2982 mL 80.5964 mL 100.7455 mL
5 mM 0.806 mL 4.0298 mL 8.0596 mL 16.1193 mL 20.1491 mL
10 mM 0.403 mL 2.0149 mL 4.0298 mL 8.0596 mL 10.0746 mL
50 mM 0.0806 mL 0.403 mL 0.806 mL 1.6119 mL 2.0149 mL
100 mM 0.0403 mL 0.2015 mL 0.403 mL 0.806 mL 1.0075 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on SR 57227 hydrochloride

5-HT3-like receptors in the rat medial prefrontal cortex: further pharmacological characterization.[Pubmed:8891244]

Brain Res. 1996 Sep 9;733(1):21-30.

The aim of the study was to further characterize the pharmacological properties of 5-hydroxytryptamine (5-HT)3-like receptors in the rat medial prefrontal cortex (mPFC) using combinations of biochemical and electrophysiological approaches. Phenylbiguanide (PBG) and three chlorinated derivatives, ortho-chloro-PBG (oCPBG), meta-chloro-PBG (mCPBG) and para-chloro-PBG (pCPBG), dose-dependently stimulated phosphoionositide (PI) turnover in fronto-cingulate cortical slices. All three chloro-isomers of PBG were equipotent in stimulating PI turnover. SR 57227A ((4-amino)-(6-chloro-2-pyridyl) L-piperidine hydrochloride, a novel compound with high affinity and selectivity for peripheral and central 5-HT3 receptors) dose-dependently stimulated PI turnover in fronto-cingulate cortical slices. The rank order of potency of all the 5-HT3 receptor agonists tested in the PI assay as compared to 5-HT was: 5-HT > 2-Me-5-HT > SR57227A > PBG = mCPBG = oCPBG = mCPBG. 5-HT and 5-HT receptor agonists depressed the firing rate of both spontaneously active and glutamate-activated quiescent mPFC cells in a current (dose)-dependent fashion. The rank order of effectiveness of these compounds was: 5-HT > SR57227A = 2-Me-5-HT = mCPBG = oCPBG = pCPBG = PBG. Unlike its action on the 5-HT3 receptors in the periphery or cultured cell lines, D-tubocurarine chloride appears to be non-specific in blocking the depressant action of 2-Me-5-HT, gamma-aminobutyric acid and dopamine. Our results combined support the view that the pharmacological properties of 5-HT3-like receptors in the mPFC are not identical to those located in peripheral tissues and in cultured cell lines.

SR 57227A: a potent and selective agonist at central and peripheral 5-HT3 receptors in vitro and in vivo.[Pubmed:7689975]

Eur J Pharmacol. 1993 Jun 24;237(2-3):299-309.

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 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes in vitro, assayed under various conditions with [3H]S-zacopride or [3H]granisetron as radioligand. Like reference 5-HT3 receptor agonists, SR 57227A stimulated the uptake of [14C]guanidinium into NG 108-15 cells in the presence of substance P (EC50 = 208 +/- 16 nM) and contracted the isolated guinea-pig ileum (EC50 = 11.2 +/- 1.1 microM), effects that were antagonised by the 5-HT3 receptor antagonist tropisetron. The agonist effect of SR 57227A was also observed in vivo, as the compound elicited the Bezold-Jarisch reflex in anesthetised rats (ED50 = 8.3 micrograms/kg i.v.), an effect that was blocked by tropisetron and R,S-zacopride, but not by methysergide. When injected unilaterally into the mouse striatum, SR 57227A, like 2-methyl-5-HT, elicited contralateral turning behaviour which was antagonised by ondansetron. Furthermore, microiontophoretic application of SR 57227A markedly inhibited the firing rate of rat cortical neurones, an effect antagonised by tropisetron. Finally, in contrast to reference 5-HT3 agonists, SR 57227A bound to 5-HT3 receptors on mouse cortical membranes after systemic administration (ED50 = 0.39 mg/kg i.p. and 0.85 mg/kg p.o.). These results suggest that SR 57227A is a potent agonist at peripheral and central 5-HT3 receptors, both in vitro and in vivo. In view of the dearth of 5-HT3 receptor agonists which are capable of crossing the blood-brain barrier, SR 57227A may be useful in the characterisation of the neuropharmacological effects produced by the stimulation of these receptors.

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