RS 102221 hydrochloride

Cat. No. 1050

RS 102221 hydrochloride C27H31F3N4O7S.HCl [187397-18-8]

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Chemical Name: 8-[5-(2,4-Dimethoxy-5-(4-trifluoromethylphenylsulphonamido)phenyl-5-oxopentyl]-1,3,8-triazaspiro[4.5]decane-2,4-dione hydrochloride

Biological Activity

Potent and selective 5-HT2C antagonist (pKi = 8.7). Displays ~ 100-fold selectivity over the 5-HT2A and 5-HT2B subtypes and is > 100-fold selective over other 5-HT receptors, α- and β-adrenergic and muscarinic ACh receptors.

Licensing Information

Sold with the permission of Roche Bioscience

Technical Data

M.Wt:
649.08
Formula:
C27H31F3N4O7S.HCl
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at RT
CAS No:
187397-18-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

Bonhaus et al (1998) Absorption and brain penetration of a high affinity, highly selective 5-HT2C receptor antagonist, RS-102221. Ann.N.Y.Acad.Sci. 861 269. PMID: 9928284.

Bonhaus et al (1997) RS-102221: a novel high affinity and selective 5-HT2C receptor antagonist. Neuropharmacology 36 621. PMID: 9225287.

Weinhardt et al (1996) Some benzenesulphonamido-substituted valerophenones that are selective antagonists for the 5-HT2C receptor. Bioorg.Med.Chem.Lett. 6 2687.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for RS 102221 hydrochloride include:

Bocchio et al (2015) Increased serotonin transporter expression reduces fear and recruitment of parvalbumin interneurons of the amygdala. Neuropsychopharmacology 40 3015. PMID: 26052039.

Gerhold et al (2015) Pronociceptive and antinociceptive effects of buprenorphine in the spinal cord dorsal horn cover a dose range of four orders of magnitude. J Neurosci 35 9580. PMID: 26134641.

Schellekens et al (2013) Promiscuous dimerization of the growth hormone secretagogue receptor (GHS-R1a) attenuates ghrelin-mediated signaling. J Biol Chem 288 181. PMID: 23161547.

Moya et al (2011) Altered 5-HT2C receptor agonist-induced responses and 5-HT2C receptor RNA editing in the amygdala of serotonin transporter knockout mice. BMC Pharmacol 11 3. PMID: 21473759.

Yu and Yamaguchi (2009) 5-HT2C-like receptors in the brain of Xenopus laevis initiate sex-typical fictive vocalizations. J Neurophysiol 102 752. PMID: 19474172.

Prahalad et al (2004) Regulation of MDCK cell-substratum adhesion by RhoA and myosin light chain kinase after ATP depletion. Am J Physiol Cell Physiol 286 C693. PMID: 14644769.

Marchese et al (2003) Haloperidol, but not clozapine, produces dramatic catalepsy in Δ9-THC-treated rats: possible clinical implications. Br J Pharmacol 140 520. PMID: 12970091.

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Keywords: RS 102221 hydrochloride, supplier, Selective, 5-HT2C, antagonist, Serotonin, Receptors, RS102221, hydrochloride, Tocris Bioscience, 5-HT2C Receptor Antagonist products

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