RS 102221 hydrochloride
Cat. No. 1050
Chemical Name: 8-[5-(2,4-Dimethoxy-5-(4-trifluorom
Biological ActivityPotent 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 InformationSold with the permission of Roche Bioscience
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 / Product Datasheet / Safety Datasheet
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.
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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.
Ward et al (2015) Regulation of oligomeric organization of the serotonin 5-hydroxytryptamine 2C (5-HT2C) receptor observed by spatial intensity distribution analysis. J Neurophysiol 290 12844. PMID: 25825490.
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.
Austgen et al (2012) 5-hydroxytryptamine 2C receptors tonically augment synaptic currents in the nucleus tractus solitarii. J Neurophysiol 108 2292. PMID: 22855775.
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 (2010) Endogenous serotonin acts on 5-HT2C-like receptors in key vocal areas of the brain stem to initiate vocalizations in Xenopus laevis. J Clin Invest 103 648. PMID: 19955293.
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