RS 102221 hydrochloride

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Cat.No. 1050 - RS 102221 hydrochloride | C27H31F3N4O7S.HCl | CAS No. 187397-18-8
Description: Selective 5-HT2C antagonist
Chemical Name: 8-[5-(2,4-Dimethoxy-5-(4-trifluoromethylphenylsulphonamido)phenyl-5-oxopentyl]-1,3,8-triazaspiro[4.5]decane-2,4-dione hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (10)
Literature

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

Compound Libraries

RS 102221 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 649.08
Formula C27H31F3N4O7S.HCl
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 187397-18-8
PubChem ID 18931299
InChI Key SZJZEJZLRDIHPB-UHFFFAOYSA-N
Smiles Cl.COC1=CC(OC)=C(NS(=O)(=O)C2=CC=C(C=C2)C(F)(F)F)C=C1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O

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.

Solubility Data

SolubilitySoluble to 100 mM in DMSO

Preparing Stock Solutions

The following data is based on the product molecular weight 649.08. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.54 mL 7.7 mL 15.41 mL
5 mM 0.31 mL 1.54 mL 3.08 mL
10 mM 0.15 mL 0.77 mL 1.54 mL
50 mM 0.03 mL 0.15 mL 0.31 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

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

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


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

10 Citations for RS 102221 hydrochloride

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

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

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

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


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