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 (14)
Reviews
Literature (4)

Biological Activity for RS 102221 hydrochloride

RS 102221 hydrochloride is a 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 for RS 102221 hydrochloride

RS 102221 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for RS 102221 hydrochloride

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for RS 102221 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 100

Preparing Stock Solutions for RS 102221 hydrochloride

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

Select a batch to recalculate based on the batch molecular weight:
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 for RS 102221 hydrochloride

Certificate of Analysis / Product Datasheet
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References for RS 102221 hydrochloride

References are publications that support the biological activity of the product.

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


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14 Citations for RS 102221 hydrochloride

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

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

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

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

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

Bigford et al (2012) 5-Hydroxytryptamine 5HT2C receptors form a protein complex with N-MthD.-aspartate GluN2A subunits and activate phosphorylation of Src protein to modulate motoneuronal depolarization. J Biol Chem 287 11049 PMID: 22291020

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

Murray et al (2011) Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors. J Neurophysiol 106 925 PMID: 21653728

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

Moutkine et al (2017) Heterodimers of serotonin receptor subtypes 2 are driven by 5-HT2C protomers. J Biol Chem 292 6352 PMID: 28258217

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

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

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

Austgen et al (2012) 5-hydroxytryptamine 2C receptors tonically augment synaptic currents in the nucleus tractus solitarii. J Neurophysiol 108 2292 PMID: 22855775

Lee et al (2018) Peripheral serotonin receptor 2B and transient receptor potential channel 4 mediate pruritus to serotonergic antidepressants in mice. J Allergy Clin Immunol 142 1349 PMID: 29920354


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