Catalog Number: 1050
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.
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.
Additional Information
Licensing Caveats:
Sold with the permission of Roche Bioscience
Background References
  1. RS-102221: a novel high affinity and selective 5-HT2C receptor antagonist.
    Bonhaus et al.
    Neuropharmacology, 1997;36:621
  2. Absorption and brain penetration of a high affinity, highly selective 5-HT2C receptor antagonist, RS-102221.
    Bonhaus et al.
    Ann.N.Y.Acad.Sci., 1998;861:269
  3. Some benzenesulphonamido-substituted valerophenones that are selective antagonists for the 5-HT2C receptor.
    Weinhardt et al.
    Bioorg.Med.Chem.Lett., 1996;6:2687
Citations:

The citations listed below are publications that use Tocris products. Selected citations for RS 102221 hydrochloride include:

10 Citations: Showing 1 - 10
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  1. Increased serotonin transporter expression reduces fear and recruitment of parvalbumin interneurons of the amygdala.
    Authors: Bocchio Et al.
    Neuropsychopharmacology 2015;40:3015
  2. Pronociceptive and antinociceptive effects of buprenorphine in the spinal cord dorsal horn cover a dose range of four orders of magnitude.
    Authors: Gerhold Et al.
    J Neurosci 2015;35:9580
  3. Regulation of oligomeric organization of the serotonin 5-hydroxytryptamine 2C (5-HT2C) receptor observed by spatial intensity distribution analysis.
    Authors: Ward Et al.
    J Neurophysiol 2015;290:12844
  4. Promiscuous dimerization of the growth hormone secretagogue receptor (GHS-R1a) attenuates ghrelin-mediated signaling.
    Authors: Schellekens Et al.
    J Biol Chem 2013;288:181
  5. 5-hydroxytryptamine 2C receptors tonically augment synaptic currents in the nucleus tractus solitarii.
    Authors: Austgen Et al.
    J Neurophysiol 2012;108:2292
  6. Altered 5-HT2C receptor agonist-induced responses and 5-HT2C receptor RNA editing in the amygdala of serotonin transporter knockout mice.
    Authors: Moya Et al.
    BMC Pharmacol 2011;11:3
  7. Endogenous serotonin acts on 5-HT2C-like receptors in key vocal areas of the brain stem to initiate vocalizations in Xenopus laevis.
    Authors: Yu and Yamaguchi
    J Clin Invest 2010;103:648
  8. 5-HT2C-like receptors in the brain of Xenopus laevis initiate sex-typical fictive vocalizations.
    Authors: Yu and Yamaguchi
    J Neurophysiol 2009;102:752
  9. Regulation of MDCK cell-substratum adhesion by RhoA and myosin light chain kinase after ATP depletion.
    Authors: Prahalad Et al.
    Am J Physiol Cell Physiol 2004;286:C693
  10. Haloperidol, but not clozapine, produces dramatic catalepsy in Δ9-THC-treated rats: possible clinical implications.
    Authors: Marchese Et al.
    Br J Pharmacol 2003;140:520

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