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RS 102221 hydrochloride

Catalog #: 1050
14 Citations Datasheet / COA / SDS
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1050/10
1050/50
RS 102221 hydrochloride | CAS No. 187397-18-8 | 5-HT2C Receptor Antagonists
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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%

Product Details
Citations (14)
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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.

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

Additional Information

Licensing Caveats:
Sold with the permission of Roche Bioscience

Background References

  1. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
    Fox JT, Sakamuru S, Huang R
    Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
  2. RS-102221: a novel high affinity and selective 5-HT2C receptor antagonist.
    Bonhaus et al.
    Neuropharmacology, 1997;36:621
  3. 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
  4. Some benzenesulphonamido-substituted valerophenones that are selective antagonists for the 5-HT2C receptor.
    Weinhardt et al.
    Bioorg.Med.Chem.Lett., 1996;6:2687

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Citations for RS 102221 hydrochloride

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

14 Citations: Showing 1 - 10

  1. Peripheral serotonin receptor 2B and transient receptor potential channel 4 mediate pruritus to serotonergic antidepressants in mice.
    Authors: Lee Et al.
    J Allergy Clin Immunol  2018;142:1349
  2. Heterodimers of serotonin receptor subtypes 2 are driven by 5-HT2C protomers.
    Authors: Moutkine Et al.
    J Biol Chem  2017;292:6352
  3. Increased serotonin transporter expression reduces fear and recruitment of parvalbumin interneurons of the amygdala.
    Authors: Bocchio Et al.
    Neuropsychopharmacology  2015;40:3015
  4. Pronociceptive and antinociceptive effects of Bupren. in the spinal cord dorsal horn cover a dose range of four orders of magnitude.
    Authors: Gerhold Et al.
    J Neurosci  2015;35:9580
  5. 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
  6. Promiscuous dimerization of the GH secretagogue receptor (GHS-R1a) attenuates ghrelin-mediated signaling.
    Authors: Schellekens Et al.
    J Biol Chem  2013;288:181
  7. 5-Hydroxytryptamine 5HT2C receptors form a protein complex with N-MthD.-aspartate GluN2A subunits and activate phosphorylation of Src protein to modulate motoneuronal depolarization.
    Authors: Bigford Et al.
    J Biol Chem  2012;287:11049
  8. 5-hydroxytryptamine 2C receptors tonically augment synaptic currents in the nucleus tractus solitarii.
    Authors: Austgen Et al.
    J Neurophysiol  2012;108:2292
  9. 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
  10. Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors.
    Authors: Murray Et al.
    J Neurophysiol  2011;106:925

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