RS 102221 hydrochloride
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 ActivityRS 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.
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.
RS-102221: a novel high affinity and selective 5-HT2C receptor antagonist.
Bonhaus et al.
Absorption and brain penetration of a high affinity, highly selective 5-HT2C receptor antagonist, RS-102221.
Bonhaus et al.
Some benzenesulphonamido-substituted valerophenones that are selective antagonists for the 5-HT2C receptor.
Weinhardt et al.
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
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
Heterodimers of serotonin receptor subtypes 2 are driven by 5-HT2C protomers.
Authors: Moutkine Et al.
J Biol Chem 2017;292:6352
Increased serotonin transporter expression reduces fear and recruitment of parvalbumin interneurons of the amygdala.
Authors: Bocchio Et al.
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
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
Promiscuous dimerization of the GH secretagogue receptor (GHS-R1a) attenuates ghrelin-mediated signaling.
Authors: Schellekens Et al.
J Biol Chem 2013;288:181
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
5-hydroxytryptamine 2C receptors tonically augment synaptic currents in the nucleus tractus solitarii.
Authors: Austgen Et al.
J Neurophysiol 2012;108:2292
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
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
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
5-HT2C-like receptors in the brain of Xenopus laevis initiate sex-typical fictive vocalizations.
Authors: Yu and Yamaguchi
J Neurophysiol 2009;102:752
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
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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