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RS-102,221 structure.png
Clinical data
Other namesRS-102,221; 8-[5-(2,4-Dimethoxy-5-(4-trifluoromethylphenylsulphonamido)phenyl -5-oxopentyl]-1,3,8-triazaspiro[4.5]decane-2,4-dione
CAS Number
PubChem CID
Chemical and physical data
Molar mass614.632 g/mol g·mol−1
3D model (JSmol)
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RS-102221 is a drug developed by Hoffmann–La Roche, which was one of the first compounds discovered that acts as a potent and selective antagonist at the serotonin 5-HT2C receptor, with around 100x selectivity over the closely related 5-HT2A and 5-HT2B receptors.[1] It has anxiolytic effects in animal studies,[2] increases the effectiveness of SSRI antidepressants,[3] and shows a complex interaction with cocaine, increasing some effects but decreasing others, reflecting a role for the 5-HT2C receptor in regulation of the dopamine signalling system in the brain.[4][5][6][7]

See also[edit]


  1. ^ Bonhaus DW, Weinhardt KK, Taylor M, DeSouza A, McNeeley PM, Szczepanski K, et al. "RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist". Neuropharmacology. 36 (4–5): 621–9. doi:10.1016/s0028-3908(97)00049-x. PMID 9225287.
  2. ^ Kuznetsova EG, Amstislavskaya TG, Shefer EA, Popova NK (July 2006). "Effect of 5-HT2C receptor antagonist RS 102221 on mouse behavior". Bulletin of Experimental Biology and Medicine. 142 (1): 76–9. doi:10.1007/s10517-006-0296-8. PMID 17369908.
  3. ^ Cremers TI, Giorgetti M, Bosker FJ, Hogg S, Arnt J, Mørk A, et al. (October 2004). "Inactivation of 5-HT(2C) receptors potentiates consequences of serotonin reuptake blockade". Neuropsychopharmacology. 29 (10): 1782–9. doi:10.1038/sj.npp.1300474. PMID 15138437.
  4. ^ Filip M, Cunningham KA (April 2002). "Serotonin 5-HT(2C) receptors in nucleus accumbens regulate expression of the hyperlocomotive and discriminative stimulus effects of cocaine". Pharmacology, Biochemistry, and Behavior. 71 (4): 745–56. doi:10.1016/s0091-3057(01)00741-9. PMID 11888566.
  5. ^ Filip M, Cunningham KA (August 2003). "Hyperlocomotive and discriminative stimulus effects of cocaine are under the control of serotonin(2C) (5-HT(2C)) receptors in rat prefrontal cortex". The Journal of Pharmacology and Experimental Therapeutics. 306 (2): 734–43. doi:10.1124/jpet.102.045716. PMID 12721337.
  6. ^ Morita K, Hamamoto M, Arai S, Kitayama S, Irifune M, Kawahara M, et al. (September 2005). "Inhibition of serotonin transporters by cocaine and meprylcaine through 5-TH2C receptor stimulation facilitates their seizure activities". Brain Research. 1057 (1–2): 153–60. doi:10.1016/j.brainres.2005.07.049. PMID 16125150.
  7. ^ Dremencov E, Weizmann Y, Kinor N, Gispan-Herman I, Yadid G (February 2006). "Modulation of dopamine transmission by 5HT2C and 5HT3 receptors: a role in the antidepressant response". Current Drug Targets. 7 (2): 165–75. doi:10.2174/138945006775515491. PMID 16475958.