Chemistry:RS-102221

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Short description: Chemical compound
RS-102221
RS-102221.svg
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
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
Chemical and physical data
FormulaC27H33F3N4O7S
Molar mass614.64 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 100× 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

References

  1. ↑ "RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist". Neuropharmacology 36 (4–5): 621–9. 1997. doi:10.1016/s0028-3908(97)00049-x. PMID 9225287. 
  2. ↑ "Effect of 5-HT2C receptor antagonist RS 102221 on mouse behavior". Bulletin of Experimental Biology and Medicine 142 (1): 76–9. July 2006. doi:10.1007/s10517-006-0296-8. PMID 17369908. 
  3. ↑ "Inactivation of 5-HT(2C) receptors potentiates consequences of serotonin reuptake blockade". Neuropsychopharmacology 29 (10): 1782–9. October 2004. doi:10.1038/sj.npp.1300474. PMID 15138437. 
  4. ↑ "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. April 2002. doi:10.1016/s0091-3057(01)00741-9. PMID 11888566. 
  5. ↑ "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. August 2003. doi:10.1124/jpet.102.045716. PMID 12721337. 
  6. ↑ "Inhibition of serotonin transporters by cocaine and meprylcaine through 5-TH2C receptor stimulation facilitates their seizure activities". Brain Research 1057 (1–2): 153–60. September 2005. doi:10.1016/j.brainres.2005.07.049. PMID 16125150. http://ir.lib.hiroshima-u.ac.jp/files/public/0/115/20141016115526561231/Brain-Res_1057-1-2_153-160_2005-9-28.pdf. 
  7. ↑ "Modulation of dopamine transmission by 5HT2C and 5HT3 receptors: a role in the antidepressant response". Current Drug Targets 7 (2): 165–75. February 2006. doi:10.2174/138945006775515491. PMID 16475958. 



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