RS-102221

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RS-102221
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
  • N-{5-[5-(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)pentanoyl] -2,4-dimethoxyphenyl}-4-(trifluoromethyl)benzenesulfonamide
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
Chemical and physical data
FormulaC27H33F3N4O7S
Molar mass614.632 g/mol g·mol−1
3D model (JSmol)
  • c4cc(C(F)(F)F)ccc4S(=O)(=O)Nc(c(OC)cc2OC)cc2C(=O)CCCCN(CC3)CCC13NC(=O)NC1=O
  • InChI=1S/C27H31F3N4O7S/c1-40-22-16-23(41-2)20(33-42(38,39)18-8-6-17(7-9-18)27(28,29)30)15-19(22)21(35)5-3-4-12-34-13-10-26(11-14-34)24(36)31-25(37)32-26/h6-9,15-16,33H,3-5,10-14H2,1-2H3,(H2,31,32,36,37)
  • Key:HZZZZODVDSHQRG-UHFFFAOYSA-N
 ☒NcheckY (what is this?)  (verify)

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

References

  1. ^ Bonhaus DW, Weinhardt KK, Taylor M, DeSouza A, McNeeley PM, Szczepanski K, Fontana DJ, Trinh J, Rocha CL, Dawson MW, Flippin LA, Eglen RM. RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):621-9. PMID 9225287
  2. ^ Kuznetsova EG, Amstislavskaya TG, Shefer EA, Popova NK. Effect of 5-HT2C receptor antagonist RS 102221 on mouse behavior. Bulletin of Experimental Biology and Medicine. 2006 Jul;142(1):76-9. PMID 17369908
  3. ^ Cremers TI, Giorgetti M, Bosker FJ, Hogg S, Arnt J, Mørk A, Honig G, Bøgesø KP, Westerink BH, den Boer H, Wikstrom HV, Tecott LH. Inactivation of 5-HT(2C) receptors potentiates consequences of serotonin reuptake blockade. Neuropsychopharmacology. 2004 Oct;29(10):1782-9. PMID 15138437
  4. ^ Filip M, Cunningham KA. Serotonin 5-HT(2C) receptors in nucleus accumbens regulate expression of the hyperlocomotive and discriminative stimulus effects of cocaine. Pharmacology Biochemistry and Behavior. 2002 Apr;71(4):745-56. PMID 11888566
  5. ^ Filip M, Cunningham KA. Hyperlocomotive and discriminative stimulus effects of cocaine are under the control of serotonin(2C) (5-HT(2C)) receptors in rat prefrontal cortex. Journal of Pharmacology and Experimental Therapeutics. 2003 Aug;306(2):734-43. PMID 12721337
  6. ^ Morita K, Hamamoto M, Arai S, Kitayama S, Irifune M, Kawahara M, Kihira K, Dohi T. Inhibition of serotonin transporters by cocaine and meprylcaine through 5-TH2C receptor stimulation facilitates their seizure activities. Brain Research. 2005 Sep 28;1057(1-2):153-60. PMID 16125150
  7. ^ Dremencov E, Weizmann Y, Kinor N, Gispan-Herman I, Yadid G. Modulation of dopamine transmission by 5HT2C and 5HT3 receptors: a role in the antidepressant response. Current Drug Targets. 2006 Feb;7(2):165-75. PMID 16475958
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