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RS-102,221

RS-102,221
IUPAC ime
N5-[5-(2,4-diokso-1,3,8-triazaspiro[4.5]dec-8-il)pentanoil] -2,4-dimetoksifenil4-(trifluorometil)benzenesulfonamid
Identifikatori
CAS broj185376-97-0 ДаY
ATC kodnone
PubChemCID 3693566
IUPHAR/BPS187
ChEMBLCHEMBL88402 ДаY
SinonimiRS-102,221; 8-[5-(2,4-Dimetoksi-5-(4-trifluorometilfenilsulfnamido)fenil -5-oksopentil]-1,3,8-triazaspiro[4.5]dekan-2,4-dion
Hemijski podaci
FormulaC27H33F3N4O7S
Molarna masa614,632 g/mol
  • c4cc(C(F)(F)F)ccc4S(=O)(=O)Nc(c(OC)cc2OC)cc2C(=O)CCCCN(CC3)CCC13NC(=O)NC1=O

RS-102,221 je lek koji je bio jedno od prvih otkrivenih jedinjenja koja deluju kao potentan i selektivan antagonist na serotoninskom 5-HT2C receptoru, sa selektivnošću od oko 100x u odnosu na blisko srodne 5-HT2A i 5-HT2B receptore.[1] On je pokazao anksiolitičke efekte u životinjskim studijama,[2] povećanje efektivnosti SSRI antidepresiva,[3] i ima kompleksne interakcije sa kokainom, tako što povećava neke i snižava druge efekte, što odražava ulogu 5-HT2C receptora i regulaciji dopaminske signalizacije u mozgu.[4][5][6][7]

Reference

  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 Behaviour. 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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