RS-102,221

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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
Klinički podaci
Identifikatori
CAS broj 185376-97-0
ATC kod nije dodeljen
PubChem[1][2] 3693566
ChEMBL[3] CHEMBL88402 YesY
Hemijski podaci
Formula C27H33F3N4O7S 
Mol. masa 614,632 g/mol
SMILES eMolekuli & PubHem
Sinonimi RS-102,221; 8-[5-(2,4-Dimetoksi-5-(4-trifluorometilfenilsulfnamido)fenil -5-oksopentil]-1,3,8-triazaspiro[4.5]dekan-2,4-dion
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

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.[4] On je pokazao anksiolitičke efekte u životinjskim studijama,[5] povećanje efektivnosti SSRI antidepresiva,[6] 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.[7][8][9][10]

Reference[uredi - уреди | uredi izvor]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. doi:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1. 
  3. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). "ChEMBL: a large-scale bioactivity database for drug discovery". Nucleic Acids Res 40 (Database issue): D1100–7. doi:10.1093/nar/gkr777. PMID 21948594.  edit
  4. 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
  5. 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
  6. 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
  7. 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
  8. 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
  9. 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
  10. 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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