Ro64-6198

Из Википедије, слободне енциклопедије
Ro64-6198
(IUPAC) ime
8-[(1S,3aS)-2,3,3a,4,5,6-heksahidro-1H-fenalen-1-il]-1-fenil-1,3,8-triazaspiro[4.5]dekan-4-on
Klinički podaci
Identifikatori
ATC kod nije dodeljen
PubChem[1][2] 9844019
Hemijski podaci
Formula C26H31N3O 
Mol. masa 401,543 g/mol
SMILES eMolekuli & PubHem
Sinonimi Ro64-6198
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

Ro64-6198 je nociceptinski lek koji se koristi u naučnim istraživanjima. On deluje kao potentan i selektivan agonist nociceptinskog receptora (ORL-1), sa više od sto puta većom selektivnošću za taj receptor nego za druge opioidne receptore.[3] On proizvodi anksiolitičke efekte u životinjskim studijama koji su ekvivalentni sa učinkom benzodiazepinskim lekovima,[4] ali nema antikonvulzivno dejstvo i ne proizvodi bilo kakve uočljive promene ponašanja.[5] Međutim, on utiče na kratkotrajnu memoriju,[6] i sprečava stresom indukovanu anoreksiju.[7][8] On takođe ima antitusivno dejstvo,[9] i umanjuje nagrađujuće i analgetsko delovanje od morfina, mada ne sprečava razvoj zavisnosti.[10][11][12] Bilo je pokazano da redukuje self-administraciju alkohola kod životinja i suzbija povraćaje u životinjskim modelima alkoholizma. ORL-1 agonisti možda mogu da nađu primenu u lečenju alkoholizma.[13]

Literatura[уреди]

  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. ^ Dautzenberg FM, Wichmann J, Higelin J, Py-Lang G, Kratzeisen C, Malherbe P, Kilpatrick GJ, Jenck F. Pharmacological characterization of the novel nonpeptide orphanin FQ/nociceptin receptor agonist Ro 64-6198: rapid and reversible desensitization of the ORL1 receptor in vitro and lack of tolerance in vivo. Journal of Pharmacology and Experimental Therapeutics. 2001 Aug;298(2):812-9. PMID 11454946
  4. ^ Varty GB, Hyde LA, Hodgson RA, Lu SX, McCool MF, Kazdoba TM, Del Vecchio RA, Guthrie DH, Pond AJ, Grzelak ME, Xu X, Korfmacher WA, Tulshian D, Parker EM, Higgins GA. Characterization of the nociceptin receptor (ORL-1) agonist, Ro64-6198, in tests of anxiety across multiple species. Psychopharmacology (Berlin). 2005 Oct;182(1):132-43. PMID 16025321
  5. ^ Jenck F, Wichmann J, Dautzenberg FM, Moreau JL, Ouagazzal AM, Martin JR, Lundstrom K, Cesura AM, Poli SM, Roever S, Kolczewski S, Adam G, Kilpatrick G. A synthetic agonist at the orphanin FQ/nociceptin receptor ORL1: anxiolytic profile in the rat. Proceedings of the National Academy of Sciences USA. 2000 Apr 25;97(9):4938-43. PMID 10758169
  6. ^ Higgins GA, Kew JN, Richards JG, Takeshima H, Jenck F, Adam G, Wichmann J, Kemp JA, Grottick AJ. A combined pharmacological and genetic approach to investigate the role of orphanin FQ in learning and memory. European Journal of Neuroscience. 2002 Mar;15(5):911-22. PMID 11906533
  7. ^ Ciccocioppo R, Biondini M, Antonelli L, Wichmann J, Jenck F, Massi M. Reversal of stress- and CRF-induced anorexia in rats by the synthetic nociceptin/orphanin FQ receptor agonist, Ro 64-6198. Psychopharmacology (Berlin). 2002 May;161(2):113-9. PMID 11981590
  8. ^ Ciccocioppo R, Cippitelli A, Economidou D, Fedeli A, Massi M. Nociceptin/orphanin FQ acts as a functional antagonist of corticotropin-releasing factor to inhibit its anorectic effect. Physiology and Behaviour. 2004 Aug;82(1):63-8. PMID 15234592
  9. ^ McLeod RL, Jia Y, Fernandez X, Parra LE, Wang X, Tulshian DB, Kiselgof EJ, Tan Z, Fawzi AB, Smith-Torhan A, Zhang H, Hey JA. Antitussive profile of the NOP agonist Ro-64-6198 in the guinea pig. Pharmacology. 2004 Jul;71(3):143-9. PMID 15161996
  10. ^ Kotlinska J, Wichmann J, Rafalski P, Talarek S, Dylag T, Silberring J. Non-peptidergic OP4 receptor agonist inhibits morphine antinociception but does not influence morphine dependence. Neuroreport. 2003 Mar 24;14(4):601-4. PMID 12657894
  11. ^ Shoblock JR, Wichmann J, Maidment NT. The effect of a systemically active ORL-1 agonist, Ro 64-6198, on the acquisition, expression, extinction, and reinstatement of morphine conditioned place preference. Neuropharmacology. 2005 Sep;49(4):439-46. PMID 15919100
  12. ^ Reiss D, Wichmann J, Tekeshima H, Kieffer BL, Ouagazzal AM. Effects of nociceptin/orphanin FQ receptor (NOP) agonist, Ro64-6198, on reactivity to acute pain in mice: comparison to morphine. European Journal of Pharmacology. 2008 Jan 28;579(1-3):141-8. PMID 18031727
  13. ^ Kuzmin A, Kreek MJ, Bakalkin G, Liljequist S. The nociceptin/orphanin FQ receptor agonist Ro 64-6198 reduces alcohol self-administration and prevents relapse-like alcohol drinking. Neuropsychopharmacology. 2007 Apr;32(4):902-10. PMID 16880770

Spoljašnje veze[уреди]



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