5'-Guanidinonaltrindol

Из Википедије, слободне енциклопедије
5'-Guanidinonaltrindol
(IUPAC) ime
5'-Guanidinyl-17-(cyclopropylmethyl)-6,7-dehydro-4,5α-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinan
Klinički podaci
Identifikatori
ATC kod nije dodeljen
PubChem[1][2] 6604846
ChEMBL[3] CHEMBL330427 YesY
Hemijski podaci
Formula C27H29N5O3 
Mol. masa 471,550 g/mol
SMILES eMolekuli & PubHem
Sinonimi 5'-Guanidinonaltrindol, GNTI
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

5'-Guanidinonaltrindol (GNTI) je opioidni antagonist koji se koristi u naučnim istraživanjima. On je veoma selektivan za κ opioidni receptor. On je pet puta pontentniji i 500 puta selektivniji od obično korištenog κ-opioidnog antagonista norbinaltorfimina.[4] On ima spor početak i dugo trajanje dejstva,[5][6] i proizvodi antidepresantske efekte u životinjskim studijama.[7] GNTI takođe povišava alodiniju putem ometanja κ-opioidnog peptida dinorfina.[8]

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. ^ 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. ^ Jones, RM; Portoghese, PS (2000). „5'-Guanidinonaltrindole, a highly selective and potent kappa-opioid receptor antagonist“. European journal of pharmacology 396 (1): 49–52. PMID 10822054. 
  5. ^ Negus, SS; Mello, NK; Linsenmayer, DC; Jones, RM; Portoghese, PS (2002). „Kappa opioid antagonist effects of the novel kappa antagonist 5'-guanidinonaltrindole (GNTI) in an assay of schedule-controlled behavior in rhesus monkeys“. Psychopharmacology 163 (3-4): 412–9. DOI:10.1007/s00213-002-1038-x. PMID 12373442. 
  6. ^ Bruchas, MR; Yang, T; Schreiber, S; Defino, M; Kwan, SC; Li, S; Chavkin, C (2007). „Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase“. The Journal of biological chemistry 282 (41): 29803–11. DOI:10.1074/jbc.M705540200. PMC 2096775. PMID 17702750. 
  7. ^ Mague, SD; Pliakas, AM; Todtenkopf, MS; Tomasiewicz, HC; Zhang, Y; Stevens Jr, WC; Jones, RM; Portoghese, PS et al. (2003). „Antidepressant-like effects of kappa-opioid receptor antagonists in the forced swim test in rats“. The Journal of pharmacology and experimental therapeutics 305 (1): 323–30. DOI:10.1124/jpet.102.046433. PMID 12649385. 
  8. ^ Obara, I; Mika, J; Schafer, MK; Przewlocka, B (2003). „Antagonists of the kappa-opioid receptor enhance allodynia in rats and mice after sciatic nerve ligation“. British journal of pharmacology 140 (3): 538–46. DOI:10.1038/sj.bjp.0705427. PMC 1574046. PMID 12970097. 



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