5'-Guanidinonaltrindol

5'-Guanidinonaltrindol
IUPAC ime
5'-Guanidinyl-17-(cyclopropylmethyl)-6,7-dehydro-4,5α-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinan
Identifikatori
ATC kodnone
PubChemCID 6604846
ChEMBLCHEMBL330427 ДаY
Sinonimi5'-Guanidinonaltrindol, GNTI
Hemijski podaci
FormulaC27H29N5O3
Molarna masa471,550 g/mol
  • C7CC7CN3CCC58c4c(ccc(O)c4OC28)CC3C5(O)Cc(c1c6)c2nc1ccc6NC(=N)N

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.[1] On ima spor početak i dugo trajanje dejstva,[2][3] i proizvodi antidepresantske efekte u životinjskim studijama.[4] GNTI takođe povišava alodiniju putem ometanja κ-opioidnog peptida dinorfina.[5]

Literatura

  1. ^ 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. 
  2. ^ 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. PMID 12373442. doi:10.1007/s00213-002-1038-x. 
  3. ^ 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. PMC 2096775 Слободан приступ. PMID 17702750. doi:10.1074/jbc.M705540200. 
  4. ^ Mague, SD; Pliakas, AM; Todtenkopf, MS; Tomasiewicz, HC; Zhang, Y; Stevens Jr, WC; Jones, RM; Portoghese, PS; Carlezon Jr, WA (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. PMID 12649385. doi:10.1124/jpet.102.046433. 
  5. ^ 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. PMC 1574046 Слободан приступ. PMID 12970097. doi:10.1038/sj.bjp.0705427. 


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