6′-Guanidinonaltrindole (6′-GNTI) is a κ–δ-opioid receptor selective ligand used in scientific research.[1]
With 6′-GNTI, evidence was provided for the first time that receptor oligomerization plays functional role in living organisms.[2]
6′-GNTI is an extremely biased agonist of the κ-opioid receptor.[1] It is a potent partial agonist of the G protein pathway but does not recruit the β-arrestin pathway.[1] Due to its functional selectivity for the G protein pathway, 6′-GNTI functions as an antagonist of nonbiased KOR agonists on the β-arrestin pathway.[1] It is thought that 6′-GTNI may be able to produce analgesia without dysphoria and with a lower incidence of tolerance.[1]
See also
References
- ^ a b c d e Rives, ML; Rossillo, M; Liu-Chen, LY; Javitch, JA (2012). "6′-Guanidinonaltrindole (6′-GNTI) is a G protein–biased κ-opioid receptor agonist that inhibits arrestin recruitment". J Biol Chem. 287 (32): 27050–4. doi:10.1074/jbc.C112.387332. PMC 3411045. PMID 22736766.
- ^ Waldhoer M, Fong J, Jones RM, Lunzer MM, Sharma SK, Kostenis E, Portoghese PS, Whistler JL (June 2005). "A heterodimer-selective agonist shows in vivo relevance of G protein–coupled receptor dimers". Proc. Natl. Acad. Sci. U.S.A. 102 (25): 9050–5. Bibcode:2005PNAS..102.9050W. doi:10.1073/pnas.0501112102. PMC 1157030. PMID 15932946.