6'-Guanidinonaltrindole Explained

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. 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. It is thought that 6′-GTNI may be able to produce analgesia without dysphoria and with a lower incidence of tolerance.

See also

• 5′-Guanidinonaltrindole
• RB-64
• Noribogaine
• ICI-199,441

Notes and References

1. 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 . . 287 . 32. 27050–4 . 22736766 . 10.1074/jbc.C112.387332 . 3411045. free .
2. Waldhoer M, Fong J, Jones RM, Lunzer MM, Sharma SK, Kostenis E, Portoghese PS, Whistler JL . 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 . June 2005 . 15932946 . 1157030 . 10.1073/pnas.0501112102 . 2005PNAS..102.9050W . free .