6′-Guanidinonaltrindole (6′-GNTI) is a κ– δ- opioid receptor selective ligand used in scientific research. With 6′-GNTI, evidence was provided for the first time that receptor oligomerization plays functional role in living organisms. 6′-GNTI is an extremely biased agonist of the κ-opioid receptor. It is a potent

partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic e ...

of the G protein pathway but does not recruit the

β-arrestin Arrestins (abbreviated Arr) are a small family of proteins important for regulating signal transduction at G protein-coupled receptors. Arrestins were first discovered as a part of a conserved two-step mechanism for regulating the activity of ...

pathway. Due to its

functional selectivity Functional selectivity (or “agonist trafficking”, “biased agonism”, “biased signaling”, "ligand bias" and “differential engagement”) is the ligand-dependent selectivity for certain signal transduction pathways relative to a referen ...

for the G protein pathway, 6′-GNTI functions as an

antagonist An antagonist is a character in a story who is presented as the chief foe of the protagonist. Etymology The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...

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 Tolerance or toleration is the state of tolerating, or putting up with, conditionally. Economics, business, and politics * Toleration Party, a historic political party active in Connecticut * Tolerant Systems, the former name of Veritas Software ...

References

Semisynthetic opioids Guanidines Indolomorphinans Kappa-opioid receptor agonists Kappa-opioid receptor antagonists Receptor heteromer ligands Biased ligands {{analgesic-stub

See also

References