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6'-Guanidinonaltrindole
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 alsoReferences
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