-opioid heterodimer receptor agonist (EC50
= 39.8, 112.5 and > 1000 nM for κ
respectively) that has no effect on opioid receptor homodimers (EC50
> 1000 nM). Displays tissue-specific analgesic effects in vitro
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Transformation of a κ-opoid receptor antagonist to a κ-agonist by transfer of a guanidinium group from the 5' to 6' position of naltrindole.
Sharma et al.
6'-guanidinonaltrindole (6'-GNTI) is a G protein-biased κ-opioid receptor agonist that inhibits arrestin recruitment.
Rives et al.
A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers.
Waldhoer et al.