Chemical Name: 6''-Guanidinyl-17-(cyclopropylmethyl)-6,7-dehydro-4,5a-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinan dihydrochloride
Biological ActivitySelective κ/δ-opioid heterodimer receptor agonist (EC50 = 39.8, 112.5 and > 1000 nM for κ/δ, κ/μ and δ/μ respectively) that has no effect on opioid receptor homodimers (EC50 > 1000 nM). Displays tissue-specific analgesic effects in vitro.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers.
Waldhoer et al.
Heterodimers of G protein-coupled receptors as novel and distinct drug targets.
Rozenfeld et al.
Drug Discov.Today Ther.Strateg., 2006;3:437
6'-guanidinonaltrindole (6'-GNTI) is a G protein-biased κ-opioid receptor agonist that inhibits arrestin recruitment.
Rives et al.
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Successfully induced ERK1/2 phosphorylation in CHO cells expressing KOR. It’s a very reliable compound.