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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
6'-guanidinonaltrindole (6'-GNTI) is a G protein-biased κ-opioid receptor agonist that inhibits arrestin recruitment.
Rives et al.
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
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