Catalog Number: 2962
Alternate Names: 6'-Guanidinonaltrindole dihydrochloride
Chemical Name: 6''-Guanidinyl-17-(cyclopropylmethyl)-6,7-dehydro-4,5a-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinan dihydrochloride
Biological Activity
Selective 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.
Technical Data
  • M.Wt:
    544.48
  • Formula:
    C27H29N5O3.2HCl
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >97%
  • Storage:
    Store at -20°C
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. 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.
    J.Med.Chem., 2001;44:2073
  2. 6'-guanidinonaltrindole (6'-GNTI) is a G protein-biased κ-opioid receptor agonist that inhibits arrestin recruitment.
    Rives et al.
    J.Biol.Chem., 2012;287:27050
  3. A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers.
    Waldhoer et al.
    Proc.Natl.Acad.Sci.USA, 2005;102:9050

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