6'-GNTI dihydrochloride

Catalog # Availability Size / Price Qty
2962/10
6'-GNTI dihydrochloride | Kappa Opioid Receptor Agonists
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Description: Selective κ/δ opioid heterodimer receptor agonist
Alternative 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

Purity: ≥97%

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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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. 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
  2. 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
  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
  4. Heterodimers of G protein-coupled receptors as novel and distinct drug targets.
    Rozenfeld et al.
    Drug Discov.Today Ther.Strateg., 2006;3:437

Product Datasheets

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