Catalog Number: 1282
Chemical Name: 5'-Guanidinyl-17-(cyclopropylmethyl)-6,7-dehydro-4,5α-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinan dihydrochloride
Biological Activity
Highly potent κ opioid receptor antagonist (Ki = 0.18 nM for human cloned κ receptors expressed in CHO cells). Displays 208- and 799-fold selectivity over μ and δ receptors respectively. Reduces feeding behavior in rats with a much higher potency (300-30,000-fold) and a shorter duration of action than nor-binaltorphimine (Cat.No. 0347).
Technical Data
  • M.Wt:
    544.48
  • Formula:
    C27H29N5O3.2HCl
  • Solubility:
    Soluble to 100 mM in water and to 100 mM in DMSO
  • Purity:
    >96%
  • Storage:
    Desiccate at -20°C
  • CAS No:
    351183-88-5
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. 5'-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist.
    Jones and Portoghese
    Eur.J.Pharmacol., 2000;396:49
  2. The kappa-opioid antagonist GNTI reduces U50,488-, DAMGO-, and deprivation-induced feeding, but not butorphanol- and neuropeptide Y-induced feeding in rats.
    Jewett et al.
    Brain Res., 2001;909:75
  3. Mutational evidence for a common κ antagonist binding pocket in the wild type κ and mutant μ[K303E] opioid receptors.
    Jones et al.
    J.Med.Chem., 1998;41:4911

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