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GNTI dihydrochloride
Other Information:
Sold with
the permission of the University of Minnesota, US Patent 6,500,824
Chemical Name:5'-Guanidinyl-17-(cyclopropylmethyl)-6,7-dehydro-4,5a-e
poxy-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 behaviour in rats
with a much higher potency (300-30,000-fold) and a shorter duration of action
than nor-binaltorphimine (Cat.No. 0347).
Joneset al (1998) Mutational evidence for a common κ
antagonist binding pocket in the wild type κ and mutant μ[K303E]
opioid receptors. J.Med.Chem. 41 4911. Jones and Portoghese
(2000) 5¢-Guanidinonaltrindole, a highly selective and potent κ-opioid
receptor antagonist. Eur.J.Pharmacol. 396 49. Jewett et
al (2001) The kappa-opioid antagonist GNTI reduces U50,488-, DAMGO-, and
deprivation-induced feeding, but not butorphanol- and neuropeptide Y-induced
feeding in rats. Brain Res. 909 75.
