GNTI dihydrochloride
Discontinued Product
Chemical Name: 5'-Guanidinyl-17-(cyclopropylmethyl)-6,7-dehydro-4,5α-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinan dihydrochloride
Purity: ≥96%
Biological Activity
GNTI dihydrochloride is a 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
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
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
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 -
5'-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist.
Jones and Portoghese
Eur.J.Pharmacol., 2000;396:49 -
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
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Citation for GNTI dihydrochloride
The citations listed below are publications that use Tocris products. Selected citations for GNTI dihydrochloride include:
1 Citation: Showing 1 - 1
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Roles of opioid receptor subtype in the spinal antinociception of selective cyclooxygenase 2 inhibitor.
Authors: Choi Et al.
Korean J Pain 2010;23:236
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