GNTI dihydrochloride

• Supplier: Tocris Bioscience
• Catalog: 5607
• Prices: $199.00, $825.00
• Sizes: 10 mg, 50 mg
• Function Type: Antagonist
• Cas Number: 351183-88-5
• Chemical Name: 5'-Guanidinyl-17-(cyclopropylmethyl)-6,7-dehydro-4,5α-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinandihydrochloride
• Formula: C27H29N5O3.2HCl
• Molecular Weight: 544.48
• Purity: >96 %
• Description: Highly potent κ opioid receptor antagonist (K i = 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).

Product References

Mutational evidence for a common kappa antagonist binding pocket in the wild-type - Mutational evidence for a common kappa antagonist binding pocket in the wild-type

Jones RM, Hjorth SA, Schwartz TW, Portoghese PS. J Med Chem. 1998 Dec 3;41(25):4911-4.

5'-Guanidinonaltrindole, a highly selective and potent kappa-opioid receptor - 5'-Guanidinonaltrindole, a highly selective and potent kappa-opioid receptor

Jones RM, Portoghese PS. Eur J Pharmacol. 2000 May 12;396(1):49-52.

The kappa-opioid antagonist GNTI reduces U50,488-, DAMGO-, and - The kappa-opioid antagonist GNTI reduces U50,488-, DAMGO-, and

Jewett DC, Grace MK, Jones RM, Billington CJ, Portoghese PS, Levine AS. Brain Res. 2001 Aug 3;909(1-2):75-80.