GNTI dihydrochloride

Cat. No. 1282

GNTI dihydrochloride C27H29N5O3.2HCl [351183-88-5]

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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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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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. PMID: 11478923.

Jones and Portoghese (2000) 5'-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist. Eur.J.Pharmacol. 396 49. PMID: 10822054.

Jones et 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. PMID: 9836606.

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Keywords: GNTI dihydrochloride, supplier, Potent, selective, κ-opioid, kappa-opioid, antagonists, KOP, Receptors, OP2, Tocris Bioscience, κ Opioid Receptor Antagonist products

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