GNTI dihydrochloride

Discontinued Product

GNTI dihydrochloride (Cat. No. 1282) has been withdrawn from sale for commercial reasons.
Description: Potent, selective κ antagonist
Chemical Name: 5'-Guanidinyl-17-(cyclopropylmethyl)-6,7-dehydro-4,5α-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinan dihydrochloride
Purity: ≥96% (HPLC)
Citations (1)
Reviews (1)
Literature (2)

Biological Activity for GNTI dihydrochloride

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 for GNTI dihydrochloride

M. Wt 544.48
Formula C27H29N5O3.2HCl
Storage Desiccate at -20°C
Purity ≥96% (HPLC)
CAS Number 351183-88-5
PubChem ID 90479777
Smiles OC3=CC=C2CC([C@@]5(O)[C@@]4(CC8)C2=C3O[C@H]4C(NC7=C6C=C(NC=N)C=C7)=C6C5)N8CC1CC1.Cl.Cl

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.

Product Datasheets for GNTI dihydrochloride

Certificate of Analysis / Product Datasheet
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References for GNTI dihydrochloride

References are publications that support the biological activity of the product.

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 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

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

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Keywords: GNTI dihydrochloride, GNTI dihydrochloride supplier, Potent, selective, κ-opioid, kappa-opioid, antagonists, KOP, Receptors, OP2, Kappa, Opioid, 1282, Tocris Bioscience

1 Citation for GNTI dihydrochloride

Citations are publications that use Tocris products. Selected citations for GNTI dihydrochloride include:

Choi et al (2010) Roles of opioid receptor subtype in the spinal antinociception of selective cyclooxygenase 2 inhibitor. Korean J Pain 23 236 PMID: 21217886

Reviews for GNTI dihydrochloride

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Very Good Product.
By Luca Zangrandi on 01/14/2020
Assay Type: Ex Vivo
Species: Human

Successfully stopped selective agonist-induced ERK phosphorylation in CHO cells.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

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