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Submit ReviewGNTI dihydrochloride
Discontinued Product
1282 has been discontinued.
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)
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 |
| InChI Key | GJPIMNXJPMPQHK-CVVXFVLRSA-N |
| 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
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
Average Rating: 5 (Based on 1 Review.)
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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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