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 |
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 54.45 | 100 | |
| water | 54.45 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 544.48. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.84 mL | 9.18 mL | 18.37 mL |
| 5 mM | 0.37 mL | 1.84 mL | 3.67 mL |
| 10 mM | 0.18 mL | 0.92 mL | 1.84 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.37 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: GNTI dihydrochloride, supplier, Potent, selective, κ-opioid, kappa-opioid, antagonists, KOP, Receptors, OP2, Kappa, Opioid, Receptors, Kappa, Opioid, Receptors, Tocris Bioscience
