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Submit Review6'-GNTI dihydrochloride
Description: Selective κ/δ opioid heterodimer receptor agonist
Alternative Names: 6'-Guanidinonaltrindole dihydrochloride
Chemical Name: 6''-Guanidinyl-17-(cyclopropylmethyl)-6,7-dehydro-4,5a-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinan dihydrochloride
Purity: ≥97% (HPLC)
Biological Activity
Selective κ/δ-opioid heterodimer receptor agonist (EC50 = 39.8, 112.5 and > 1000 nM for κ/δ, κ/μ and δ/μ respectively) that has no effect on opioid receptor homodimers (EC50 > 1000 nM). Displays tissue-specific analgesic effects in vitro.
Technical Data
| M. Wt | 544.48 |
| Formula | C27H29N5O3.2HCl |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| PubChem ID | 90488790 |
| InChI Key | OCMMBKYOHYNDPT-GXOQRFFGSA-N |
| Smiles | OC1=CC=C2CC([C@@]3(O)[C@@]4(CC5)C2=C1O[C@H]4C(NC6=C7C=CC(NC(N)=N)=C6)=C7C3)N5CC8CC8.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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 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 the degree 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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References
References are publications that support the biological activity of the product.
Sharma et al (2001) Transformation of a κ-opoid receptor antagonist to a κ-agonist by transfer of a guanidinium group from the 5' to 6' position of naltrindole. J.Med.Chem. 44 2073 PMID: 11405645
Waldhoer et al (2005) A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers. Proc.Natl.Acad.Sci.USA 102 9050
Rozenfeld et al (2006) Heterodimers of G protein-coupled receptors as novel and distinct drug targets. Drug Discov.Today Ther.Strateg. 3 437
Rives et al (2012) 6'-guanidinonaltrindole (6'-GNTI) is a G protein-biased κ-opioid receptor agonist that inhibits arrestin recruitment. J.Biol.Chem. 287 27050 PMID: 22736766
If you know of a relevant reference for 6'-GNTI dihydrochloride, please let us know.
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Keywords: 6'-GNTI dihydrochloride, 6'-GNTI dihydrochloride supplier, Selective, kappa/δ-opioid, delta-opioid, κ-opioid, kappa-opioid, heterodimer, receptor, agonists, KOP, Receptors, OP2, DOP, OP1, 6'-Guanidinonaltrindole, dihydrochloride, Kappa, Opioid, Delta, 2962, Tocris Bioscience
Citations for 6'-GNTI dihydrochloride
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