6'-GNTI dihydrochloride

Discontinued Product

2962 has been discontinued.

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)
Datasheet
Citations
Reviews (1)
Literature (2)

Biological Activity for 6'-GNTI dihydrochloride

6'-GNTI dihydrochloride is a 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 for 6'-GNTI dihydrochloride

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.

Product Datasheets for 6'-GNTI dihydrochloride

Certificate of Analysis / Product Datasheet
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References for 6'-GNTI dihydrochloride

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

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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

Citations are publications that use Tocris products.

Currently there are no citations for 6'-GNTI dihydrochloride.

Reviews for 6'-GNTI dihydrochloride

Average Rating: 5 (Based on 1 Review.)

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Good product..
By Anonymous on 01/14/2020
Assay Type: In Vitro
Species: Human

Successfully induced ERK1/2 phosphorylation in CHO cells expressing KOR. It’s a very reliable compound.

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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!

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