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
Technical Data
Solubility
Calculators
Datasheets
References
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).
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
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Jewettet 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
Joneset 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