The selectivity of the opioid antagonist, naltrindole, for delta-opioid receptors

In the mouse vas deferens, naltrindole gave pKB values of 9.7, 8.3, and 7.5 at the delta-, mu-, and kappa-sites and in binding assays, pIC50 values of 9.6, 7.8 and 7.2 at the same sites. The affinity of naltrindole for the delta binding site was increased in the presence of sodium ions and 5'-g...

Full description

Saved in:
Bibliographic Details
Published inJournal of pharmacy and pharmacology Vol. 42; no. 5; p. 358
Main Authors Rogers, H, Hayes, A G, Birch, P J, Traynor, J R, Lawrence, A J
Format Journal Article
LanguageEnglish
Published England 01.05.1990
Subjects
Animals
Electric Stimulation
Enkephalin, Ala-MePhe-Gly
Enkephalin, D-Penicillamine (2,5)
Enkephalins - pharmacology
Guanylyl Imidodiphosphate - pharmacology
Guinea Pigs
In Vitro Techniques
Indoles - pharmacology
Male
Mice
Mice, Inbred Strains
Morphinans - pharmacology
Muscle, Smooth - drug effects
Muscle, Smooth - metabolism
Naltrexone - analogs & derivatives
Narcotic Antagonists - pharmacology
Receptors, Opioid - metabolism
Receptors, Opioid, delta
Receptors, Opioid, kappa
Receptors, Opioid, mu
Sodium - pharmacology
Vas Deferens - drug effects
Vas Deferens - metabolism
Online AccessGet more information

Cover

More Information
Summary:In the mouse vas deferens, naltrindole gave pKB values of 9.7, 8.3, and 7.5 at the delta-, mu-, and kappa-sites and in binding assays, pIC50 values of 9.6, 7.8 and 7.2 at the same sites. The affinity of naltrindole for the delta binding site was increased in the presence of sodium ions and 5'-guanylylimidophosphate. Naltrindole is, thus, a potent opioid antagonist with marked selectivity for the delta-opioid receptor.
ISSN:0022-3573
2042-7158
DOI:10.1111/j.2042-7158.1990.tb05428.x