Kinetic parameters of antagonism by the delta opioid receptor selective peptide antagonist Boc-Tyr-Pro-Gly-Phe-Leu-Thr against selective and non-selective agonists in the mouse vas deferens

A. Rónai, A. Magyar, K. Medzihradszky

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

The kinetic parameters of antagonism by the delta opioid receptor selective antagonist N-t-Boc-Tyr-Pro-Gly-Phe-Leu-Thr, obtained by using moderately selective or selective agonists, were compared in the mouse vas deferens bioassay. The apparent affinity for the preferred receptor type was 6.8 times higher when selective agonist was used, resulting in a Ke of 81.4 nM (66.3-99.9, n = 6) against [D-Ala2, D-Leu5]-enkephalin, with a 3700-fold delta over mu or kappa selectivity ratio.

Original languageEnglish
Pages (from-to)127-129
Number of pages3
JournalNeuropeptides
Volume25
Issue number2
DOIs
Publication statusPublished - 1993

Fingerprint

delta Opioid Receptor
Vas Deferens
Narcotic Antagonists
Bioassay
Enkephalins
Kinetic parameters
Biological Assay
Peptides
(1,1-dimethylethoxy)carbonyl-tyrosyl-prolyl-glycyl-phenylalanyl-leucyl-threonine
Ala(2)-enkephalinamide-met

ASJC Scopus subject areas

  • Biochemistry
  • Endocrinology
  • Endocrinology, Diabetes and Metabolism
  • Clinical Neurology
  • Neuroscience(all)
  • Cellular and Molecular Neuroscience

Cite this

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abstract = "The kinetic parameters of antagonism by the delta opioid receptor selective antagonist N-t-Boc-Tyr-Pro-Gly-Phe-Leu-Thr, obtained by using moderately selective or selective agonists, were compared in the mouse vas deferens bioassay. The apparent affinity for the preferred receptor type was 6.8 times higher when selective agonist was used, resulting in a Ke of 81.4 nM (66.3-99.9, n = 6) against [D-Ala2, D-Leu5]-enkephalin, with a 3700-fold delta over mu or kappa selectivity ratio.",
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AU - Magyar, A.

AU - Medzihradszky, K.

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AB - The kinetic parameters of antagonism by the delta opioid receptor selective antagonist N-t-Boc-Tyr-Pro-Gly-Phe-Leu-Thr, obtained by using moderately selective or selective agonists, were compared in the mouse vas deferens bioassay. The apparent affinity for the preferred receptor type was 6.8 times higher when selective agonist was used, resulting in a Ke of 81.4 nM (66.3-99.9, n = 6) against [D-Ala2, D-Leu5]-enkephalin, with a 3700-fold delta over mu or kappa selectivity ratio.

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