Studies in vitro with ICI 174, 864, [D-Pen2, D-Pen5]-enkephalin (DPDPE) and [D-Ala2, NMePhe4, Gly-ol]-enkephalin (DAGO)

Lane D. Hirning, Henry I. Mosberg, Robin Hurst, Victor J Hruby, Thomas F. Burks, Frank Porreca

Research output: Contribution to journalArticle

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Abstract

The interactions of a proposed, selective delta receptor antagonist (ICI 174, 864) and selective agonists at mu and delta receptors, [D-Ala2, NMePhe4, Gly-ol]-enkephalin (DAGO) and [D-Pen2, D-Pen5]-enkephalin (DPDPE), respectively, have been studied using the electrically-stimulated mouse isolated vas deferens (MVD) and the guinea-pig isolated ileum (GPI). Incubation of increasing concentrations of ICI 174, 864 (10, 30, 100 and 300 nM) produced a dose-related and parallel rightward displacement of the DPDPE dose-response curve in the MVD. In contrast, ICI 174, 864 (300-3000 nM) failed to affect the DAGO dose-response curve in the same tissue. Analysis of the DPDPE-ICI 174, 864 interaction in the MVD using the pA2 method revealed a Schild plot slope of -0.68 suggesting the involvement of more than one population of receptors. ICI 174, 864 (300 nM) failed to antagonize DPDPE in the GPI at doses up to 30 uM. These results suggest that (a) ICI 174, 864 acts as a selective delta antagonist in the MVD; (b) DPDPE interacts with mu receptors in the MVD but only at very high concentrations, and (c) delta receptors appear not to be of functional importance in the GPI.

Original languageEnglish (US)
Pages (from-to)383-386
Number of pages4
JournalNeuropeptides
Volume5
Issue number4-6
DOIs
StatePublished - 1985

Fingerprint

D-Penicillamine (2,5)-Enkephalin
Enkephalins
Vas Deferens
delta Opioid Receptor
Ileum
Guinea Pigs
mu Opioid Receptor
In Vitro Techniques
Tissue
Population

ASJC Scopus subject areas

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

Cite this

Studies in vitro with ICI 174, 864, [D-Pen2, D-Pen5]-enkephalin (DPDPE) and [D-Ala2, NMePhe4, Gly-ol]-enkephalin (DAGO). / Hirning, Lane D.; Mosberg, Henry I.; Hurst, Robin; Hruby, Victor J; Burks, Thomas F.; Porreca, Frank.

In: Neuropeptides, Vol. 5, No. 4-6, 1985, p. 383-386.

Research output: Contribution to journalArticle

Hirning, Lane D. ; Mosberg, Henry I. ; Hurst, Robin ; Hruby, Victor J ; Burks, Thomas F. ; Porreca, Frank. / Studies in vitro with ICI 174, 864, [D-Pen2, D-Pen5]-enkephalin (DPDPE) and [D-Ala2, NMePhe4, Gly-ol]-enkephalin (DAGO). In: Neuropeptides. 1985 ; Vol. 5, No. 4-6. pp. 383-386.
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