Binding of BW 373U86, a non-peptidic δ opioid receptor agonist, is not regulated by guanine nucleotides and sodium

Kenneth D. Wild, Lei Fang, Robert W. McNutt, Kwen Jen Chang, Geza Toth, Ana Borsodi, Henry I. Yamamura, Frank Porreca

Research output: Contribution to journalArticle

16 Scopus citations

Abstract

BW 373U86 is a novel, non-peptidic δ-opioid receptor ligand with agonist properties in mouse brain and in the mouse isolated vas deferens. The sensitivity of BW 373U86, and of the peptidic δ-opioid agonists [d-Pen2, D-Pen5]enkephalin (DPDPE) and [d-Ala2,Glu4]deltorphin, to regulation by guanine nucleotides and sodium was evaluated in competition studies against the 5 selective radioligand [3H]naltrindole. The IC50 values for DPDPE and [d-Ala2,Glu4]deltorphin were significantly increased in brain and mouse vas deferens in the presence of Gpp(NH)p and NaCl. In contrast, the IC50 values for BW 373U86 were not altered in the presence of Gpp(NH)p and NaCl in either tissue. The data indicate that the agonist properties of BW 373U86 may not be affected by the supposed uncoupling of the α-subunit of the G-protein from a receptor thought to be G-protein linked.

Original languageEnglish (US)
Pages (from-to)289-292
Number of pages4
JournalEuropean Journal of Pharmacology: Molecular Pharmacology
Volume246
Issue number3
DOIs
StatePublished - Aug 15 1993

Keywords

  • BW 373U86
  • Guanine nucleotides
  • Opioids
  • Radioligand binding
  • δ-Opioid receptors

ASJC Scopus subject areas

  • Pharmacology

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