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 Citations (Scopus)

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

Fingerprint

Guanine Nucleotides
Opioid Receptors
Sodium
Guanylyl Imidodiphosphate
naltrindole
Vas Deferens
GTP-Binding Proteins
Inhibitory Concentration 50
Brain
Opioid Analgesics
Ligands
BW 373U86
Ala(2)-enkephalinamide-met
deltorphin

Keywords

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

ASJC Scopus subject areas

  • Pharmacology

Cite this

Binding of BW 373U86, a non-peptidic δ opioid receptor agonist, is not regulated by guanine nucleotides and sodium. / Wild, Kenneth D.; Fang, Lei; McNutt, Robert W.; Chang, Kwen Jen; Toth, Geza; Borsodi, Ana; Yamamura, Henry I.; Porreca, Frank.

In: European Journal of Pharmacology: Molecular Pharmacology, Vol. 246, No. 3, 15.08.1993, p. 289-292.

Research output: Contribution to journalArticle

Wild, Kenneth D. ; Fang, Lei ; McNutt, Robert W. ; Chang, Kwen Jen ; Toth, Geza ; Borsodi, Ana ; Yamamura, Henry I. ; Porreca, Frank. / Binding of BW 373U86, a non-peptidic δ opioid receptor agonist, is not regulated by guanine nucleotides and sodium. In: European Journal of Pharmacology: Molecular Pharmacology. 1993 ; Vol. 246, No. 3. pp. 289-292.
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N2 - 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.

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