Binding of [3H](+)-BW373U86 to delta-opioid receptors in rat brain membranes.

Journal Article (Journal Article)

A tritiated form of the non-peptide delta-opioid receptor agonist (+)-BW373U86 ((+)-4-((alpha-R)-alpha-((2S,5R)-4-allyl-2, 5-dimethyl-l-piperazinyl)-3-hydroxybenzyl)-N,N-diethylbenzamide) was synthesized and its binding characteristics studied. [3H](+)-BW373U86 bound with subnanomolar affinity to rat brain membranes and was displaced most effectively by ligands selective for delta-opioid receptors. Naltrindole, naltriben, and 7-benzylidenenaltrexone exhibited apparent inhibition constants of 0.06, 1.54, and 4.49 nM, respectively, while mu- or kappa-selective ligands showed little affinity for this site. [3H](+)-BW373U86 binding was sensitive to the presence of guanine nucleotides; GDP caused a 3-fold decrease and 5'-guanylyl-imidodiphosphate (Gpp[NH]p) caused a 25% increase in binding affinity.

Full Text

Duke Authors

Cited Authors

  • Campa, MJ; McNutt, RW; Hill, JA; Patz, EF; Chang, KJ

Published Date

  • August 29, 1996

Published In

Volume / Issue

  • 310 / 2-3

Start / End Page

  • 263 - 267

PubMed ID

  • 8884225

International Standard Serial Number (ISSN)

  • 0014-2999

Digital Object Identifier (DOI)

  • 10.1016/0014-2999(96)00483-9


  • eng

Conference Location

  • Netherlands