Identification and characterization of leukotriene D4 receptors in adult and fetal human lung

Biochem Pharmacol. 1985 Dec 15;34(24):4311-7. doi: 10.1016/0006-2952(85)90290-4.

Abstract

Leukotriene D4 (LTD4) receptors were identified and characterized in adult and fetal human lung membranes. Macroscopically normal adult lung tissue was selected from seventeen surgical biopsy specimens, and twenty-seven fetal lung samples were obtained from therapeutic abortions. Binding assays were performed using pooled adult or fetal human lung membranes at 30 degrees under conditions which prevented metabolism of [3H]LTD4. Specific binding reached equilibrium within 30 min, remained constant for 60 min, was enhanced by Mg2+, and was inhibited by Na+ and guanyl-5'-yl-imidodiphosphate. Computer-assisted analyses of saturation binding data showed a single class of binding sites with similar apparent Kd (0.15 +/- 0.09 and 0.12 +/- 0.003 nM) and Bmax (68 +/- 29 and 62 +/- 14 fmoles/mg protein) values for adult and fetal samples respectively. Competition binding studies with [3H]LTD4 showed the same rank order potency for adult and fetal lung receptors (5S, 6R-LTD4 greater than 5S, 6R-LTD1 greater than 5R, 6S-LTD4 greater than 5S,6R-LTE4 greater than FPL 55712). A comparison of the receptor binding affinities of these compounds with their smooth muscle contractile agonist (pD2) and antagonist (-log[KB]) activities in guinea pig lung and trachea showed a good correlation (r = 0.88), suggesting that the saturable, high-affinity, stereoselective [3H]LTD4 specific binding sites identified in human lung may be physiologically relevant receptor moieties.

MeSH terms

  • Adult
  • Binding, Competitive
  • Chromones / pharmacology
  • Female
  • Fetus / analysis*
  • Humans
  • In Vitro Techniques
  • Lung / analysis*
  • Lung / drug effects
  • Lung / metabolism
  • Muscle Contraction / drug effects
  • Pregnancy
  • Radioligand Assay
  • Receptors, Cell Surface / analysis*
  • Receptors, Leukotriene
  • Receptors, Prostaglandin / analysis*
  • SRS-A / metabolism
  • Tritium

Substances

  • Chromones
  • Receptors, Cell Surface
  • Receptors, Leukotriene
  • Receptors, Prostaglandin
  • SRS-A
  • Tritium
  • FPL 55712