Corpus ID: 21467051

Binding of radiolabeled high affinity antagonist to leukotriene D4 receptor in guinea pig lung membranes: interconversion of agonist-receptor binding affinity states.

  title={Binding of radiolabeled high affinity antagonist to leukotriene D4 receptor in guinea pig lung membranes: interconversion of agonist-receptor binding affinity states.},
  author={Brian P. O'sullivan and Seymour Mong},
  journal={Molecular pharmacology},
  volume={35 6},
The kinetic parameters and the pharmacological specificity of a high affinity leukotriene D4 (LTD4) receptor antagonist, ICI-198615, binding to guinea pig lung membranes were characterized. Binding of [3H]ICI-198615 to the membranes was rapid and displaceable with excess ICI-198615. The specific binding of [3H] ICI-198615 was dependent upon the concentration of membrane protein. Monovalent cations (Na+, Li+, and Cs+), divalent cations (Mg2+, Ca2+, and Mn2+), and guanine nucleotides did not… Expand
Heterogeneity of binding sites for ICI 198,615 in human lung parenchyma.
A heterogeneity of binding sites for ICI 198,615 in membranes from human lung parenchyma is indicated and this novel compound is a very potent and selective antagonist of LTD4 receptors in this tissue. Expand
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Pharmacological characterization of the cysteinyl‐leukotriene antagonists CGP 45715A (iralukast) and CGP 57698 in human airways in vitro
The results of the present in vitro investigation indicate that iralukast and CGP 57698 are potent antagonists of LTD4 in human airways, with affinities in the nanomolar range, similar to those obtained for ICI 204,219 and ONO 1078, two of the most clinically advanced CysLT receptor antagonists. Expand
Binding to cysteinyl-leukotriene receptors.
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Studies on molecular properties and functional regulation of terminal leukotriene C4 synthases and cysteinyl-leukotriene receptor signalling in human endothelium
The transformation of the unstable intermediate leukotriene (LT) A4 into the glutathione conjugate LTC4, the parent compound of LTD4 and LTE4, is catalysed by leukotriene C4 synthase (LTC4S) as wellExpand
Chemical Tools for Studying Lipid-Binding Class A G Protein–Coupled Receptors
This study reviews the radioligands, fluorescent ligands, covalent ligand, and antibodies that have been used to study these lipid-binding receptors and describes the characteristics and design rationale along with in vitro and in vivo applications. Expand
Novel Inhibitors of Leukotrienes
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Evaluation of the pharmacological activity of the pure cysteinyl-leukotriene receptor antagonists CGP 45715A (iralukast) and CGP 57698 in human airways.
Cysteinyl-containing leukotrienes (cysteinyl-LTs) produce bronchoconstriction, mucus hypersecretion, and pro-inflammatory effects (Dahlen et al., 1980; Dahlen et al., 1981; Foster C von Sprecher etExpand
The cysteinyl leukotriene receptors.
  • Jilly F. Evans
  • Chemistry, Medicine
  • Prostaglandins, leukotrienes, and essential fatty acids
  • 2003
The cysteinyl leukotriene receptors are putative 7 transmembrane spanning G protein-coupled receptors (GPCRs) of the rhodopsin subfamily of GPCRs and the properties of these receptors agrees well with previous pharmacological CysLT agonist and antagonist characterizations. Expand