title: Characterization of PAF receptors on human neutrophils using the specific antagonist, WEB 2086. Correlation between receptor binding and function.
abstract: The antagonism of PAF effects by WEB 2086 and the receptor binding of [3H]WEB 2086 were investigated in isolated human neutrophils. WEB 2086 inhibited PAF-induced beta-glucuronidase release and [3H]WEB 2086 bound specifically to high-affinity sites on the cells. Close concordance between affinity constants for WEB 2086 from functional and radioligand-binding studies suggests that WEB 2086 interacts with the neutrophil PAF receptors and that [3H]WEB 2086 may be a useful ligand in investigation of these receptors.
authors.affiliation: Department of Thoracic Medicine, National Heart & Lung Institute, London, England.
authors.forename: G
authors.initials: G
authors.lastname: Dent
authors.forename: D
authors.initials: D
authors.lastname: Ukena
authors.forename: P
authors.initials: P
authors.lastname: Chanez
authors.forename: G
authors.initials: G
authors.lastname: Sybrecht
authors.forename: P
authors.initials: P
authors.lastname: Barnes
mesh_terms: D001381:Azepines / Q000378:metabolism* / Q000494:pharmacology; D005966:Glucuronidase / Q000097:blood; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D009504:Neutrophils / Q000187:drug effects / Q000378:metabolism*; D010972:Platelet Activating Factor / Q000037:antagonists & inhibitors / Q000378:metabolism*; D010980:Platelet Membrane Glycoproteins; D011956:Receptors, Cell Surface / Q000187:drug effects / Q000378:metabolism*; D043562:Receptors, G-Protein-Coupled; D014227:Triazines / Q000378:metabolism* / Q000494:pharmacology; D014230:Triazoles
chemical_list: D001381:Azepines; D010972:Platelet Activating Factor; D010980:Platelet Membrane Glycoproteins; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; D014227:Triazines; D014230:Triazoles; C039351:platelet activating factor receptor; C052518:WEB 2086; D005966:Glucuronidase