Characterization of PAF receptors on human neutrophils using the specific antagonist, WEB 2086. Correlation between receptor binding and function.
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.
Dent
G
G
Department of Thoracic Medicine, National Heart & Lung Institute, London, England.
Ukena
D
D
Chanez
P
P
Sybrecht
G
G
Barnes
P
P
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
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