Characterization of PAF receptors on human neutrophils using the specific antagonist, WEB 2086. Correlation between receptor binding and function

G Dent; D Ukena; P Chanez; G Sybrecht; P Barnes

doi:10.1016/0014-5793(89)80564-2

Characterization of PAF receptors on human neutrophils using the specific antagonist, WEB 2086. Correlation between receptor binding and function

FEBS Lett. 1989 Feb 27;244(2):365-8. doi: 10.1016/0014-5793(89)80564-2.

Authors

G Dent¹, D Ukena, P Chanez, G Sybrecht, P Barnes

Affiliation

¹ Department of Thoracic Medicine, National Heart & Lung Institute, London, England.

PMID: 2537761
DOI: 10.1016/0014-5793(89)80564-2

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Azepines / metabolism*
Azepines / pharmacology
Glucuronidase / blood
Humans
In Vitro Techniques
Kinetics
Neutrophils / drug effects
Neutrophils / metabolism*
Platelet Activating Factor / antagonists & inhibitors
Platelet Activating Factor / metabolism*
Platelet Membrane Glycoproteins*
Receptors, Cell Surface / drug effects
Receptors, Cell Surface / metabolism*
Receptors, G-Protein-Coupled*
Triazines / metabolism*
Triazines / pharmacology
Triazoles*

Substances

Azepines
Platelet Activating Factor
Platelet Membrane Glycoproteins
Receptors, Cell Surface
Receptors, G-Protein-Coupled
Triazines
Triazoles
platelet activating factor receptor
WEB 2086
Glucuronidase