Characterization of specific binding sites for PAF in the iris and ciliary body of rabbit.
The protective effect exerted by BN 52021 a specific PAF-receptor antagonist in experimentally induced ocular inflammatory disorders led us to investigate the possible presence of specific receptors for PAF in rabbit iris and ciliary body. Two classes of PAF binding sites were found in isolated iris and ciliary process of pigmented rabbit eyes: a high affinity site Kd1 congruent to 4.9 +/- 0.47 nM, Bmax1 congruent to 3.17 +/- 0.50 pmoles/mg protein, a low affinity sites Kd2 congruent to 11.6 +/- 0.33 nM, Bmax2 congruent to 12.46 +/- 2.3 pmoles/mg protein for iris. The specific binding was not affected by lyso-PAF the biologically inactive precursor and metabolite of PAF, up to 10(-6) M; inhibition by unlabelled PAF demonstrated a biphasic curve partially antagonized by BN 52021. The present results demonstrate the presence of specific binding sites for PAF in rabbit eyes which could mediate the action of this mediator in eye inflammatory processes and explain the protective effect observed with BN 52021.
Domingo
M T
MT
Institut Henri Beaufour LES ULIS, France.
Chabrier
P E
PE
Van Delft
J L
JL
Verbeij
N L
NL
Van Haeringen
N J
NJ
Braquet
P
P
D000818:Animals; D001667:Binding, Competitive; D002924:Ciliary Body / Q000032:analysis*; D004224:Diterpenes; D005260:Female; D046934:Ginkgolides; D007498:Iris / Q000032:analysis*; D007700:Kinetics; D007783:Lactones / Q000494:pharmacology; D008297:Male; D010972:Platelet Activating Factor / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors / Q000378:metabolism / Q000494:pharmacology; D010980:Platelet Membrane Glycoproteins; D011817:Rabbits; D011956:Receptors, Cell Surface / Q000032:analysis* / Q000187:drug effects / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled; D014316:Tritium
D004224:Diterpenes; D046934:Ginkgolides; D007783:Lactones; C029271:O-deacetyl platelet activating factor; D010972:Platelet Activating Factor; D010980:Platelet Membrane Glycoproteins; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; C039351:platelet activating factor receptor; D014316:Tritium; C045856:ginkgolide B