Structure-activity relationships for platelet-activating factor (PAF) and analogues reveal differences between PAF receptors on platelets and macrophages.
Analogues of PAF were examined for their potency in stimulating either platelet aggregation or macrophage superoxide anion generation. Modification of either the alkyl side-chain or the acetyl side-chain increased the relative potency of PAF analogues in macrophages, but all these compounds were more active in platelets. However, an analogue of PAF with an increased inter-ionic distance in the polar head group, hexanolamine PAF, showed a greater potency in macrophages than platelets. The latter compound also appeared to act as a partial agonist in both rabbit platelets and guinea-pig macrophages, but not in guinea-pig platelets. Differences in the rank order of potency of the PAF analogues in stimulating these cell elements suggest that platelet and macrophage PAF receptors differ.
Stewart
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AG
Department of Physiology, University of Melbourne, Parkville, Victoria, Australia.
Grigoriadis
G
G
D000818:Animals; D001792:Blood Platelets / Q000502:physiology*; D006168:Guinea Pigs; D008262:Macrophage Activation; D008264:Macrophages / Q000378:metabolism*; D008297:Male; D010972:Platelet Activating Factor / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D010974:Platelet Aggregation; D010980:Platelet Membrane Glycoproteins; D011817:Rabbits; D011956:Receptors, Cell Surface / Q000378:metabolism*; D043562:Receptors, G-Protein-Coupled; D013329:Structure-Activity Relationship; D013481:Superoxides / Q000378:metabolism
D010972:Platelet Activating Factor; D010980:Platelet Membrane Glycoproteins; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; C039351:platelet activating factor receptor; D013481:Superoxides