Structure-activity relationships for platelet-activating factor (PAF) and analogues reveal differences between PAF receptors on platelets and macrophages

Alastair G Stewart, George Grigoriadis

Research output: Contribution to journalArticleResearchpeer-review

Abstract

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.
Original languageEnglish
Pages (from-to)299 - 308
Number of pages10
JournalJournal of Lipid Mediators
Volume4
Issue number3
Publication statusPublished - 1991

Cite this

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title = "Structure-activity relationships for platelet-activating factor (PAF) and analogues reveal differences between PAF receptors on platelets and macrophages",
abstract = "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.",
author = "Stewart, {Alastair G} and George Grigoriadis",
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pages = "299 -- 308",
journal = "Journal of Lipid Mediators",
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Structure-activity relationships for platelet-activating factor (PAF) and analogues reveal differences between PAF receptors on platelets and macrophages. / Stewart, Alastair G; Grigoriadis, George.

In: Journal of Lipid Mediators, Vol. 4, No. 3, 1991, p. 299 - 308.

Research output: Contribution to journalArticleResearchpeer-review

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T1 - Structure-activity relationships for platelet-activating factor (PAF) and analogues reveal differences between PAF receptors on platelets and macrophages

AU - Stewart, Alastair G

AU - Grigoriadis, George

PY - 1991

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N2 - 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.

AB - 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.

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