2-(3-Pyridyl)thiazolidine-4-carboxamides. 1. Novel Orally Active Antagonists of Platelet-Activating Factor (PAF).
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چکیده
منابع مشابه
Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF).
Rupatadine (UR-12592, 8-chloro-6, 11-dihydro-11-[1-[(5-methyl3-pyridinyl) methyl]-4-piperidinylidene]-5H-benzo[5,6]-cyclohepta[1,2b]pyridine ) is a novel compound that inhibits both platelet-activating factor (PAF) and histamine (H1) effects through its interaction with specific receptors (Ki(app) values against [3H]WEB-2086 binding to rabbit platelet membranes and [3H]-pyrilamine binding to gu...
متن کاملPreparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.
Ginkgolides are structurally unique constituents of Ginkgo biloba extracts and are known antagonists of the platelet-activating factor (PAF) receptor. Ginkgolide C is 25-fold less potent than ginkgolide B as a PAF receptor antagonist, due to the presence of the 7beta-OH. Recently, we found that 7alpha-fluoro ginkgolide B was equipotent to ginkgolide B underlining the critical importance of the ...
متن کاملEffect of platelet-activating factor (PAF) on human platelets.
The effect of pure synthetic PAF (1-0-alkyl-2-acetyl-sn-glycero-3-phosphorylcholine) was studied in human platelets. PAF (0.2--2.0 micrograms/ml) produced a dose-dependent aggregation in human platelet-rich plasma (PRP) or platelet suspension obtained by gel-filtration (GFP). In addition, PAF (0.8 microgram/ml) induced secretion of 14C-serotonin (45% +/- 10%; mean +/- SD, n = 9) and platelet fa...
متن کاملPlatelet-activating factor and platelet-activating factor antagonists in acute pancreatitis.
INTRODUCTION Acute pancreatitis causes platelet-activating factor (PAF) to be released which induces systemic effects that contribute to circulatory disturbances and multiple organ failure. PAF has also been implicated as a key mediator in the progression of severe acute pancreatitis, which can lead to complications and unacceptably high mortality rates. MODE OF ACTION OF PAF IN ACUTE PANCREA...
متن کاملPlatelet-activating factor (PAF)-induced rhinitis and involvement of PAF in allergic rhinitis in guinea pigs.
The effects of inhaled PAF on the guinea pig nasal mucosa were investigated. Intranasal pressure (INP) was recorded as an index of intranasal resistance. To access the capillary premeability of nasal mucosa, exudation of Evans blue into the nasal lavage fluid was determined. Inhalations of histamine and PAF markedly and significantly increased INP and dye exudation into the nasal cavities. The ...
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ژورنال
عنوان ژورنال: Chemical and Pharmaceutical Bulletin
سال: 1997
ISSN: 0009-2363,1347-5223
DOI: 10.1248/cpb.45.1659