Inhibition of cutaneous and platelet responses to platelet-activating factor by oral WEB 2086 in man. 1991

J P Hayes, and S M Ridge, and S Griffith, and P J Barnes, and K F Chung
Department of Thoracic Medicine, National Heart & Lung Institute, London, England.

WEB 2086, an antagonist of platelet-activating factor (PAF), was assessed against the cutaneous response in vivo and the aggregation of platelets ex vivo induced by PAF in a double-blind, placebo-controlled, crossover study in 12 normal male volunteers. Wheal-and-flare responses to intradermal PAF (200 ng) and histamine (1 microgram) were measured 1 hour after placebo or control administration. Wheal volumes were significantly reduced by 66% +/- 8.7% (mean +/- SEM), 86% +/- 8.3%, and 90% +/- 6.0% after 10, 40, and 100 mg of WEB 2086 compared to placebo administration (p less than 0.005). Flare responses were correspondingly inhibited by 66% +/- 8.3%, 82% +/- 8.7%, and 84% +/- 7.8% at 10, 40, and 100 mg of WEB 2086, respectively. Cutaneous responses to histamine were unaffected. Ex vivo platelet responses to PAF were significantly inhibited at all three doses of WEB 2086. Oral WEB 2086 is a potent and specific inhibitor of cutaneous and platelet responses to PAF in man.

UI MeSH Term Description Entries
D007271 Injections, Intradermal The forcing into the skin of liquid medication, nutrient, or other fluid through a hollow needle, piercing the top skin layer. Intradermal Injections,Injection, Intradermal,Intradermal Injection
D008297 Male Males
D010919 Placebos Any dummy medication or treatment. Although placebos originally were medicinal preparations having no specific pharmacological activity against a targeted condition, the concept has been extended to include treatments or procedures, especially those administered to control groups in clinical trials in order to provide baseline measurements for the experimental protocol. Sham Treatment
D010972 Platelet Activating Factor A phospholipid derivative formed by PLATELETS; BASOPHILS; NEUTROPHILS; MONOCYTES; and MACROPHAGES. It is a potent platelet aggregating agent and inducer of systemic anaphylactic symptoms, including HYPOTENSION; THROMBOCYTOPENIA; NEUTROPENIA; and BRONCHOCONSTRICTION. AGEPC,Acetyl Glyceryl Ether Phosphorylcholine,PAF-Acether,Phosphorylcholine, Acetyl Glyceryl Ether,1-Alkyl-2-acetyl-sn-glycerophosphocholine,Platelet Aggregating Factor,Platelet Aggregation Enhancing Factor,Platelet-Activating Substance,Thrombocyte Aggregating Activity,1 Alkyl 2 acetyl sn glycerophosphocholine,Aggregating Factor, Platelet,Factor, Platelet Activating,PAF Acether,Platelet Activating Substance
D010974 Platelet Aggregation The attachment of PLATELETS to one another. This clumping together can be induced by a number of agents (e.g., THROMBIN; COLLAGEN) and is part of the mechanism leading to the formation of a THROMBUS. Aggregation, Platelet
D010975 Platelet Aggregation Inhibitors Drugs or agents which antagonize or impair any mechanism leading to blood platelet aggregation, whether during the phases of activation and shape change or following the dense-granule release reaction and stimulation of the prostaglandin-thromboxane system. Antiaggregants, Platelet,Antiplatelet Agent,Antiplatelet Agents,Antiplatelet Drug,Blood Platelet Aggregation Inhibitor,Blood Platelet Antagonist,Blood Platelet Antiaggregant,PAR-1 Antagonists,Platelet Aggregation Inhibitor,Platelet Antagonist,Platelet Antagonists,Platelet Antiaggregant,Platelet Antiaggregants,Platelet Inhibitor,Protease-Activated Receptor-1 Antagonists,Antiplatelet Drugs,Blood Platelet Aggregation Inhibitors,Blood Platelet Antagonists,Blood Platelet Antiaggregants,Platelet Inhibitors,Agent, Antiplatelet,Aggregation Inhibitor, Platelet,Antagonist, Blood Platelet,Antagonist, Platelet,Antiaggregant, Blood Platelet,Antiaggregant, Platelet,Drug, Antiplatelet,Inhibitor, Platelet,Inhibitor, Platelet Aggregation,PAR 1 Antagonists,Platelet Antagonist, Blood,Platelet Antiaggregant, Blood,Protease Activated Receptor 1 Antagonists
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004311 Double-Blind Method A method of studying a drug or procedure in which both the subjects and investigators are kept unaware of who is actually getting which specific treatment. Double-Masked Study,Double-Blind Study,Double-Masked Method,Double Blind Method,Double Blind Study,Double Masked Method,Double Masked Study,Double-Blind Methods,Double-Blind Studies,Double-Masked Methods,Double-Masked Studies,Method, Double-Blind,Method, Double-Masked,Methods, Double-Blind,Methods, Double-Masked,Studies, Double-Blind,Studies, Double-Masked,Study, Double-Blind,Study, Double-Masked
D006632 Histamine An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter. Ceplene,Histamine Dihydrochloride,Histamine Hydrochloride,Peremin
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man

Related Publications

J P Hayes, and S M Ridge, and S Griffith, and P J Barnes, and K F Chung
January 1992, International archives of allergy and immunology,
J P Hayes, and S M Ridge, and S Griffith, and P J Barnes, and K F Chung
January 1990, Methods in enzymology,
J P Hayes, and S M Ridge, and S Griffith, and P J Barnes, and K F Chung
June 1993, Thorax,
J P Hayes, and S M Ridge, and S Griffith, and P J Barnes, and K F Chung
February 1994, Journal of molecular and cellular cardiology,
J P Hayes, and S M Ridge, and S Griffith, and P J Barnes, and K F Chung
September 1996, Zentralblatt fur Veterinarmedizin. Reihe A,
J P Hayes, and S M Ridge, and S Griffith, and P J Barnes, and K F Chung
February 1993, American journal of veterinary research,
J P Hayes, and S M Ridge, and S Griffith, and P J Barnes, and K F Chung
June 1987, The Journal of pharmacology and experimental therapeutics,
J P Hayes, and S M Ridge, and S Griffith, and P J Barnes, and K F Chung
October 1989, European journal of pharmacology,
J P Hayes, and S M Ridge, and S Griffith, and P J Barnes, and K F Chung
January 1990, The European respiratory journal,
J P Hayes, and S M Ridge, and S Griffith, and P J Barnes, and K F Chung
January 1996, Annals of vascular surgery,
Copied contents to your clipboard!