A comparison of the actions of platelet activating factor (PAF) antagonists WEB 2170 and WEB 2086 in the horse.
Abstract: The effects of the selective platelet activating factor (PAF) receptor antagonist WEB 2170 on PAF-induced responses in equine cells and tissues have been examined and compared with those of WEB 2086. In initial experiments WEB 2170 was shown to inhibit in vitro platelet aggregation in a dose-dependent, competitive reversible manner (pA2 = 7.21). Co-administration of the antagonists with either PAF or histamine also inhibited PAF, but not histamine, induced wheal formation and PAF-induced neutrophil accumulation in vivo in equine skin. Intravenous (i.v.) administration of both drugs at a dose of 0.1 mg/kg blocked PAF-induced ex vivo platelet aggregation. The inhibition produced by WEB 2170 was greater and, at 30 min, this drug also reduced the slope and maximal response. Wheal formation in the skin was significantly inhibited for up to 6 h by WEB 2170 administered i.v., the reduction being more prolonged than that obtained with WEB 2086. Neutrophil accumulation in the skin was also significantly reduced for up to 24 h by WEB 2170, whilst no significant inhibition was produced by WEB 2086. These results demonstrate that WEB 2170, like WEB 2086, is an effective antagonist of PAF in the horse. Moreover, when given i.v., WEB 2170 appears to be a more potent PAF inhibitor than WEB 2086.
Publication Date: 1993-12-01 PubMed ID: 8126765DOI: 10.1111/j.1365-2885.1993.tb00214.xGoogle Scholar: Lookup
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- Comparative Study
- Journal Article
- Research Support
- Non-U.S. Gov't
Summary
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This study compares the impacts of two selective platelet activating factor (PAF) receptor antagonists, WEB 2170 and WEB 2086, on horse cells and tissues. The research indicates that WEB 2170, administered intravenously (IV), may be a more effective PAF inhibitor than WEB 2086.
Introduction to the Research Objectives
- This research intends to examine and contrast the effects of two PAF antagonists: WEB 2170 and WEB 2086, on horse cells and tissues.
- The objective is to find out which of the two drugs is more useful in blocking PAF-related responses.
Research Methods
- Initial experiments demonstrated that WEB 2170 inhibits in vitro (in a controlled lab environment) platelet aggregation in a dose-dependent, reversible manner.
- The combined administration of these antagonists with either PAF or histamine was used to observe their ability to inhibit PAF and histamine-induced wheel formations.
- Both drugs were administered intravenously (i.v) at a dose of 0.1 mg/kg to block PAF-induced ex vivo (outside the body) platelet aggregation.
Key Research Findings
- WEB 2170 effectively inhibited PAF, but not histamine-induced wheel formations and neutrophil accumulation in equine skin.
- When administered intravenously, WEB 2170 blocked PAF-induced ex vivo platelet aggregation more efficiently than WEB 2086, reducing both the slope and maximal response at 30 minutes post administration.
- IV administration of WEB 2170 resulted in significant inhibition of wheel formation in the skin for up to 6 hours, a longer effect than WEB 2086.
- Neutrophil accumulation in the skin was significantly reduced for up to 24 hours by WEB 2170, while WEB 2086 failed to produce significant inhibition.
- These results suggest that both WEB 2170 and WEB 2086 are effective antagonists of PAF in horses, but the former seems to be more potent when administered IV.
Conclusion of the Research
- The research concludes that, when administered intravenously, WEB 2170 emerges as a more compelling inhibitor of PAF responses in horse tissues than WEB 2086.
- This indicates that WEB 2170 could be an essential tool in the treatment or study of conditions related to PAF in equine healthcare.
Cite This Article
APA
Foster AP, Cunningham FM, Andrews MJ, Lees P.
(1993).
A comparison of the actions of platelet activating factor (PAF) antagonists WEB 2170 and WEB 2086 in the horse.
J Vet Pharmacol Ther, 16(4), 477-487.
https://doi.org/10.1111/j.1365-2885.1993.tb00214.x Publication
Researcher Affiliations
- Department of Veterinary Basic Sciences, Royal Veterinary College (University of London), Hatfield, Herts, UK.
MeSH Terms
- Animals
- Azepines / pharmacology
- Capillary Permeability / drug effects
- Dose-Response Relationship, Drug
- Histamine / pharmacology
- Horses / blood
- Horses / metabolism
- Leukocyte Count / veterinary
- Male
- Neutrophils / drug effects
- Platelet Activating Factor / antagonists & inhibitors
- Platelet Aggregation / drug effects
- Platelet Aggregation Inhibitors / pharmacology
- Skin / cytology
- Triazoles / pharmacology
Citations
This article has been cited 1 times.- Foster AP, Lees P, Cunningham FM. Actions of PAF receptor antagonists in horses with the allergic skin disease sweet itch. Inflamm Res 1995 Oct;44(10):412-7.
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