Related Experiment Videos
WEB 2086. A potent PAF antagonist exerts protective effect toward PAF-induced gastric damage
Abstract:
Single intravenous administration of platelet activating factor (PAF; 4 micrograms/kg) induced reproducible gastric damage in the conscious rat which was prevented by WEB 2086, a potent and specific PAF-antagonist. Intravenous and oral ED50s in protecting rats from gastric damage were 61 and 633 micrograms/kg, respectively. Because of the reported association between septic shock and gastrointestinal ulceration, the therapeutic potential of PAF-antagonists might be broader than previously thought.
Insights
Platelet activating factor (PAF) causes gastric damage in rats, but the antagonist WEB 2086 prevents this effect. This suggests PAF-antagonists may have broader therapeutic uses beyond initial expectations.
Area of Science:
- Pharmacology
- Gastroenterology
Background:
- Platelet activating factor (PAF) is implicated in various physiological and pathological processes.
- Septic shock is associated with gastrointestinal ulceration, suggesting a potential role for PAF in its pathogenesis.
Purpose of the Study:
- To investigate the role of PAF in inducing gastric damage in a rat model.
- To evaluate the efficacy of a specific PAF-antagonist, WEB 2086, in preventing PAF-induced gastric injury.
Main Methods:
- Administration of a single intravenous dose of PAF (4 micrograms/kg) to conscious rats.
- Assessment of gastric damage following PAF administration.
- Evaluation of the protective effects of WEB 2086 against PAF-induced gastric damage, determining intravenous and oral ED50 values.
Main Results:
- Single intravenous PAF administration reliably induced gastric damage in conscious rats.
- WEB 2086, a potent and specific PAF-antagonist, effectively prevented PAF-induced gastric damage.
- The ED50 for intravenous WEB 2086 was 61 micrograms/kg, and for oral administration, it was 633 micrograms/kg.
Conclusions:
- PAF is a potent inducer of gastric damage in rats.
- PAF-antagonists, such as WEB 2086, demonstrate significant therapeutic potential in preventing gastric injury.
- The findings suggest that PAF-antagonists may be beneficial in conditions involving gastrointestinal ulceration, including potentially those related to septic shock.