Platelet-Activating Factor Antagonists: Scientific Background and Possible Clinical Applications

Koltai, M.; Guinot, Philippe; Hosford, David; Pg, Braquet

doi:10.1016/s1054-3589(08)60494-9

Cited by 35 publications

(1 citation statement)

References 263 publications

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“…Control animals received equal volumes of saline; the research technicians responsible for the feeding protocol were unaware of the treatment groups. The antagonists tested included WEB 2170 {Bepafant, 5‐(2‐chloro‐phenyl)‐3,4‐dihydro‐10‐methyl ‐ 3 ‐ [(4 ‐ morpholinyl)carbonyl] ‐ 2 H, 7 H ‐cyclopenta (4,5)thieno[3,2‐ f ][1,2,4 triazolo‐[4,3‐ a ][1,4]diazepine} and WEB 2086 {Apafant; (3,[4‐(‐chlorophenyl)‐9‐methyl‐6 H ‐thieno[3,2‐ f ][1,2,4]‐triazolo‐[4,3‐ a ][1,4]‐diazepine‐2‐yl]‐1‐(4‐morpholinyl)‐1‐propanone} given via orogastric tube twice daily (generous gift from H. Heuer, Behringer Ingelheim, KG) (19,20). These compounds are triazolam derivatives that exert potent competitive blockade on the PAF receptor.…”

Section: Methodsmentioning

confidence: 99%

The Platelet‐Activating Factor Receptor Antagonist WEB 2170 Prevents Neonatal Necrotizing Enterocolitis in Rats

Caplan,

Hedlund,

Adler

et al. 1997

J. pediatr. gastroenterol. nutr.

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Background:To evaluate the role of platelet‐activating factor (PAF) in a neonatal rat model of necrotizing enterocolitis (NEC).Methods:NEC was reproduced in newborn rats following exposure to formula feeding, asphyxia, and bacterial colonization. The role of endogenous PAF in neonatal NEC was studied by pretreating animals with PAF receptor antagonists (WEB 2170 and WEB 2086) and by measuring intestinal PAF content in animals with NEC, WEB‐treated animals, and controls.Results:We found that WEB 2170 (dosed using 10 mg/kg in a.m. and 30 mg/kg in p.m.) markedly reduced the incidence of NEC (3/17 vs. 14/18 control; p < 0.001) and death (6/17 vs. 17/18 control; p < 0.001) compared with saline‐treated animals. Although lower WEB 2170 doses prevented NEC, neither fourfold higher dosing with WEB 2170 nor similar dosing with WEB 2086 affected the incidence of disease in this study. PAF content in intestine was elevated in NEC animals (270 ± 80 pg/g) compared with WEB 2170‐treated animals (0 pg/g) and maternally fed controls (70 ± 50 pg/g).Conclusions:The data support the role of PAF in the final common pathway of neonatal NEC.

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Section: Methodsmentioning

confidence: 99%

The Platelet‐Activating Factor Receptor Antagonist WEB 2170 Prevents Neonatal Necrotizing Enterocolitis in Rats

Caplan,

Hedlund,

Adler

et al. 1997

J. pediatr. gastroenterol. nutr.

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The Effect of 3‐Month Ingestion of Ginkgo biloba Extract on Pancreatic β‐Cell Function in Response to Glucose Loading in Normal Glucose Tolerant Individuals

Kudolo

2000

The Journal of Clinical Pharma

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Ginkgo biloba extract is ingested on a chronic basis for enhancing mental focus and improving cognitive function in the elderly. This study was undertaken to determine the effect of Ginkgo biloba extract on glucose-stimulated pancreatic beta-cell function in normal glucose-tolerant individuals. Twenty individuals (14 females and 6 males, ages 21-57 years) underwent a 2-hour 75 g oral glucose tolerance test (OGTT) before and after ingestion of Ginkgo biloba extract (120 mg/day at bedtime) for 3 months. Ginkgo biloba extract ingestion caused a decrease in systolic blood pressure from 125 +/- 15 to 118 +/- 12 mmHg (p < 0.05) and in diastolic blood pressure from 86 +/- 10 to 68 +/- 10 (p < 0.01). Fasting plasma insulin and C-peptide were increased, and the insulin and C-peptide areas under the curve during the OGTT changed from 136 +/- 55 to 162 +/- 94 microU/ml/h (p = 0.1232) and 9.67 +/- 5.34 to 16.88 +/- 5.20 ng/ml/h (p < 0.001), respectively. The observed dissimilar insulin/C-peptide response curves may be due to Ginkgo biloba-induced increase of the rate of insulin metabolic clearance.

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Metabolism and Functions of Platelet-Activating Factor (PAF) in the Nervous Tissue

Goracci¹,

Balestrieri²,

Nardicchi³

2009

Handbook of Neurochemistry and Molecular Neurobiology

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Platelet-Activating Factor Antagonists: Scientific Background and Possible Clinical Applications

Cited by 35 publications

References 263 publications

The Platelet‐Activating Factor Receptor Antagonist WEB 2170 Prevents Neonatal Necrotizing Enterocolitis in Rats

The Platelet‐Activating Factor Receptor Antagonist WEB 2170 Prevents Neonatal Necrotizing Enterocolitis in Rats

The Effect of 3‐Month Ingestion of Ginkgo biloba Extract on Pancreatic β‐Cell Function in Response to Glucose Loading in Normal Glucose Tolerant Individuals

Metabolism and Functions of Platelet-Activating Factor (PAF) in the Nervous Tissue

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