50] Use of WEB 2086 and WEB 2170 as platelet-activating factor antagonists/at

Abstract

Publisher Summary The chapter presents a study on the utilization of WEB 2086 and WEB 2170 as platelet-activating factor (PAF) antagonists. The chapter presents the physicochemical properties and the pharmacological use of these new PAF antagonists. Since the discovery of the platelet-activating factor (PAF, 1- O -aikyl-2- acetyl- sn -glycerophosphorylcholine) in 1972, the interest in studying its physiological and pharmacological responses as well as its pathophysiological role has created a demand for specific and potent PAF antagonists. The search for these antagonists yielded several types of compounds differing in origin and structure .Among these, two synthetic compounds derived from the thienotriazolodiazepine brotizolam, a hypnotic, have recently been described under the code number WEB 2086 and WEB 2170. These compounds are specific and very potent PAF antagonists, free from hypnotic and sedative activity. They are expected to facilitate research in this area and to be therapeutically useful. WEB 2086 and WEB 2170 belong to the group of thienotriazolo-l,4-diazepines (hetrazepines). WEB 2086 and WEB 2170 are potent and selective antagonists of PAF in vitro and, more importantly , in vivo with a long duration of action. For oral use in rats, WEB 2170 may be preferred to WEB 2086 because of the higher potency and long duration of action. Both compounds are suitable tools for investigating the significance of PAF in the pathophysiology of different diseases.