Inhibition of human platelet thromboxane synthetase by 11a-carbathromboxane A 2 analogs

Abstract

Summary Three 11a-carbathromboxane A 2 analogs were synthesized and evaluated for “thromboxane A 2 -like” biological activity in human platelets and rat aortic strips. All three analogs were potent inhibitors of either prostaglandin H 2 or arachidonic acid-induced human platelet aggregation, and proved to be both receptor level antagonists of thromboxane A 2 and thromboxane synthetase inhibitors. The three 11a-carba analogs were devoid of either agonist or antagonist activity on rat aortic strips, suggesting that the thromboxane A 2 receptor in platelets exhibits different binding characteristics than the thromboxane receptor in vascular smooth muscle.