Synthesis of a fluorescent labeled thromboxane A2 receptor antagonist

✍ Scribed by Chandra Prakash; Sam Saleh; Rosemary Murray; Garret A. FltzGerald; Ian A. Blair

• Publisher: Elsevier Science
• Year: 1995
• Tongue: English
• Weight: 193 KB
• Volume: 5
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/0960-894x(95)00284-z

✦ Synopsis

The synthesis and biological evaluation of a fluorescent labeled probe for the thromboxane A2 receptor is described.

Since the discovery of thromboxane A2 (TXA2, 1), an unstable metabolite of the arachidonic acid cascade, 4 a variety of stable analogs, each with a modified ring system, have been prepared and their biological characteristics have been evaluated. 5,6 TXA2 is a powerful inducer of platelet aggregation and vascular and respiratory smooth muscle constriction.4,7, 8 The in vivo formation of TXA2 is thought to play a key role in the pathogenesis of various circulatory and renal disorders. 9-11 Considerable efforts have been directed towards the synthesis of therapeutic agents that can either inhibit TXA2 biosynthesis or antagonize its binding at the receptor level. Such compounds could potentially have value for the treatment for of a variety of pathophysiological disorders. 12"15