Synthesis of an 125I analog of MK-0591 and characterization of a 5-lipoxygenase activating protein binding assay

✍ Scribed by J. F. Eggler; J. B. Cheng; K. Cooper; L. M. Hanak; J. S. Pillar; M. Zdankiewicz

• Publisher: John Wiley and Sons
• Year: 1994
• Tongue: French
• Weight: 388 KB
• Volume: 34
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.2580341204

✦ Synopsis

Abstract

The ^125^I analog of MK‐0591, 1, has been prepared for use as a radioligand for developing a 5‐lipoxygenase activating protein (FLAP) binding assay. The radiosynthesis involves a two step oxidative iododestannylation‐saponification procedure. A FLAP binding assay has been developed in human neutrophil membranes. The binding of 1 to human neutrophil FLAP is rapid, reversible, of high affinity, saturable and selective for FLAP inhibitors.