Fluorescent Angiotensin AT1 Receptor Antagonists

Fluorescent selective angiotensin AT1 receptor antagonists (sartans) that contain naphthalene (6, 7, 10, and 11), anthracene (12 and 14), acenaphthene (13 and 15), and coumarin (8 and 9) substituents have been prepared and their preliminary pharmacology evaluated in Chinese hamster ovary (CHO) cell based assays. Compounds 6–15 proved to be effective sartans with pKB estimates in the range of 6.7–10.5; their potential as cellular imaging agents is also discussed. Molecules of a sartan nature: Fluorescent selective angiotensin AT1 receptor antagonists (sartans) have been prepared and their pharmacology evaluated in Chinese hamster ovary (CHO) cell based assays. Preliminary imaging studies on using these compounds as probes for the localisation of AT1 receptors in cells are also presented.