Current Topics in Medicinal Chemistry

Author(s): William B. Mathews and Zsolt Szabo

DOI: 10.2174/156802610793176729

Radioligands for the Angiotensin II Subtype 1 (AT1) Receptor

Page: [1585 - 1599] Pages: 15

  • * (Excluding Mailing and Handling)

Abstract

Over the last years, ligands for angiotensin II subtype 1 receptor (AT1R) have been developed as an alternative to the use of angiotensin-converting enzyme (ACE) inhibitors for controlling high blood pressure. Radiolabeled versions of these ligands have proven vital to the development of more potent and specific drugs for the treatment of hypertension. Imaging studies using radiolabeled AT1R ligands have also elucidated the role these receptors play in angiogenesis as well as in various disease states beyond hypertension.

Keywords: Angiotensin, AT1, carbon-11, hypertension, iodine-125, Losartan, radioligand, tritium, Angiotensin II, (AT1) Receptor, angiotensin-converting enzyme (ACE), renin-angiotensin system (RAS), ACE inhibitors, Physiological regulation, atherosclerosis, renal fibrosis, myocardial remodeling, carcinogenesis, arterial hypertension, Fibrocyte accumulation, extracellular matrix (ECM), protein kinases (MAPKs), renin-angiotensin system, ANG II PEPTIDE ANALOGS, Losartan derivatives, blood-brain barrier (BBB), Candesartan, 18F-labeled AT1 antagonist, Eprosartan, Irbesartan, Telmisartan, Valsartan, Olmesartan, SK-1080, KR31173