114798-94-6Relevant articles and documents
[11C] Methyl-losartan as a potential ligand for PET imaging angiotensin II AT1 receptors
Hadizad, Tayebeh,Collins, Jeffrey,Antoun, Rawad E.,Beanlands, Rob S.,Dasilva, Jean N.
, p. 754 - 757 (2012/01/13)
The renin-angiotensin system regulates blood pressure via activation of the angiotensin II type 1 receptor (AT1R). The AT1R is involved in the pathology of cardiac and renal diseases such as heart failure and diabetic nephropathy. The aim of this study was to synthesize and characterize the O-[11 C]methylated derivative of the clinically used AT1 receptor blocker losartan as a novel AT1R PET imaging radioligand. [11 C]Methyl-losartan was reliably synthesized (n ≥ 40) via methylation of tetrazole-protected losartan followed by deprotection using HCl in an overall yield of 30%-60% (decay-corrected from [11 C]MeI). Radiochemical purity was >99% and specific activity 700-3600 mCi/μmol. Copyright 2011 John Wiley & Sons, Ltd. [11 C]Methyl-losartan has been synthesized in three steps: 1) protection of the tetrazole group, 2) [11 C]methylation of hydroxyl group, and 3) deprotection in acidic conditions. Copyright