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[11C]Methyl-losartan as a potential ligand for PET imaging angiotensin II AT1 receptors

✍ Scribed by Tayebeh Hadizad; Jeffrey Collins; Rawad E. Antoun; Rob S. Beanlands; Jean N. DaSilva

Publisher
John Wiley and Sons
Year
2011
Tongue
French
Weight
357 KB
Volume
54
Category
Article
ISSN
0022-2135

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✦ Synopsis

The renin‐angiotensin system regulates blood pressure via activation of the angiotensin II type 1 receptor (AT~1~R). The AT~1~R 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 AT~1~ receptor blocker losartan as a novel AT~1~R 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.

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