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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 tetrazoleprotected 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 700-3600mCi/mmol.

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