Key result
[11C]Methyl-losartan was reliably synthesized with an overall yield of 30%-60%, radiochemical purity >99%, and specific activity of 700-3600 mCi/µmol.
[11C]Methyl-losartan was successfully synthesized with high radiochemical purity and specific activity, demonstrating potential as a novel PET imaging radioligand for AT1 receptors.
May enable AT1R PET imaging in cardiac disease; leaves open clinical validation and utility.
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.
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Hadizad et al. (2011) studied this question. [11C]Methyl-losartan was evaluated on Radiochemical synthesis yield and purity. [11C]Methyl-losartan was reliably synthesized with an overall yield of 30%-60%, radiochemical purity >99%, and specific activity of 700-3600 mCi/µmol.
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