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Herein we present a novel <jats:sup>18<\/jats:sup>F\u2010labeled derivative of the drug irbesartan, one of the most prescribed angiotensin\u2005II type\u20051 receptor (AT<jats:sub>1<\/jats:sub>R) antagonists, for in vivo positron emission tomography (PET). This allows the in vivo measurement of AT<jats:sub>1<\/jats:sub>R expression, and thus the evaluation of functional changes in its expression under pathophysiological conditions. We followed various synthetic approaches optimized for the introduction of fluorine into different positions of the aliphatic side chain of irbesartan. Radioligand binding studies revealed that fluorine atoms at specified positions (\u03b1\u2010position (IC<jats:sub>50<\/jats:sub>=6.6\u2005n<jats:sc>m<\/jats:sc>) and \u03b4\u2010position (IC<jats:sub>50<\/jats:sub>=8.5\u2005n<jats:sc>m<\/jats:sc>) of the aliphatic side chain) do not alter the binding properties of irbesartan (IC<jats:sub>50<\/jats:sub>=1.6\u2005n<jats:sc>m<\/jats:sc>). 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