Biodistribution and urinary excretion of 4‐IODO‐L‐<i>meta</i>‐tyrosine

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<jats:title>Abstract</jats:title><jats:p>We examined the biodistribution and urinary excretion of <jats:sup>125</jats:sup>I‐4‐iodo‐L‐<jats:italic>meta</jats:italic>‐tyrosine (4‐<jats:sup>125</jats:sup>I‐L‐mTyr) in mice, in order to compare the results with that of 3‐[<jats:sup>125</jats:sup>I]iodo‐alpha‐methyl‐L‐tyrosine (<jats:sup>125</jats:sup>I‐L‐AMT). Three hours after administration, more than 70% of the excretion of 4‐<jats:sup>125</jats:sup>I‐L‐mTyr was in the urine, and less than 5% was found in the feces. The kidney homogenate and urine analysis on its metabolites revealed that most of the accumulated radioactivity belonged to intact 4‐<jats:sup>125</jats:sup>I‐L‐mTyr (>95%). These results indicated its high metabolic stability, which was comparable to <jats:sup>125</jats:sup>I‐L‐AMT stability. However, the blood clearance of 4‐<jats:sup>125</jats:sup>I‐L‐mTyr was faster than that of <jats:sup>125</jats:sup>I‐L‐AMT. 4‐<jats:sup>125</jats:sup>I‐L‐mTyr accumulation in mouse kidney cortex was approximately 80% lower than that of <jats:sup>125</jats:sup>I‐L‐AMT. Probenecid reduced the 4‐<jats:sup>125</jats:sup>I‐L‐mTyr accumulation in the kidney and urinary excretion, similar to <jats:sup>125</jats:sup>I‐L‐AMT.</jats:p>

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