Autoradiographic study of the distribution and cellular uptake of (14C)-streptozotocin in the rat

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Abstract
The distribution and cellular accumulation, in the rat, of three specifically 14C-labelled forms of streptozotocin were investigated. A significant pancreatic accumulation of radioactivity was observed with (3′-methyl-14C)-streptozotocin only. Autoradiographic studies revealed high levels of bound radioactivity in the islet tissue following the administration of (3′-methyl-14C)-streptozotocin whereas much lower levels of radioactivity were detected in the pancreatic tissue following the administration of either (1-14C)-streptozotocin or (2′-14C)-streptozotocin. In the pancreas, the amount of radioactivity bound to islet tissue was always significantly higher than that bound to acinar tissue. In addition to the islet tissue, the kidney cortex showed a very high level of bound radioactivity after the administration of (3′-methyl-14C)-streptozotocin. The results suggest that streptozotocin is rapidly metabolised by the rat. The apparent specificity for the accumulation of radiolabel from (3′-methyl-14C)-streptozotocin suggests that a metabolite derived from the methyl bearing ureido side chain of the drug may be specifically involved in the induction of tissue damage and the consequent development of diabetes.