Autoradiographic studies of the distribution of [14C]changrolin in mice

Changrolin is 4-{3’,5’-bis[(N-pyrrolidinyl) methyl]-4’-hydroxyanilino}-quinazoline. It was first synthesized and developed in our Institute as a novel antiarrhythmia agent. Male mice were injected iv [14C]changrolin 82 mg (2.74 MBq)/kg. At 20 min, higher radioactivities were found in gut and its content, liver, salivary gland and lung; moderate in kidney, spleen, and vertebra; least in heart, thymus, thyroid an dadrenal. The radioactivities tended to decrease after 2 h except in the salivary gland and gut in which accumulation of radioactivities persisted. After 24 h, the radioactivity was not detected. After iv 2.74 MBq/kg for 3 d, only a trace of radioactivity was detected in liver and intestine. These results indicate that there is no obvious accumulation within 3 days.