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Blood or plasma levels, metabolism and excretion were investigated after a single intravenous ad ministration of 14C-MCI-186 (2 mg/kg) to male dogs. 1) Decrease of radioactivity from whole blood was more delayed than from plasma, and transfer rates to blood cells increased parallel with the course of time.2) Unchanged MCI-186 in plasma decreased rapidly with the half-lives of 0.07 hr (t1/2.) and 0.70 hr (t112,6). Areas under the concentration time curves (AUC0.co) of unchanged MCI-186, sulfate and glucuronide of MCI-186 in plasma consisted 5.2/, 61.1% 16.2% of the AUC0__ of the radioactivity in plas ma, respectively.3) The dosed radioactivity was excreted to urine and feces until 120 hr after administration, in 84.1% and 13.2%, respectively, and main excretion route of MCI-186 was urinary excretion in dogs. 2.8%, 66.2% and 9.4% of the dosed radioactivity were excreted to urine as the forms of unchanged MCI-186, sulfate and glucuronide of respectively. 4) In dogs, the clearance of unchanged MCI-186 and percentages of MCI-186 sulfate to total radioactivi ty in plasma and urine were higher than those in rats. And unknown metabolites observed in dogs, accounted for a small fraction.