Absorption, metabolism and excretion of 14C-NZ-105 were studied in male dogs after oral (10mg/kg) administration. Serum protein binding was investigated in the rat, dog and human.
1. Blood levels of radioactivity reached a peak level (564ng eq./ml) at 2hr after administration and then decreased with the half-life of 3. 1hr until 12hr.
2. The excretion of radioactivity in urine and feces within 120hr after oral administration was 3.1% and 98.5% of dose, respectively.
3. The in vitro binding to rat, dog and human serum proteins was 98% or more at 200, 600 and 2000ng/ml. That observed in vivo was 85.8 ?? 89.7% at 0.5, 2 and 6hr after oral administration in rats and 38.5 ?? 45.6% at 2, 4 and 8hr after dosing in dogs.
4. The unchanged drug and oxidatively deaminated compound (AL) were mainly detected in the plasma.
