Biotransformation of 5-phenyl-1,3,4-benzotriazepines

After administration of three 2-aminosubstituted 5-phenyl-1,3,4-benzotriazepines with hypoglycemic effects to rats 10 metabolites were isolated from urine and feces besides traces of the unchanged drugs. N-Dealkylation, aromatic hydroxylation, N-acetylation and ring contraction by hydrolytic processes beginning in the stomach occurred. The main excretion route is with the feces.