[Investigations of pharmacokinetics and metabolic behavior of N-L-pnenylalanyl-L-2-amino-1-phenylpropane (author's transl)].
To elucidate the pharmacokinetic and metabolic behavior of N-L-phenylalanyl-L-2-amino-1-phenylpropane (7), which resembles antidepressants in its pharmacological spectrum, 14C-labelled 7 was synthesized. After i.p. application of 7 to the mouse on accumulation in the gastrointestinal tract, liver, kidney, bile and brain was shown by autoradiograms of the whole body. In the mouse 7 is excreted predominantly by the kidney (54% of the applied 14C-activity 8 h p.i.) and also considerably with the feces (11% of the applied 14C-activity 8 h p.i.). After 48 h the clearance is largely completed (85% of the applied 14C-activity). In the mouse the maximum 14C-activity in the brain (1.87% of the applied 14C-activity) is already reached after 0.25 h, 93.38% of it consisting of 7 and of amphetamine (5) liberated from 7, quantity ratio 5:7 = 1.43, and 5.00% hydroxylated metabolites of 5. With decreasing concentration of 5 and 7 the quantity ratio of 5:7 reaches a maximum value of 3.56 after 4 h. The steadily raised spontaneous motility by 7 after i.p. application lasting 4 h is attributed to 5, which is antagonized by 7. Due to pharmacokinetic and pharmacological data 5 and 7 are discussed as originators of the adrenergic effects of 7.
D000626:Aminopeptidases / Q000378:metabolism; D000818:Animals; D001345:Autoradiography; D001711:Biotransformation; D001923:Brain Chemistry; D005243:Feces / Q000032:analysis; D007408:Intestinal Absorption; D007700:Kinetics; D008297:Male; D051379:Mice; D010649:Phenylalanine / Q000031:analogs & derivatives* / Q000378:metabolism; D014018:Tissue Distribution
D010649:Phenylalanine; C032863:N-L-phenylalanyl-L-2-amino-1-phenylpropane; D000626:Aminopeptidases
Untersuchungen zu Pharmakokinetik und Metabolismus von N-L-Phenylalanyl-L-2-amino-1-phenylpropan.