61925-94-8Relevant academic research and scientific papers
Investigations of pharmacokinetics and metabolic behavior of N-L-phenylalanyl-L-2-amino-1-phenylpropane
Beck,Hoelzl,Schoenenberger
, p. 1726 - 1731 (2007/10/02)
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 an 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 kidneys (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.
