[Biotransformation and excretion of N,N'-bis(3-(2-ethoxyphenoxy)-2-hydroxypropyl)ethylenediamine dihydrochloride (Falirytmin) in rats].
Falirytmin (1) was metabolized in rats almost completely. Besides small amounts of 1 in urine and feces 18 metabolites could be separated. The proposed structures of 14 compounds demonstrate aromatic hydroxylation, N- and O-dealkylation, side-chain oxidation, alcohol dehydrogenation and N-acetylation. The main route of excretion of 1 and metabolites was with the feces. After p.o. or i.v. administration of 14C-O-ethyl-1 the average excretion of radioactivity in urine, feces and expired air was about 75% in 96 h. The residual activity in organs was about 2-2.5%. Whole-body autoradiography confirms these results. Only slight 14C-activity was seen in muscle, fat, liver, bone marrow and gut.
Pfeifer
S
S
Fachbereich Pharmazie, Humboldt-Universität zu Berlin, DDR.
Plonka
G R
GR
Dobbrodt
I
I
Franke
P
P
Steenbeck
L
L
D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000378:metabolism* / Q000493:pharmacokinetics; D001345:Autoradiography; D001711:Biotransformation; D002245:Carbon Dioxide / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D005029:Ethylenediamines / Q000378:metabolism* / Q000493:pharmacokinetics; D008297:Male; D013058:Mass Spectrometry; D051381:Rats; D011919:Rats, Inbred Strains
D000889:Anti-Arrhythmia Agents; D005029:Ethylenediamines; D002245:Carbon Dioxide; C012783:Falirytmin
Biotransformation und Ausscheidung von N,N'-Bis[3-(2-ethoxy-phenoxy)-2- hydroxy-propyl]ethylendiamin-dihydrochlorid (Falirytmin) bei der Ratte.