Biotransformation of stobadine, a gamma-carboline antiarrhythmic and cardioprotective agent, in rat liver microsomes.
1. The metabolism of stobadine, a gamma-carboline antiarrhythmic and cardioprotective agent, was investigated in vitro using fortified rat liver microsomal preparations. 2. Two metabolic products, N-desmethyl stobadine and stobadine N-oxide were isolated and identified by means of t.l.c.,g.l.c. -mass spectrometry, n.m.r. spectrometry and comparison with synthetic reference compounds. 3. Stobadine N-oxide was resolved into two optically active stereoisomers which were produced enzymically in approximately equal quantities.
Institute of Experimental Pharmacology, Slovak Academy of Sciences, Bratislava, Czechoslovakia.
M
M
Stefek
L
L
Benes
M
M
Jergelová
V
V
Scasnár
L
L
Turi-Nagy
P
P
Kocis
D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000493:pharmacokinetics*; D001711:Biotransformation; D002243:Carbolines / Q000493:pharmacokinetics*; D002316:Cardiotonic Agents / Q000493:pharmacokinetics*; D002849:Chromatography, Gas; D002855:Chromatography, Thin Layer; D008401:Gas Chromatography-Mass Spectrometry; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008862:Microsomes, Liver / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains
D000889:Anti-Arrhythmia Agents; D002243:Carbolines; D002316:Cardiotonic Agents; C100106:dicarbine