Interactions between substituted tryptamine analogues, MAO inhibitors and cytochrome P-450.
The effects of some MAO inhibitors, N-acetylenic analogues of tryptamine, on rat liver microsomal cytochrome P-450 (cyt P-450) have been investigated. All the compounds tested interacted with cyt P-450 with Ks values ranging between 14 and 358 microM (clorgyline Ks = 10.5 microM). Compounds with a tertiary amine and those possessing a secondary amine group in the acetylenic side chain exhibited type I and type II difference spectra, respectively. Aniline hydroxylase activity was inhibited irreversibly and in a time-dependent fashion by all compounds tested with IC50 ranging between 7 x 10(-5) and 7 x 10(-3) M (clorgyline 10(-4) M).
Valoti
M
M
Department de Bioquimica i Biologia Molecular, Universidad Autonoma de Barcelona, Spain.
Costanzo
M
M
Perez
V
V
Unzeta
M
M
Sgaragli
G P
GP
D000818:Animals; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism*; D008862:Microsomes, Liver / Q000201:enzymology*; D008996:Monoamine Oxidase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D014363:Tryptamines / Q000737:chemistry / Q000494:pharmacology*
D008996:Monoamine Oxidase Inhibitors; D014363:Tryptamines; D003577:Cytochrome P-450 Enzyme System