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 μM (clorgyline Ks = 10.5 μM). 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).
KeywordsTertiary Amine Difference Spectrum Secondary Amine Group NADPH Generate System Aniline Hydroxylase
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- Balsa D, Fernandez-Alvarez E, Tipton KF, Unzeta M (1990) Inhibition of MAO by substituted tryptamine analogues. J Neural Transm [Suppl] 32: 103–105.Google Scholar
- Callingham BA, Valoti M, Sgaragli GP (1991) Drug and enzyme interactions with moclobemide. In: Racagni G, Brunello N, Fukuda T (eds) International Congress Series 968. Elsevier Science Publisher, Amsterdam, pp 846–849.Google Scholar
- Lake B (1987) Preparation and characterisation of microsomal fractions for studies on xenobiotic metabolism. In: Snell K, Mullock B (eds) Biochemical toxicology a practical approach. IRL Press, Oxford, pp 183–215.Google Scholar