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Inhibition of Cytochrome P450c11 by Biogenic Amines and an Aziridine Precursor, 2-(4-Acetoxyphenyl)-2-Chloro-N-Methyl-Ethylammonium Chloride

A Louw, F Allie, Swart Ac, P Swart
2000 Endocrine Research  

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The interaction of several biogenic amines and Compound A (2-(4acetoxyphenyl)-2-chloro-N-methyl-ethylammonium chloride), an analogue of the active substance in a HPLC fraction isolated from the shrub, Salsola tuberculatiformis Botsch., with cytochrome P450c11 was investigated. Noradrenaline, octopamine and Compound A inhibited the type I DOC induced difference spectrum of P450c11 and elicited a type II difference spectrum when added alone. The Ks-values for noradrenaline, octopamine, and
more » ... d A were 0.8 mM, 0.16 mM and 0.36 mM, respectively. Dopamine, adrenaline and synephrine did not interact with, or inhibit, P450c11. Further investigation of Compound A indicated that it is a mixed inhibitor of sheep P450c11 with a stronger competitive (Kic = 106-110 M) than uncompetitive (Kiu = 667-737 M) element.
doi:10.3109/07435800009048593 pmid:11196449 fatcat:qk4jkzgatfb45beyocjnt7tf6u
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A Louw, F Allie, Swart Ac, P Swart. "Inhibition of Cytochrome P450c11 by Biogenic Amines and an Aziridine Precursor, 2-(4-Acetoxyphenyl)-2-Chloro-N-Methyl-Ethylammonium Chloride." Endocrine Research 26.4 (2000) 729-736