Title : Orphenadrine and methimazole inhibit multiple cytochrome P450 enzymes in human liver microsomes.

Pub. Date : 1997 Mar

PMID : 9172960






6 Functional Relationships(s)
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1 Orphenadrine and methimazole inhibit multiple cytochrome P450 enzymes in human liver microsomes. Orphenadrine cytochrome P450 family 2 subfamily B member 6 Homo sapiens
2 The specificities of orphenadrine and methimazole on eight human liver P450 enzyme activities were evaluated by studying the extent of inhibition at different concentrations in two protocols: competitive inhibition and preincubation. Orphenadrine cytochrome P450 family 2 subfamily B member 6 Homo sapiens
3 In the competitive inhibition protocol, orphenadrine decreased CYP2B6 marker activity up to 45-57% in human liver microsomes and up to 80-97% in cell microsomes containing cDNA-expressed CYP2B6. Orphenadrine cytochrome P450 family 2 subfamily B member 6 Homo sapiens
4 In the competitive inhibition protocol, orphenadrine decreased CYP2B6 marker activity up to 45-57% in human liver microsomes and up to 80-97% in cell microsomes containing cDNA-expressed CYP2B6. Orphenadrine cytochrome P450 family 2 subfamily B member 6 Homo sapiens
5 In the preincubation protocol, orphenadrine decreased the CYP2B6 activity in cDNA-expressed cell microsomes to completion. Orphenadrine cytochrome P450 family 2 subfamily B member 6 Homo sapiens
6 In human liver microsomes, orphenadrine strongly decreased the marker activities of CYP2B6, CYP2D6, as well as CYP2C9; and partially decreased the marker activities of CYP1A2, CYP2A6, CYP3A4, and CYP2C19. Orphenadrine cytochrome P450 family 2 subfamily B member 6 Homo sapiens