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Cytochrome P450 isozymes involved in propranolol metabolism in human liver microsomes. The role of CYP2D6 as ring-hydroxylase and CYP1A2 as N-desisopropylase.
Results indicate that propranolol 5-hydroxylation, as well as 4-hydrogenation, is mainly catalyzed by CYP2D6 in human liver microsomes, and not with the other P450 isozyme contents or metabolic activities. Expand
Effects of continuous ingestion of green tea or grape seed extracts on the pharmacokinetics of midazolam.
The studies indicate that subchronic ingestion of GTE or GSE may alter the pharmacokinetics of MDZ, and the effects ofGTE on CYP3A activity appear opposite between liver and small intestine, which could not be predicted from in vitro experiments. Expand
Catalytic activity of three variants (Ile, Leu, and Thr) at amino acid residue 359 in human CYP2C9 gene and simultaneous detection using single-strand conformation polymorphism analysis.
The PCR-SSCP approach is useful for identifying these three variants of the CYP2C9 gene, and the effect of the two variants on diclofenac 4'-hydroxylation appears to be different because Leu359 variant was associated with a high Km, and Thr359 with a low Vmax. Expand
Effects of endogenous steroids on CYP3A4-mediated drug metabolism by human liver microsomes.
The data demonstrate that endogenous steroids, especially androgens, strongly affect CYP3A4-mediated drug metabolism in vitro and the postulated mechanisms of the interactions between AND and CBZ or ZNS are discussed. Expand
Bioactivation of monocrotaline by P-450 3A in rat liver.
P-450 3A was predominantly responsible for the metabolism of MCT to MCTP in rat liver and suggested a tight linkage between the degree of PH and the activity of liver P-450 2A and 3A. Expand
Cytochrome P450-dependent drug oxidation activities in liver microsomes of various animal species including rats, guinea pigs, dogs, monkeys, and humans
Levels of cytochrome P450 proteins immunoreactive to antibodies raised against human CYP1A2, 2A6, 2C9, 2E1, and 3A4, monkey CYP2B17, and rat CyP2D1 were determined in liver microsomes of rats, guinea pigs, dogs, monkeys, and humans; the differences in these animal species varied with the P450 enzymes examined and the substrates used. Expand
Characterization of human liver microsomal cytochrome P450 involved in the reductive metabolism of zonisamide.
The metabolism of zonisamide to SMAP was almost completely inhibited by anti-P450 3A4 antibody but not by anti -P450 2C9 or anti- P450 2D6 antibodies, suggesting that the amount of P 450 3A enzyme may be a major factor influencing the level of metabolism ofZonisamideto SMAP in human liver microsomes. Expand
Interaction of Drugs and Chinese Herbs: Pharmacokinetic Changes of Tolbutamide and Diazepam Caused by Extract of Angelica dahurica
The inhibitory effects of Angelica dahurica root extract on rat liver microsomal cytochrome P450 and drug‐drug interactions were studied.
Comparison of basal gene expression and induction of CYP3As in HepG2 and human fetal liver cells.
The character of HFL cells with regard to CYP expression was different from that of HepG2 cells, and CYP3A5 mRNA expression levels were markedly up-regulated by dexamethasone (DEX), but not by rifampicin (RIF). Expand
Purification and characterization of two forms of hepatic microsomal cytochrome P450 from untreated cynomolgus monkeys.
Results demonstrate that this P450 enzyme is in the P450 3A subfamily and P450 CMLb is expressed constitutively as one of the minor forms of P450 in liver microsomes of untreated cynomolgus monkeys and is inducible by phenobarbital. Expand