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In vitro metabolism of simvastatin in humans [SBT]identification of metabolizing enzymes and effect of the drug on hepatic P450s.
- T. Prueksaritanont, L. Gorham, K. Vyas
- Biology, ChemistryDrug Metabolism And Disposition
- 1 October 1997
It is concluded that CYP3A is the major enzyme subfamily responsible for the metabolism of SV by human liver microsomes, and metabolic activities mediated by the other P450 enzymes tested are unlikely to be affected by SV.
AVERMECTINS. STRUCTURE DETERMINATION
In vitro and in vivo biotransformation of simvastatin, an inhibitor of HMG CoA reductase.
Several metabolites resulting from microsomal oxidation (after subsequent conversion from lactones to hydroxy acids) are effective inhibitors of 3-hydroxy-3-methylglutaryl-CoA reductase and may contribute to the cholesterol lowering effect of SV.
Metabolic profiles of montelukast sodium (Singulair), a potent cysteinyl leukotriene1 receptor antagonist, in human plasma and bile.
It could be concluded that a major part of the radioactivity of montelukast was excreted via bile, and the levels of metabolites in the systemic circulation were low in the fed as well as fasted subjects, with <2% of the circulating radioactivity being due to metabolites M5a, M5b, M6a, and M6b.
The pterin component of the molybdenum cofactor. Structural characterization of two fluorescent derivatives.
Identification of cytochrome P4503A4 as the major enzyme responsible for the metabolism of ivermectin by human liver microsomes.
- Z. Zeng, N. Andrew, B. Arison, D. Luffer-Atlas, R. Wang
- Biology, ChemistryXenobiotica; the fate of foreign compounds in…
To determine which human cytochrome P450 isoform(s) is responsible for the metabolism of ivermectin, chemical inhibitors including sulphaphenazole, quinidine, furafylline, troleandomycin (TAO) and diethyldithiocarbamate (DDC) were used to evaluate their effect on iverMectin metabolism.
Characterization of methyltransferase and hydroxylase genes involved in the biosynthesis of the immunosuppressants FK506 and FK520
- H. Motamedi, A. Shafiee, S. Cai, S. Streicher, B. Arison, R. Miller
- Biology, ChemistryJournal of Bacteriology
- 1 September 1996
Heterologous expression of f kbM in Streptomyces lividans established that fkbM encodes an O-methyltransferase catalyzing the methylation of the C-31 hydroxyl group of 31-O-demethyl-FK506 and FK520.
Disposition and metabolism of (+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d] cyclohepten-5,10-imine in rats, dogs, and monkeys.
- H. Hucker, J. Hutt, S. D. White, B. Arison, A. G. Zacchei
- Biology, ChemistryDrug metabolism and disposition: the biological…
Radioactivity was extensively excreted in rat bile and was widely distributed among various tissues and major metabolites of the drug in rat and dog urine were the 2- and 8-Hydroxy analogs (rat) and the N-hydroxy derivative (dog).
Farnesol-derived Dicarboxylic Acids in the Urine of Animals Treated with Zaragozic Acid A or with Farnesol*
- R. Bostedor, J. D. Karkas, J. Bergstrom
- Chemistry, BiologyJournal of Biological Chemistry
- 4 April 1997
The high level of FDDCAs that were found suggests that their synthesis is the major metabolic fate for carbon diverted from cholesterol synthesis by a squalene synthase inhibitor.
Photodegradation of avermectin B1a thin films on glass
Photodegradation of avermectin B 1a thin films under artificial light (above 260 nm) for short periods of time (greater than 60% of parent compound remaining) resulted in the formation of at least 10…