Back to Search
Start Over
Metabolism of a New Antiaggregant, Indolinone Derivative.
- Source :
-
Bulletin of experimental biology and medicine [Bull Exp Biol Med] 2020 Apr; Vol. 168 (6), pp. 739-742. Date of Electronic Publication: 2020 Apr 25. - Publication Year :
- 2020
-
Abstract
- Cytochrome p450-mediated metabolism of GRS (indolinone antiaggregant) and its effects on activities of cytochrome p450 isoenzymes were studied. Inhibition of 6 isomers of cytochrome p450 in human liver microsomes was studied with the use of specific substrates. It was found that human liver cytochrome p450 enzymes could not induce degradation of GRS and that GRS was not an inductor or inhibitor of cytochrome p450 family members 1A2, 2C9, 2C19, 2D6, 2C8, and 3A4. Hence, clinical use of the prospective antiaggregant would not involve the risk of uncontrolled fluctuations in GRS concentrations in the organism because of interactions between the drugs.
- Subjects :
- Animals
Biotransformation drug effects
Cytochrome P-450 CYP1A2 metabolism
Cytochrome P-450 CYP2C19 metabolism
Cytochrome P-450 CYP2C8 metabolism
Cytochrome P-450 CYP2C9 metabolism
Cytochrome P-450 CYP2D6 metabolism
Cytochrome P-450 CYP3A metabolism
Enzyme Assays
Gene Expression
Humans
Kinetics
Liver drug effects
Liver enzymology
Microsomes, Liver enzymology
NADP metabolism
Rats
Verapamil pharmacology
Microsomes, Liver drug effects
Oxindoles pharmacology
Platelet Aggregation Inhibitors pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1573-8221
- Volume :
- 168
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Bulletin of experimental biology and medicine
- Publication Type :
- Academic Journal
- Accession number :
- 32333310
- Full Text :
- https://doi.org/10.1007/s10517-020-04792-y