Metabolism of a New Antiaggregant, Indolinone Derivative
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 cytochro...
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| Veröffentlicht in: | Bulletin of experimental biology and medicine 2020-04, Vol.168 (6), p.739-742 |
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| container_title | Bulletin of experimental biology and medicine |
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| creator | Bykov, V. V. Leonov, K. A. Serebrov, V. Yu Chernysheva, G. A. Smol’yakova, V. I. Solov’ev, M. A. Udut, E. V. Fisenko, V. P. Udut, V. V. |
| description | 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. |
| doi_str_mv | 10.1007/s10517-020-04792-y |
| format | Article |
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V.</creatorcontrib><creatorcontrib>Leonov, K. A.</creatorcontrib><creatorcontrib>Serebrov, V. Yu</creatorcontrib><creatorcontrib>Chernysheva, G. A.</creatorcontrib><creatorcontrib>Smol’yakova, V. I.</creatorcontrib><creatorcontrib>Solov’ev, M. A.</creatorcontrib><creatorcontrib>Udut, E. V.</creatorcontrib><creatorcontrib>Fisenko, V. P.</creatorcontrib><creatorcontrib>Udut, V. V.</creatorcontrib><title>Metabolism of a New Antiaggregant, Indolinone Derivative</title><title>Bulletin of experimental biology and medicine</title><addtitle>Bull Exp Biol Med</addtitle><addtitle>Bull Exp Biol Med</addtitle><description>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.</description><subject>Animals</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Biotransformation - drug effects</subject><subject>Cell Biology</subject><subject>Clopidogrel</subject><subject>Cytochrome P-450 CYP1A2 - metabolism</subject><subject>Cytochrome P-450 CYP2C19 - metabolism</subject><subject>Cytochrome P-450 CYP2C8 - metabolism</subject><subject>Cytochrome P-450 CYP2C9 - metabolism</subject><subject>Cytochrome P-450 CYP2D6 - metabolism</subject><subject>Cytochrome P-450 CYP3A - metabolism</subject><subject>Enzyme Assays</subject><subject>Gene Expression</subject><subject>Humans</subject><subject>Internal Medicine</subject><subject>Isoenzymes</subject><subject>Kinetics</subject><subject>Laboratory Medicine</subject><subject>Liver - drug effects</subject><subject>Liver - enzymology</subject><subject>Mephenytoin</subject><subject>Microsomes, Liver - drug effects</subject><subject>Microsomes, Liver - enzymology</subject><subject>NADP - metabolism</subject><subject>Oxindoles - pharmacology</subject><subject>Pathology</subject><subject>Pharmacology and Toxicology</subject><subject>Platelet Aggregation Inhibitors - pharmacology</subject><subject>Rats</subject><subject>Verapamil - pharmacology</subject><issn>0007-4888</issn><issn>1573-8221</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2020</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kV9LwzAUxYMobk6_gA9SEHyy86ZJ2-Rx-Hcw9UWfQ9YmXUabjqRT9u3NrIoDMfch3NzfOYR7EDrFMMYA-ZXHkOI8hgRioDlP4s0eGuI0JzFLEryPhhComDLGBujI--W2hQwfogFJSDgYhog9qk7O29r4Jmp1JKMn9R5NbGdkVTlVSdtdRlNbBsC2VkU3ypk32Zk3dYwOtKy9Ovm6R-j17vbl-iGePd9PryezuKA07WKpdJZhCTnXXBPNywJomuFUMpozXirNCS_npMR5LjOqKAPGNKecc9CswJyM0HnvW8laCWN12zlZNMYXYpIRgCzYpYEa_0GFKlVjivBzbcL7juDil2ChZN0tfFuvO9NavwsmPVi41nuntFg500i3ERjENgbRxyBCDOIzBrEJorNetFrPG1X-SL73HgDSAz6MbKWcWLZrZ8Mi_7P9ALlij7Q</recordid><startdate>20200401</startdate><enddate>20200401</enddate><creator>Bykov, V. 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V.</creatorcontrib><creatorcontrib>Leonov, K. A.</creatorcontrib><creatorcontrib>Serebrov, V. Yu</creatorcontrib><creatorcontrib>Chernysheva, G. A.</creatorcontrib><creatorcontrib>Smol’yakova, V. I.</creatorcontrib><creatorcontrib>Solov’ev, M. A.</creatorcontrib><creatorcontrib>Udut, E. V.</creatorcontrib><creatorcontrib>Fisenko, V. P.</creatorcontrib><creatorcontrib>Udut, V. V.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><jtitle>Bulletin of experimental biology and medicine</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Bykov, V. V.</au><au>Leonov, K. A.</au><au>Serebrov, V. Yu</au><au>Chernysheva, G. A.</au><au>Smol’yakova, V. I.</au><au>Solov’ev, M. A.</au><au>Udut, E. V.</au><au>Fisenko, V. P.</au><au>Udut, V. V.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Metabolism of a New Antiaggregant, Indolinone Derivative</atitle><jtitle>Bulletin of experimental biology and medicine</jtitle><stitle>Bull Exp Biol Med</stitle><addtitle>Bull Exp Biol Med</addtitle><date>2020-04-01</date><risdate>2020</risdate><volume>168</volume><issue>6</issue><spage>739</spage><epage>742</epage><pages>739-742</pages><issn>0007-4888</issn><eissn>1573-8221</eissn><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. 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| subjects | Animals Biomedical and Life Sciences Biomedicine Biotransformation - drug effects Cell Biology Clopidogrel 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 Internal Medicine Isoenzymes Kinetics Laboratory Medicine Liver - drug effects Liver - enzymology Mephenytoin Microsomes, Liver - drug effects Microsomes, Liver - enzymology NADP - metabolism Oxindoles - pharmacology Pathology Pharmacology and Toxicology Platelet Aggregation Inhibitors - pharmacology Rats Verapamil - pharmacology |
| title | Metabolism of a New Antiaggregant, Indolinone Derivative |
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