Abstract
Several reference compounds such as Cyclosporin A, Tamoxifen, Verapamil, and our compound 1, known as P-gp modulators, have been tested for their P-gp modulating activity in isolated organ bath. Compound 1 showed the best result in organ bath experiment (EC(50)=14.7 microM), Cyclosporin A and Tamoxifen displayed EC(50)=25.2 and 39.4 microM, respectively.
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / chemistry*
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Animals
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Caco-2 Cells
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Chemistry, Pharmaceutical / methods
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Cyclosporine / pharmacology
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Cytochrome P-450 CYP3A / chemistry
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Cytochrome P-450 Enzyme System / chemistry
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Drug Resistance, Multiple
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Guinea Pigs
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Humans
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Ileum / drug effects*
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Ileum / metabolism
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Models, Chemical
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Rhodamine 123 / chemistry*
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Rhodamine 123 / pharmacokinetics*
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Tamoxifen / pharmacology
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Verapamil / pharmacology
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Tamoxifen
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Rhodamine 123
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Cyclosporine
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Cytochrome P-450 Enzyme System
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Verapamil
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Cytochrome P-450 CYP3A
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CYP3A4 protein, human