Characterization of P-glycoprotein transport and inhibition in vivo
| Autor: | E, Barbarics, J F, Kronauge, D, Cohen, A, Davison, A G, Jones, J M, Croop |
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| Rok vydání: | 1998 |
| Předmět: |
Technetium Tc 99m Sestamibi
Dose-Response Relationship Drug Transplantation Heterologous Mice Nude Biological Transport Breast Neoplasms Cyclosporins Neoplasms Experimental Mice Tumor Cells Cultured Animals Humans Female Tissue Distribution ATP Binding Cassette Transporter Subfamily B Member 1 Radiopharmaceuticals |
| Zdroj: | Cancer research. 58(2) |
| ISSN: | 0008-5472 |
| Popis: | The P-glycoprotein is an energy-dependent efflux pump capable of decreasing the intracellular concentration of a broad range of chemotherapeutic agents. [99mTc]Sestamibi, a P-glycoprotein transport substrate, is a sensitive probe of P-glycoprotein function both in vitro and in vivo. A human tumor model in nude mice was evaluated to determine whether [99mTc]Sestamibi could detect in vivo differences in P-glycoprotein expression and P-glycoprotein modulation by the reversal agent SDZ PSC 833. Differential [99mTc]Sestamibi accumulation based upon P-glycoprotein expression was demonstrated in xenografts in vivo. Dose-dependent inhibition of P-glycoprotein function was achieved with SDZ PSC 833. Administration of the reversal agent increased [99mTc]Sestamibi accumulation in the xenografts expressing P-glycoprotein. These observations show that [99mTc]Sestamibi as capable of detecting the modulation of P-glycoprotein in a solid tumor model by the reversal agent SDZ PSC 833. |
| Databáze: | OpenAIRE |
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