| |  Online-Ressource |
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| Verfasst von: | Drewe, Jürgen [VerfasserIn]  |
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| | Gutmann, Heike [VerfasserIn] |
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| | Fricker, Gert [VerfasserIn] |
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| | Török, Michael [VerfasserIn] |
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| | Beglinger, Christoph [VerfasserIn] |
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| | Huwyler, Jörg [VerfasserIn] |
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| Titel: | HIV protease inhibitor ritonavir |
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| Titelzusatz: | a more potent inhibitor of P-glycoprotein than the cyclosporine analog SDZ PSC 833 |
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| Verf.angabe: | Jürgen Drewe, Heike Gutmann, Gert Fricker, Michael Török, Christoph Beglinger, and Jörg Huwyler |
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| Jahr: | 1999 |
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| Umfang: | 6 S. |
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| Fussnoten: | Gesehen am 26.04.2017 |
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| Titel Quelle: | Enthalten in: Biochemical pharmacology |
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| Ort Quelle: | Amsterdam [u.a.] : Elsevier Science, 1958 |
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| Jahr Quelle: | 1999 |
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| Band/Heft Quelle: | 57(1999), 10, Seite 1147-1152 |
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| ISSN Quelle: | 1873-2968 |
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| Abstract: | The effect of P-glycoprotein inhibition on the uptake of the HIV type 1 protease inhibitor saquinavir into brain capillary endothelial cells was studied using porcine primary brain capillary endothelial cell monolayers as an in vitro test system. As confirmed by polymerase chain reaction and Western blot analysis, this system functionally expressed class I P-glycoprotein (pgp1A). P-Glycoprotein isoforms pgp1B or pgp1D could not be detected. The uptake of saquinavir into endothelial cells could be described as the result of a diffusional term of uptake and an oppositely directed saturable extrusion process. Net uptake of saquinavir into cultured brain endothelial cells could be increased significantly up to 2-fold by SDZ PSC 833 in a dose-dependent manner, with an ic50 of 1.13 μM. In addition, the HIV protease inhibitor ritonavir inhibited p-glycoprotein-mediated extrusion of saquinavir with an ic50 of 0.2 μM, indicating a high affinity of ritonavir for p-glycoprotein. In conclusion, we showed that the HIV protease inhibitor ritonavir is a more potent inhibitor of P-glycoprotein than the multidrug resistance (MDR)-reversing agent SDZ PSC 833. The inclusion of this drug in combination regimens may greatly facilitate brain uptake of HIV protease inhibitors, which is especially important in patients suffering from AIDS dementia complex. |
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| DOI: | doi:10.1016/S0006-2952(99)00026-X |
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| URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
kostenfrei registrierungspflichtig: Volltext: http://dx.doi.org/10.1016/S0006-2952(99)00026-X |
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| | kostenfrei registrierungspflichtig: Volltext: http://www.sciencedirect.com/science/article/pii/S000629529900026X |
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| | DOI: https://doi.org/10.1016/S0006-2952(99)00026-X |
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| Datenträger: | Online-Ressource |
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| Sprache: | eng |
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| Sach-SW: | AIDS |
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| | AIDS dementia complex |
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| | blood-brain barrier |
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| | HIV protease inhibitors |
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| | indinavir |
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| | nelfinavir |
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| | P-glycoprotein |
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| | ritonavir |
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| | saquinavir |
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| | SDZ PSC 833 |
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| K10plus-PPN: | 1556980795 |
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| Verknüpfungen: | → Zeitschrift |
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HIV protease inhibitor ritonavir / Drewe, Jürgen [VerfasserIn]; 1999 (Online-Ressource)
