Altered aldosterone disposition in P-Glycoprotein knockout mice
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Enhanced Brain Disposition and Effects of Δ9-Tetrahydrocannabinol in P-Glycoprotein and Breast Cancer Resistance Protein Knockout Mice
The ABC transporters P-glycoprotein (P-gp, Abcb1) and breast cancer resistance protein (Bcrp, Abcg2) regulate the CNS disposition of many drugs. The main psychoactive constituent of cannabis Δ(9)-tetrahydrocannabinol (THC) has affinity for P-gp and Bcrp, however it is unknown whether these transporters modulate the brain accumulation of THC and its functional effects on the CNS. Here we aim to ...
متن کاملAltered pharmacokinetics of vinblastine in Mdr1a P-glycoprotein-deficient Mice.
BACKGROUND P-glycoprotein (Pgp) is a membrane protein that acts as an extrusion pump for many cytotoxic drugs. Pgp is expressed in normal tissues, and its (over)expression in tumor cells contributes to their drug resistance. Human Pgp is encoded by the MDR1 gene, In mice, two Pgps (encoded by the mdr1a and mdr1b genes) appear to perform the same function as the single human protein. The simulta...
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Previous studies have indicated that P-glycoprotein (P-gp) attenuates the central nervous system penetration and central activity of some opioids. The impact of P-gp-mediated efflux on the disposition and efficacy of the synthetic opioid alfentanil currently is unknown. In this study, P-gp-competent [mdr1a(+/+)] and P-gp-deficient [mdr1a(-/-)] mice were used to investigate the impact of P-gp-me...
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INTRODUCTION The timing and quality of sleep are controlled by the interaction of a homeostatic process, that tracks sleep need as a function of the previous sleep/wake history, and a circadian process that ensures the appropriate timing of sleep relative to the daily light-dark alternation.1,2 Although these two processes seem functionally and neurophysiologically distinct, at the molecular le...
متن کاملThe disposition of saquinavir in normal and P-glycoprotein deficient mice, rats, and in cultured cells.
Protease inhibitors are very effective in treating patients infected with HIV. However, many drugs in this class penetrate poorly into the central nervous system (CNS) and may permit this site to be a sanctuary from which resistant virus can emerge. Previous studies have shown that the protease inhibitor saquinavir (SQV) interacts with the multidrug transport system, P-glycoprotein (P-gp), expr...
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ژورنال
عنوان ژورنال: Journal of the American College of Cardiology
سال: 2003
ISSN: 0735-1097
DOI: 10.1016/s0735-1097(03)81532-2