کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
4348019 1296873 2008 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood–brain barrier in a rat brain endothelial cell model
موضوعات مرتبط
علوم زیستی و بیوفناوری علم عصب شناسی علوم اعصاب (عمومی)
پیش نمایش صفحه اول مقاله
Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood–brain barrier in a rat brain endothelial cell model
چکیده انگلیسی

Parkinson's disease is a neurodegenerative disorder that requires treatment by dopaminergic agonists, which may be responsible for central side effects. We hypothesized that the efflux transporter ABCB1/P-glycoprotein played a role in brain disposition of antiparkinsonian drugs and could control central toxicity. We aimed to evaluate antiparkinsonian drugs as ABCB1 substrates and/or inhibitors in rat brain endothelial cells GPNT, in order to predict potential clinical drug–drug interactions. Among the antiparkinsonian drugs tested, levodopa, bromocriptine, pergolide and pramipexole were ABCB1 substrates. However, only bromocriptine could inhibit ABCB1 functionality with an IC50 of 6.71 μM on Rhodamine 123 uptake and an IC50 of 1.71 μM on digoxine uptake. Thus, bromocriptine at 100 μM is responsible for an increase of levodopa intracellular transport of about 2.05-fold versus control. Therefore, we can conclude that bromocriptine is a potent drug for medicinal interactions in vitro. Hence, in patients with Parkinson's disease, these results may be considered to optimise treatments individually.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Neuroscience Letters - Volume 442, Issue 1, 5 September 2008, Pages 19–23
نویسندگان
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