Role of Two Efflux Proteins, ABCB1 and ABCG2 in Blood-Brain Barrier Transport of Bromocriptine in a Murine Model of MPTP-Induced Dopaminergic Degeneration

Purpose: MPTP-induced dopaminergic degeneration is an experimental model commonly used to explore Parkinson’s disease. Cerebral drug transport by ABC transporters in MPTP models has never been reported. Methods: We have investigated the transport of bromocriptine through the blood-brain barrier (BBB) in a MPTP model to understand the influence of the dopaminergic degeneration on ABCB1 and ABCG2. Results: We have shown that in MPTP treated mice, bromocriptine is widely distributed to brain (2.3-fold versus control, p

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Role of ABC transporters at the blood–brain barrier

Toxicology Letters ◽

10.1016/j.toxlet.2009.06.011 ◽

2009 ◽

Vol 189 ◽

pp. S18

Author(s):

Heidrun Potschka

Keyword(s):

Blood Brain Barrier ◽

Abc Transporters ◽

Brain Barrier ◽

Blood Brain

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In vivobioluminescence imaging of neurogenesis - the role of the blood brain barrier in an experimental model of Parkinson's disease

European Journal of Neuroscience ◽

10.1111/ejn.13540 ◽

2017 ◽

Vol 45 (7) ◽

pp. 975-986 ◽

Cited By ~ 3

Author(s):

Inga B. Fricke ◽

Sonja Schelhaas ◽

Bastian Zinnhardt ◽

Thomas Viel ◽

Sven Hermann ◽

...

Keyword(s):

Parkinson’S Disease ◽

Parkinson's Disease ◽

Experimental Model ◽

Blood Brain Barrier ◽

Brain Barrier ◽

Blood Brain

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The role of ABC transporters of the blood-brain barrier in opioid tolerance development

Postępy Higieny i Medycyny Doświadczalnej ◽

10.5604/01.3001.0010.8805 ◽

2018 ◽

Vol 72 ◽

pp. 58-68

Author(s):

Kamila Środa-Pomianek ◽

Anna Palko-Łabuz ◽

Przemysław Pomianek ◽

Olga Wesołowska

Keyword(s):

Chronic Pain ◽

Substrate Specificity ◽

Blood Brain Barrier ◽

Abc Transporters ◽

Pain Treatment ◽

Brain Barrier ◽

P Glycoprotein ◽

Blood Brain ◽

Chronic Pain Treatment

Opioids constitute an important group of drugs used in chronic pain treatment, e.g. cancer pain. Unfortunately, the development of the organism’s tolerance to the analgesic activity of opioids, the tendency to develop addictions and undesirable side effects are the main causes reducing opioid efficiency in chronic pain treatment. Among many mechanisms connected to emerging of opioid resistance the ATP-binding cassette (ABC) transporters present at the blood-brain barrier may play an important role. These transporter proteins, especially P-glycoprotein (ABCB1, MDR1), affect pharmacokinetics of many drugs and xenobiotics that are their substrates. ABC transporters reduce cellular uptake of drugs and/or increase their export from brain tissue to blood. Substrate specificity of P-glycoprotein is extremely wide and comprises many structurally and functionally unrelated compounds. What is interesting, substrate specificity of P-glycoprotein overlaps to a great extent the specificity of the isoforms of cytochrome P450 involved in drug metabolism. In the present review, the ABC proteins-mediated transport of opioids was discussed as well as the mechanisms of transport regulation. Cellular metabolism of various opioid drugs and the role of ABC transporters in their absorption, distribution and elimination were also described.

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