Abstract
P-glycoprotein (P-gp) at the blood-brain barrier (BBB) functions as an active efflux pump by extruding a wide range of substrates from the brain. This is important for maintaining loco-regional homeostasis and for protecting the brain against blood-borne toxic substances. Altered P-gp function seems to be involved in the pathophysiology of neurodegenerative disease and various neurological and psychiatric disorders. Positron emission tomography (PET) with the radiotracer (11)C-verapamil (VPM-PET) is a validated technique allowing measurement of P-gp function at the human BBB. In this review, we highlight changes of P-gp function, as measured with VPM-PET, in aging and in the pathogenesis and progression of neurodegenerative disease, as well as their role in depressive disorders.
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / chemistry
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism*
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Aging
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Blood-Brain Barrier / diagnostic imaging*
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Blood-Brain Barrier / metabolism
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Blood-Brain Barrier / physiopathology
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Brain Diseases / diagnostic imaging*
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Brain Diseases / metabolism
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Brain Diseases / physiopathology
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Carbon Radioisotopes
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Depressive Disorder / diagnostic imaging*
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Depressive Disorder / metabolism
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Depressive Disorder / physiopathology
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Humans
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Neurodegenerative Diseases / diagnostic imaging*
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Neurodegenerative Diseases / metabolism
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Neurodegenerative Diseases / physiopathology
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Positron-Emission Tomography
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Verapamil / chemistry
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Verapamil / pharmacokinetics*
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Carbon Radioisotopes
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Verapamil