11C-verapamil to assess P-gp function in human brain during aging, depression and neurodegenerative disease.
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.
Bartels
A L
AL
Dept. of Neurology, University Medical Center Groningen, The Netherlands. a.l.bartels@neuro.umcg.nl
de Klerk
O L
OL
Kortekaas
R
R
de Vries
J J
JJ
Leenders
K L
KL
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000737:chemistry / Q000378:metabolism*; D000375:Aging; D001812:Blood-Brain Barrier / Q000000981:diagnostic imaging* / Q000378:metabolism / Q000503:physiopathology; D001927:Brain Diseases / Q000000981:diagnostic imaging* / Q000378:metabolism / Q000503:physiopathology; D002250:Carbon Radioisotopes; D003866:Depressive Disorder / Q000000981:diagnostic imaging* / Q000378:metabolism / Q000503:physiopathology; D006801:Humans; D019636:Neurodegenerative Diseases / Q000000981:diagnostic imaging* / Q000378:metabolism / Q000503:physiopathology; D049268:Positron-Emission Tomography; D014700:Verapamil / Q000737:chemistry / Q000493:pharmacokinetics*
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D002250:Carbon Radioisotopes; D014700:Verapamil