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C-11-verapamil to Assess P-gp Function in Human Brain During Aging, Depression and Neurodegenerative Disease

  作者 Bartels, AL; de Klerk, OL; Kortekaas, R; de Vries, JJ; Leenders, KL  
  选自 期刊  Current Topics in Medicinal Chemistry;  卷期  2010年10-17;  页码  1775-1784  
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[摘要]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 C-11-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.

 
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