blood-brain transfer of pittsburgh compound b in humans

In the labeled form, the Pittsburgh compound B (2-(4’-{N-methyl-[11C]}methyl-aminophenyl)-6-hydroxybenzothiazole,[11C]PiB), is used as a biomarker for positron emission tomography (PET) of brain □-amyloiddeposition in Alzheimer’s disease (AD). The permeability of [11C]PiB in the blood-brain barrier is held tobe high but the permeability-surface area product and extraction fractions in patients or healthy volunteersare not known. We used PET to determine the clearance associated with the unidrectional blood-braintransfer of [11C]PiB and the corresponding cerebral blood flow rates in frontal lobe, whole cerebral cortex,and cerebellum of patients with Alzheimer’s disease and healthy volunteers. Regional cerebral blood flowrates differed significantly between the two groups, but regional and whole-brain permeability-surface areaproducts were identical, in agreement with the observation that numerically, but insignificantly, unidirectionalblood-brain clearances are lower and extraction fractions higher in the patients. The evidence of unchangedpermeability-surface area products in the patients implies that blood flow changes can be deduced from theunidirectional blood-brain clearances of [11C]PiB in the patients.