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  • SAGE Publications  (2)
  • Schneider, Mary L  (2)
  • 1
    In: Journal of Cerebral Blood Flow & Metabolism, SAGE Publications, Vol. 30, No. 5 ( 2010-05), p. 994-1007
    Abstract: 18 F-Fallypride and 11 C-FLB457 are commonly used PET radioligands for imaging extrastriatal dopamine D 2 /D 3 receptors, but differences in their in vivo kinetics may affect the sensitivity for measuring subtle changes in receptor binding. Focusing on regions of low binding, a direct comparison of the kinetics of 18 F-fallypride and 11 C-FLB457 was made using a MI protocol. Injection protocols were designed to estimate K 1 , k 2 , f ND k on , B max , and k off in the midbrain and cortical regions of the rhesus monkey. 11 C-FLB457 cleared from the arterial plasma faster and yielded a ND space distribution volume ( K 1 / k 2 ) that is three times higher than 18 F-fallypride, primarily due to a slower k 2 (FAL:FLB; k 2 =0.54 min −1 :0.18 min −1 ). The dissociation rate constant, k off , was slower for 11 C-FLB457, resulting in a lower K Dapp than 18 F-fallypride (FAL:FLB; 0.39 nM:0.13 nM). Specific D 2 /D 3 binding could be detected in the cerebellum for 11 C-FLB457 but not 18 F-fallypride. Both radioligands can be used to image extrastriatal D 2 /D 3 receptors, with 11 C-FLB457 providing greater sensitivity to subtle changes in low-receptor-density cortical regions and 18 F-fallypride being more sensitive to endogenous dopamine displacement in medium-to-high-receptor-density regions. In the presence of specific D 2 /D 3 binding in the cerebellum, reference region analysis methods will give a greater bias in BP ND with 11 C-FLB457 than with 18 F-fallypride.
    Type of Medium: Online Resource
    ISSN: 0271-678X , 1559-7016
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2010
    detail.hit.zdb_id: 2039456-1
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  • 2
    In: Journal of Cerebral Blood Flow & Metabolism, SAGE Publications, Vol. 32, No. 8 ( 2012-08), p. 1546-1558
    Abstract: The goal of this work was to characterize the in-vivo behavior of [ 18 F]mefway as a suitable positron emission tomography (PET) radiotracer for the assay of 5-hydroxytryptamine 1A (5-HT 1A ) receptor density ( B max ). Six rhesus monkeys were studied using a multiple-injection (M-I) protocol consisting of three sequential bolus injections of [ 18 F]mefway. Injection times and amounts of unlabeled mefway were optimized for the precise measurement of B max and specific binding parameters k off and k on for estimation of apparent K D . The PET time series were acquired for 180 minutes with arterial sampling performed throughout. Compartmental analysis using the arterial input function was performed to obtain estimates for K 1 , k 2 , k off , B max , and K Dapp in the cerebral cortex and raphe nuclei (RN) using a model that accounted for nontracer doses of mefway. Averaged over subjects, highest binding was seen in the mesial temporal and dorsal anterior cingulate cortices with B max values of 42±8 and 36±8 pmol/mL, respectively, and lower values in the superior temporal cortex, RN, and parietal cortex of 24±4, 19±4, and 13±2 pmol/mL, respectively. The K Dapp of mefway for the 5-HT 1A receptor sites was 4.3±1.3 nmol/L. In conclusion, these results show that M-I [ 18 F]mefway PET experiments can be used for the in-vivo measurement of 5-HT 1A receptor density.
    Type of Medium: Online Resource
    ISSN: 0271-678X , 1559-7016
    Language: English
    Publisher: SAGE Publications
    Publication Date: 2012
    detail.hit.zdb_id: 2039456-1
    Location Call Number Limitation Availability
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