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Development of a Novel Ligand, [C]TGN-020, for Aquaporin 4 Positron Emission Tomography Imaging.

Nakamura Y, Suzuki Y, Tsujita M, Huber VJ, Yamada K, Nakada T - ACS Chem Neurosci (2011)

Bottom Line: Considering its clinical relevance, it is highly desirable to develop a noninvasive method for the quantitative analysis of AQP distribution in humans under clinical settings.Currently, the method of choice for such diagnostic examinations continues to be positron emission tomography (PET).Utilizing [(11)C]-TGN-020, PET images were successfully generated in wild type and AQP4 mice, providing a basis for future evaluation regarding its suitability for clinical studies.

View Article: PubMed Central - PubMed

Affiliation: Center for Integrated Human Brain Science, Brain Research Institute, University of Niigata , 1 Asahimachi, Niigata 951-8585, Japan.

ABSTRACT
Aquaporin 4 (AQP4), the most abundant isozyme of the water specific membrane transporter aquaporin family, has now been implicated to play a significant role in the pathogenesis of various disease processes of the nervous system from epilepsy to Alzheimer's disease. Considering its clinical relevance, it is highly desirable to develop a noninvasive method for the quantitative analysis of AQP distribution in humans under clinical settings. Currently, the method of choice for such diagnostic examinations continues to be positron emission tomography (PET). Here, we report the successful development of a PET ligand for AQP4 imaging based on TGN-020, a potent AQP4 inhibitor developed previously in our laboratory. Utilizing [(11)C]-TGN-020, PET images were successfully generated in wild type and AQP4 mice, providing a basis for future evaluation regarding its suitability for clinical studies.

No MeSH data available.


Related in: MedlinePlus

Ex vivo PET images of the brain. (a) WT and (b) KO mouse brains. (c) MRI images of the corresponding brain slices.
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fig2: Ex vivo PET images of the brain. (a) WT and (b) KO mouse brains. (c) MRI images of the corresponding brain slices.

Mentions: To analyze brain distribution of ligand by eliminating significant interference from skin and muscles, an ex vivo study was performed. Brains of WT and KO mice were harvested en bloc 10 min following the administration of [11C]TGN-020 under identical conditions to the in vivo study. Subsequently, ex vivo PET images were obtained (Figure 2). There is a dramatic difference in ligand uptake within the brain between WT and KO mice. Low but definitely remaining radioactivity within the brain of AQP4 KO mice is believed to reflect uptake of ligand by the tissue with AQP1 such red blood cells.


Development of a Novel Ligand, [C]TGN-020, for Aquaporin 4 Positron Emission Tomography Imaging.

Nakamura Y, Suzuki Y, Tsujita M, Huber VJ, Yamada K, Nakada T - ACS Chem Neurosci (2011)

Ex vivo PET images of the brain. (a) WT and (b) KO mouse brains. (c) MRI images of the corresponding brain slices.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3198134&req=5

fig2: Ex vivo PET images of the brain. (a) WT and (b) KO mouse brains. (c) MRI images of the corresponding brain slices.
Mentions: To analyze brain distribution of ligand by eliminating significant interference from skin and muscles, an ex vivo study was performed. Brains of WT and KO mice were harvested en bloc 10 min following the administration of [11C]TGN-020 under identical conditions to the in vivo study. Subsequently, ex vivo PET images were obtained (Figure 2). There is a dramatic difference in ligand uptake within the brain between WT and KO mice. Low but definitely remaining radioactivity within the brain of AQP4 KO mice is believed to reflect uptake of ligand by the tissue with AQP1 such red blood cells.

Bottom Line: Considering its clinical relevance, it is highly desirable to develop a noninvasive method for the quantitative analysis of AQP distribution in humans under clinical settings.Currently, the method of choice for such diagnostic examinations continues to be positron emission tomography (PET).Utilizing [(11)C]-TGN-020, PET images were successfully generated in wild type and AQP4 mice, providing a basis for future evaluation regarding its suitability for clinical studies.

View Article: PubMed Central - PubMed

Affiliation: Center for Integrated Human Brain Science, Brain Research Institute, University of Niigata , 1 Asahimachi, Niigata 951-8585, Japan.

ABSTRACT
Aquaporin 4 (AQP4), the most abundant isozyme of the water specific membrane transporter aquaporin family, has now been implicated to play a significant role in the pathogenesis of various disease processes of the nervous system from epilepsy to Alzheimer's disease. Considering its clinical relevance, it is highly desirable to develop a noninvasive method for the quantitative analysis of AQP distribution in humans under clinical settings. Currently, the method of choice for such diagnostic examinations continues to be positron emission tomography (PET). Here, we report the successful development of a PET ligand for AQP4 imaging based on TGN-020, a potent AQP4 inhibitor developed previously in our laboratory. Utilizing [(11)C]-TGN-020, PET images were successfully generated in wild type and AQP4 mice, providing a basis for future evaluation regarding its suitability for clinical studies.

No MeSH data available.


Related in: MedlinePlus