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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

Synthesis of [11C]TGN-020(a) n-BuLi, ether, He, −70 °C, 30 min. (b) [11C]CO2 (g), −70 °C, 3 min. (c) 2-Amino-1,3,4-thiadiazole, EDC·HCl, DMF, 50 °C, 5 min.
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sch1: Synthesis of [11C]TGN-020(a) n-BuLi, ether, He, −70 °C, 30 min. (b) [11C]CO2 (g), −70 °C, 3 min. (c) 2-Amino-1,3,4-thiadiazole, EDC·HCl, DMF, 50 °C, 5 min.


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)

Synthesis of [11C]TGN-020(a) n-BuLi, ether, He, −70 °C, 30 min. (b) [11C]CO2 (g), −70 °C, 3 min. (c) 2-Amino-1,3,4-thiadiazole, EDC·HCl, DMF, 50 °C, 5 min.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

sch1: Synthesis of [11C]TGN-020(a) n-BuLi, ether, He, −70 °C, 30 min. (b) [11C]CO2 (g), −70 °C, 3 min. (c) 2-Amino-1,3,4-thiadiazole, EDC·HCl, DMF, 50 °C, 5 min.
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