• Yukihiro Nakamura, Yuji Suzuki, Mika Tsujita, Vincent J Huber, Kenichi Yamada, and Tsutomu Nakada.
• Center for Integrated Human Brain Science, Brain Research Institute, University of Niigata , 1 Asahimachi, Niigata 951-8585, Japan.
• Acs Chem Neurosci. 2011 Oct 19; 2 (10): 568-571.

AbstractAquaporin 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 null mice, providing a basis for future evaluation regarding its suitability for clinical studies.

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