Development of a Novel Ligand, [C-11]TGN-020, for Aquaporin 4 Positron Emission Tomography Imaging

作者：Nakamura Yukihiro; Suzuki Yuji; Tsujita Mika; Huber Vincent J; Yamada Kenichi; Nakada Tsutomu^*

来源：ACS Chemical Neuroscience, 2011, 2(10): 568-571.

DOI：10.1021/cn2000525

• Aquaporin 4
• positron emission tomography
• C-11
• TGN-020

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 [C-11]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.

• 出版日期2011-10