Deng, XY; Zhang, YD; Chen, Z; Kumata, K; Van, R; Rong, J; Shao, T; Hatori, A; Mori, W; Yu, QZ; Hu, K; Fujinaga, M; Wey, HY; Shao, YH; Josephson, L; Murtas, G; Pollegioni, L; Zhang, MR; Liang, S in [Deng, Xiaoyun; Chen, Zhen; Rong, Jian; Shao, Tuo; Yu, Qingzhen; Wey, Hsiao-Ying; Josephson, Lee; Liang, Steven] Massachusetts Gen Hosp, Dept Radiol, 55 Fruit St, Boston, MA 02114 USA; [Deng, Xiaoyun; Chen, Zhen; Rong, Jian; Shao, Tuo; Yu, Qingzhen; Wey, Hsiao-Ying; Josephson, Lee; Liang, Steven] Harvard Med Sch, 55 Fruit St, Boston, MA 02114 USA; [Zhang, Yiding; Kumata, Katsushi; Hatori, Akiko; Mori, Wakana; Hu, Kuan; Fujinaga, Masayuki; Zhang, Ming-Rong] Natl Inst Quantum & Radiol Sci & Technol, Natl Inst Radiol Sci, Dept Radiopharmaceut Dev, Chiba 2638555, Japan; [Van, Richard; Shao, Yihan] Univ Oklahoma, Dept Chem & Biochem, Norman, OK 73019 USA; [Murtas, Giulia; Pollegioni, Loredano] Univ Insubria, Dipartimento Biotecnol & Sci Vita, I-21100 Varese, Italy published Synthesis and preliminary evaluation of 4-hydroxy-6-(3-[C-11]methoxyphenethyl)pyridazin-3(2H)-one, a C-11-labeled D-amino acid oxidase (DAAO) inhibitor for PET imaging in 2020.0, Cited 45.0. Category: indole-building-block. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6.
Selective DAAO inhibitors have demonstrated promising therapeutic effects in clinical studies, including clinically alleviating symptoms of schizophrenic patients and ameliorating cognitive function in Alzheimer’s patients with early phase. Herein we report the synthesis and preliminary evaluation of a C-11-labeled positron emission tomography ligand based on a DAAO inhibitor, DAO-1903 (8). C-11-Isotopologue of 8 was prepared in high radiochemical yield with high radiochemical purity (> 99%) and high molar activity (> 37 GBq/umol). In vitro autoradiography studies indicated that the ligand possessed high in vitro specific binding to DAAO, while in vivo dynamic PET studies demonstrated that [C-11]8 failed to cross the blood-brain barrier possibly due to moderate brain efflux mechanism. Further chemical scaffold optimization is necessary to overcome limited brain permeability and improve specific binding.
Category: indole-building-block. About Benzyl Alcohol, If you have any questions, you can contact Deng, XY; Zhang, YD; Chen, Z; Kumata, K; Van, R; Rong, J; Shao, T; Hatori, A; Mori, W; Yu, QZ; Hu, K; Fujinaga, M; Wey, HY; Shao, YH; Josephson, L; Murtas, G; Pollegioni, L; Zhang, MR; Liang, S or concate me.
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles