Discovery of 1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one (TAK-063), a highly potent, selective, and orally active phosphodiesterase 10A (PDE10A) inhibitor.
第一作者:
Jun,Kunitomo
第一单位:
Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited , 26-1, Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan.
作者:
主题词
投药, 口服(Administration, Oral);动物(Animals);脑(Brain);结晶学, X线(Crystallography, X-Ray);环GMP(Cyclic GMP);药物设计(Drug Design);人类(Humans);半数抑制浓度(Inhibitory Concentration 50);男(雄)性(Male);小鼠(Mice);小鼠, 近交C57BL(Mice, Inbred C57BL);小鼠, 近交ICR(Mice, Inbred ICR);微粒体, 肝(Microsomes, Liver);运动(Movement)(Movement);苯环利定(Phencyclidine);磷酸二酯酶抑制剂(Phosphodiesterase Inhibitors);磷酸二酯水解酶类(Phosphoric Diester Hydrolases);蛋白质构象(Protein Conformation);吡唑类(Pyrazoles);哒嗪类(Pyridazines)
DOI
10.1021/jm5013648
PMID
25384088
发布时间
2014-11-26
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