Characterization of Binding and Inhibitory Properties of TAK-063, a Novel Phosphodiesterase 10A Inhibitor

@inproceedings{Harada2015CharacterizationOB,
  title={Characterization of Binding and Inhibitory Properties of TAK-063, a Novel Phosphodiesterase 10A Inhibitor},
  author={Akina Harada and Kazunori Suzuki and Naomi Kamiguchi and Maki Miyamoto and Kimio Tohyama and Kosuke Nakashima and Takahiko Taniguchi and Haruhide Kimura},
  booktitle={PloS one},
  year={2015}
}
Phosphodiesterase 10A (PDE10A) inhibition is a novel and promising approach for the treatment of central nervous system disorders such as schizophrenia and Huntington's disease. A novel PDE10A inhibitor, TAK-063 [1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)-pyridazin-4(1H)-one] has shown high inhibitory activity and selectivity for human recombinant PDE10A2 in vitro; the half-maximal inhibitory concentration was 0.30 nM, and selectivity over other… CONTINUE READING

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