ASP5736, a novel 5-HT5A receptor antagonist, ameliorates positive symptoms and cognitive impairment in animal models of schizophrenia

@article{Yamazaki2014ASP5736AN,
  title={ASP5736, a novel 5-HT5A receptor antagonist, ameliorates positive symptoms and cognitive impairment in animal models of schizophrenia},
  author={Mayako Yamazaki and Katsuya Harada and Noriyuki Yamamoto and Junko Yarimizu and Mayuko Okabe and Takeshi Shimada and Keni Ni and Nobuya Matsuoka},
  journal={European Neuropsychopharmacology},
  year={2014},
  volume={24},
  pages={1698-1708}
}
We recently identified ASP5736, (N-(diaminomethylene)-1-(3,5-difluoropyridin-4-yl)-4-fluoroisoquinoline-7-carboxamide (2E)-but-2-enedioate), a novel antagonist of 5-HT5A receptor, and here describe the in vitro and in vivo characterization of this compound. ASP5736 exhibited a high affinity for the human 5-HT5A receptor (Ki = 3.6 ± 0.66 nM) and antagonized 5-carboxamidotryptamine (5-CT)-induced Ca(2+) influx in human cells stably expressing the 5-HT5A receptor with approximately 200-fold… CONTINUE READING
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