Mika Nakajima

Publications (2)5.47 Total impact

• Article: Synthesis, SAR studies, and evaluation of 1,4-benzoxazepine derivatives as selective 5-HT1A receptor agonists with neuroprotective effect: Discovery of Piclozotan.

  Katsuhide Kamei, Noriko Maeda, Kayoko Nomura, Makoto Shibata, Ryoko Katsuragi-Ogino, Makoto Koyama, Mika Nakajima, Teruyoshi Inoue, Tomochika Ohno, Toshio Tatsuoka
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  ABSTRACT: A new series of 1,4-benzoxazepine derivatives was designed, synthesized, and evaluated for binding to 5-HT1A receptor and cerebral anti-ischemic effect. A lot of compounds exhibited nanomolar affinity for 5-HT1A receptor with good selectivity over both dopamine D2 and alpha1-adrenergic receptors. Among these compounds, 3-chloro-4-[4-[4-(2-pyridinyl)-1,2,3,6-tetrahydropyridin-1-yl]butyl]-1, 4-benzoxazepin-5(4H)-one (50: SUN N4057 (Piclozotan) as 2HCl salt) showed remarkable neuroprotective activity in a transient middle cerebral artery occlusion (t-MCAO) model.
  Bioorganic & Medicinal Chemistry 04/2006; 14(6):1978-92. · 2.92 Impact Factor
• Article: New piperidinyl- and 1,2,3,6-tetrahydropyridinyl-pyrimidine derivatives as selective 5-HT1A receptor agonists with highly potent anti-ischemic effects.

  Katsuhide Kamei, Noriko Maeda, Ryoko Katsuragi-Ogino, Makoto Koyama, Mika Nakajima, Toshio Tatsuoka, Tomochika Ohno, Teruyoshi Inoue
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  ABSTRACT: A series of new piperidinyl- and 1,2,3,6-tetrahydropyridinyl-pyrimidine derivatives were synthesized. Among these compounds, 4-methyl-2-(1,2,3,6-tetrahydropyridin-4-yl)pyrimidine derivative 23 (SUN N5147) exhibited sub-nanomolar affinity for 5-HT1A receptor with 1000-fold selectivity over both dopamine D2 and alpha1-adrenergic receptors and remarkable neuroprotective activity in a transient middle cerebral artery occlusion (t-MCAO) model.
  Bioorganic & Medicinal Chemistry Letters 07/2005; 15(12):2990-3. · 2.55 Impact Factor