Cortex Pharmaceuticals Inc., 15231 Barranca Parkway, Irvine, CA 92618, USA.
Bioorg Med Chem Lett. 2011 Oct 15;21(20):6170-5. doi: 10.1016/j.bmcl.2011.07.098. Epub 2011 Aug 12.
AMPA receptors (AMPARs) have been demonstrated to be an important therapeutic CNS target. A series of substituted benzotriazinone and benzopyrimidinone derivatives were prepared with the aim to improve in vivo activity over the previously reported bis-benzoxazinone based AMPAKINE series from our laboratory. These compounds were shown to be potent, positive allosteric AMPAR modulators that have better in vivo activity and improved metabolic stability over the analogous benzoxazinone derivatives.
AMPA 受体（AMPA 受体）已被证明是中枢神经系统的重要治疗靶点。本研究旨在通过一系列取代的苯并三嗪酮和苯并嘧啶酮衍生物，改善之前实验室报道的基于双苯并恶嗪酮的 AMPAKINE 系列化合物的体内活性。这些化合物被证明是有效的、正变构的 AMPA 受体调节剂，与类似的苯并恶嗪酮衍生物相比，具有更好的体内活性和改善的代谢稳定性。
