...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >M(4) agonists/5HT(7) antagonists with potential as antischizophrenic drugs: Serominic compounds.
【24h】

M(4) agonists/5HT(7) antagonists with potential as antischizophrenic drugs: Serominic compounds.

机译：M（4）激动剂/ 5HT（7）拮抗剂，有可能作为抗精神分裂症药物：血清素化合物。

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Chronic low-dose treatment of rats with the psychomimetic drug, phencyclidine, induces regionally specific metabolic and neurochemical changes in the CNS that mirror those observed in the brains of schizophrenic patients. Recent evidence suggests that drugs targeting serotoninergic and muscarinic receptors, and in particular 5-HT(7) antagonists and M(4) agonists, exert beneficial effects in this model of schizophrenia. Compounds that display this combined pattern of activity we refer to as serominic compounds. Based upon leads from natural product screening, we have designed and synthesised such serominic compounds, which are principally arylamidine derivatives of tetrahydroisoquinolines, and shown that they have the required serominic profile in ligand binding assays and show potential antipsychotic activity in functional assays.
机译：用拟精神病药物苯环利定对大鼠进行长期低剂量治疗，可在CNS中引起区域特异性的代谢和神经化学变化，与精神分裂症患者大脑中观察到的变化相似。最近的证据表明，针对5-羟色胺能和毒蕈碱受体的药物，尤其是5-HT（7）拮抗剂和M（4）激动剂，在这种精神分裂症模型中发挥有益作用。表现出这种结合的活性模式的化合物我们称为血清素化合物。基于天然产物筛选的线索，我们设计并合成了此类血清素化合物，这些化合物主要是四氢异喹啉的芳胺衍生物，并显示它们在配体结合测定中具有所需的血清素谱，并在功能测定中显示出潜在的抗精神病活性。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号