作为IK（Ca）通道阻滞剂的4-苯基-4H-吡喃
4-Phenyl-4H-pyrans as IK(Ca) channel blockers.
作者信息
Urbahns Klaus, Horváth Ervin, Stasch Johannes Peter, Mauler Frank
机构信息
Institute of Medicinal Chemistry, Pharma Research Center, Bayer AG, D-42096, Wuppertal, Germany.
出版信息
Bioorg Med Chem Lett. 2003 Aug 18;13(16):2637-9. doi: 10.1016/s0960-894x(03)00560-2.
Abstract
4-Phenyl-4H-pyrans have been identified as potent and specific IK(Ca) channel blockers. Their synthesis and structure-activity relationships are described. A selected derivative, rac-11, reduces the infarct volume in a rat subdural hematoma model of traumatic brain injury after iv administration.
摘要
4-苯基-4H-吡喃已被确定为强效且特异性的IK(Ca)通道阻滞剂。文中描述了它们的合成方法及构效关系。一种选定的衍生物rac-11，在静脉给药后可减少创伤性脑损伤大鼠硬膜下血肿模型中的梗死体积。
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