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Composition useful for treating respiratory disease, comprises a peptide that activates guanylate cyclase C, and is delivered to the apical membrane through the respiratory tract

机译:用于治疗呼吸系统疾病的组合物,其包含激活鸟苷酸环化酶C的肽,并通过呼吸道传递至顶膜

摘要

Medicine (A), in a formulation that is delivered to the apical membrane of mucosal epithelial cells through the respiratory tract, contains at least one peptide (I) that activates guanylate cyclase C (GCC). Independent claims are also included for the following: (1) Inhalation device containing (A); and (2) Diagnosing diseases that are accompanied by breathing disorders or disorders of mucus secretion in the respiratory tract, by detecting at least one (I). - ACTIVITY : Antiasthmatic; Antiinflammatory. No details of tests for these activities are given. - MECHANISM OF ACTION : Stimulation or activation of GCC, a G protein-coupled receptor that catalyzes conversion of guanosine triphophate to cyclic guanosine monophosphate (cGMP) and is present on the apical (air) side of respiratory epithelial cells but not on the basolateral (blood) side. cGMP activates membrane-associated type II protein kinase which in turn activates the regulatory domain of the cystic fibrosis transmembrane conductance regulator, resulting in secretion of chloride ions and water from the cells, causing fluidization of the mucus. No biological data given.
机译:通过呼吸道递送至粘膜上皮细胞的顶膜的制剂中的药物(A)包含至少一种激活鸟苷酸环化酶C(GCC)的肽(I)。还包括以下方面的独立权利要求:(1)包含(A)的吸入装置; (2)通过检测至少一种(I)来诊断伴随呼吸障碍或呼吸道粘液分泌障碍的疾病。 -活动:平喘;消炎(药。没有提供这些活动的测试详细信息。 -作用机理:GCC的刺激或激活,GCC是一种蛋白偶联受体,可催化鸟嘌呤三磷酸鸟嘌呤向环状单磷酸鸟苷(cGMP)的转化,并存在于呼吸道上皮细胞的顶端(空气)侧,而不是在基底外侧(血)方。 cGMP激活与膜相关的II型蛋白激酶,进而激活囊性纤维化跨膜电导调节剂的调节域,导致细胞中氯离子和水的分泌,导致粘液流化。没有给出生物学数据。

著录项

  • 公开/公告号DE20121564U1

    专利类型

  • 公开/公告日2003-04-17

    原文格式PDF

  • 申请/专利权人 SAVAS YUEKSEL;CETIN YALCIN;

    申请/专利号DE2001221564U

  • 发明设计人

    申请日2001-06-05

  • 分类号A61K38/10;

  • 国家 DE

  • 入库时间 2022-08-21 23:41:44

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