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Treatment of the symptoms of bladder irritation

机译:膀胱刺激症状的治疗

摘要

1-(pyrid-4-ylamino)-indole (I), its salts and derivatives convertible to (I) in vivo are used to prepare a composition for treating symptoms of irritation of the bladder. An independent claim is included for the use of indole derivatives of formula (II) and their salts, to prepare a composition for treating symptoms of irritation of the bladder. R = group convertible into hydrogen by biotransformation. [Image] ACTIVITY : Uropathic. MECHANISM OF ACTION : (I) acts on the afferent pathway, reducing the frequency of contractions in the isolated bladder but not altering the maximum pressure of these contractions. (I) was tested using rat bladder model described in . (I), infused as a solution in saline, caused a dose-dependent reduction in the number of bladder contractions, e.g. at a dose of 3.5 mg/kg it reduced the number of contractions to 15% of that in a control. This concentration had no significant effect on the maximum pressure of those isovolumetric, rhythmic contractions that were not inhibited.
机译:1-(吡啶-4-基氨基)-吲哚(I),其盐和在体内可转化为(I)的衍生物用于制备治疗膀胱刺激症状的组合物。包括独立的权利要求,其涉及式(II)的吲哚衍生物及其盐在制备用于治疗膀胱刺激症状的组合物中的用途。 R =通过生物转化可转化为氢的基团。活动:空灵。作用机理:(I)作用于传入途径,减少了离体膀胱收缩的频率,但不改变这些收缩的最大压力。 (I)使用中所述的大鼠膀胱模型进行了测试。 (I),以盐溶液形式注入,引起膀胱收缩次数的剂量依赖性降低,例如剂量为3.5 mg / kg时,收缩次数减少至对照组​​的15%。该浓度对那些未被抑制的等体积,节律性收缩的最大压力没有明显影响。

著录项

  • 公开/公告号ZA200803240B

    专利类型

  • 公开/公告日2009-01-28

    原文格式PDF

  • 申请/专利权人 UROGENE;

    申请/专利号ZA20080003240

  • 发明设计人 BIENAYME HUGUES;FERTE JACQUES;

    申请日2008-04-11

  • 分类号A61K;A61P;

  • 国家 ZA

  • 入库时间 2022-08-21 19:25:16

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