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Use of NMDA antagonists for treatment of irritable bowel syndrome (IBS) and compounds with NMDA receptor antagonistic properties

机译:NMDA拮抗剂在治疗肠易激综合症(IBS)和具有NMDA受体拮抗作用的化合物中的用途

摘要

Described is the use of pharmaceutical compounds having NMDA antagonist activity for treating certain conditions in the gastrointestinal tract, such as functional gastrointestinal disorders, and in particular irritable bowel syndrome (IBS). Also described are pharmaceutical compositions to be used in the treatment of IBS and products comprising such compositions and a pharmaceutical acceptable carrier. Figure 5 shows the results for memantine and Figure 6 shows the corresponding results with 2-amidino-6- (2-amino-2- phenyl)-ethylpyridine. Results and conclusions: Intra-arterially injected memantine reduced, in a dose-dependent fashion, the pelvic nerve activity elicited by distension of the colon (80 mm Hg), as can be seen from Figure 5. The observations hereby provided are consistent with a model in which the non-competitive NMDA-antagonist memantine reduces the pelvic nerve activity elicited by colorectal distension by a peripheral mechanism of action. The data shown in Figure 6 was obtained when the experiment was repeated with 2amidino-6- (2-amino-2-phenyl)-ethylpyridine.
机译:描述了具有NMDA拮抗剂活性的药物化合物用于治疗胃肠道中的某些状况,例如功能性胃肠道疾病,特别是肠易激综合症(IBS)的用途。还描述了用于治疗IBS的药物组合物以及包含这种组合物和药学上可接受的载体的产品。图5显示了美金刚的结果,图6显示了2-ami基-6-(2-氨基-2-苯基)-乙基吡啶的相应结果。结果和结论:从图5可以看出,动脉内注射美金刚以剂量依赖性方式减少了结肠扩张(80 mm Hg)引起的盆腔神经活动。非竞争性NMDA拮抗剂美金刚胺通过外围作用机制降低大肠扩张引起的盆腔神经活动的模型。当用2-ami基-6-(2-氨基-2-苯基)-乙基吡啶重复实验时,获得图6所示的数据。

著录项

  • 公开/公告号NZ507436A

    专利类型

  • 公开/公告日2003-09-26

    原文格式PDF

  • 申请/专利权人 ASTRAZENECA AB;

    申请/专利号NZ19990507436

  • 申请日1999-04-28

  • 分类号A61K31/165;A61K31/13;A61K31/41;A61K31/44;A61K31/495;

  • 国家 NZ

  • 入库时间 2022-08-22 00:01:45

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