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Review Article

组胺 H3 和 Sigma-1 受体配体的双重靶向方法作为治疗 CNS 相关疾病的有前景的药理学工具

卷 28, 期 15, 2021

发表于: 06 August, 2020

页: [2974 - 2995] 页: 22

弟呕挨: 10.2174/0929867327666200806103144

价格: $65

摘要

随着最近 Pitolisant (WakixR) 的市场批准，新型多功能组胺 H3 受体拮抗剂的临床应用兴趣明显增加。许多制药公司和学术机构已经合成了不同 H3R 药效团与其他 G 蛋白偶联受体、转运蛋白或酶的药效团元件的几种组合。由于中枢神经系统疾病的特点是多种生理功能障碍和信号通路复杂网络的失调，因此最佳的多能药物应同时且特别地调节选定的生物靶标组。有趣的是，最近的研究表明，一些临床评估的组胺 H3 受体拮抗剂对 sigma-1 受体结合位点具有纳摩尔的亲和力，表明这种特性可能在其整体功效中发挥作用。 sigma-1 受体是一种不寻常但又不为人知的蛋白质，应该通过神经保护和神经可塑性参与许多中枢神经系统病理学。这两种不同的生物结构，组胺 H3 和 sigma-1 受体相结合，可以代表治疗多种人类疾病的治疗发展的潜在富有成效的目标。

关键词: 组胺 H3 受体、sigma-1 受体、双靶向配体、Pitolistant、CNS 病理学、H3R 药效团。

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