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埃卢克萨多林 (Viberzi) 的内脏镇痛作用:一个中心作用的作用
Jyoti N Sengupta1, Maia Terashvili1, Bidyut K Medda1
1Division of Gastroenterology & Hepatology, Medical College of Wisconsin, Milwaukee, Wisconsin.
埃卢克萨多林通过作用于脊髓神经元而不是外围神经来缓解结肠和膀疼痛. 这种双功能阿片类连接体为IBS和PBS等疾病的疼痛缓解提供了中心机制.
科学领域:
- 神经科学是一个神经科学.
- 药理学 药理学是指药理学的学科.
- 胃肠病学 胃肠病学
背景情况:
- 疼痛性膀综合征 (PBS) 和刺激性肠综合征 (IBS) 影响全球数百万人,有效治疗方法有限.
- 目前用于PBS和IBS的治疗方法通常会导致不良影响,包括便秘和阿片类药物使用成.
研究的目的:
- 阐明埃卢克萨多林 (ELX) 在内脏疼痛通路中的中央止痛机制.
- 为了确定ELX的缓解疼痛效果是否发生在外围或中心.
主要方法:
- 在ELX和阿片类受体对抗剂的存在下,对器官张张的视觉运动反应 (VMR) 被记录下来.
- 用外围 (纳洛 - 甲化物) 和中央 (纳洛) 抗剂来区分作用部位.
- 电生理学评估了ELX对脊髓神经元和内脏 afferent 纤维的影响.
主要成果:
- 埃卢克萨多林 (ELX) 抑制了VMRs,表明减少了疼痛.
- 中枢纳洛,但不是外围纳洛-甲化,逆转了ELX诱导的VMR抑制,这表明了作用的中心部位.
- ELX减弱了参与膀和结肠疼痛信号传递的脊髓神经元的激发,而不会影响外围 afferent 纤维.
结论:
- 埃卢克萨多林 (ELX) 通过中央机制对结肠和膀疼痛产生镇痛.
- ELX通过调节腰椎神经元 (L6-S1) 脊髓神经元的活动来起作用,与其对肠道运动的外围影响不同.
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