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对pH敏感的阿片类药物在肠炎的小鼠模型中不表现出止痛耐受性

Claudius E Degro^1,2, Nestor Nivardo Jiménez-Vargas¹, Mabel Guzman-Rodriguez¹

¹Gastrointestinal Diseases Research Unit, Kingston General Hospital, Queen's University, Kingston, Ontario, Canada.

British journal of pharmacology

|October 13, 2024

概括

一种新的pH敏感阿片类药物NFEPP避免了炎症性疼痛模型中的耐受性发展,与芬太尼不同. 这可以防止剂量升级,减少与阿片类药物治疗相关的副作用和成风险.

科学领域:

药理学药理学是指药理学的学科.
神经科学是一个神经科学.
疼痛管理疼痛管理

背景情况:

阿片类药物耐受性导致剂量升级,增加副作用和成风险.
传统的阿片类药物,如芬太尼,诱导耐受性,使疼痛管理复杂化.
需要新的止痛药来缓解阿片类药物耐受性和相关危害.

研究的目的:

为了比较对芬太尼的耐受性发展与一种新的pH敏感μ-阿片类受体 (MOR) 激动剂NFEPP相比.
调查NFEPP是否仅在酸性炎症环境中活跃,可以防止阿片类药物耐受性.
评估NFEPP在炎症性疼痛模型中的 nociception 和交叉耐受性的影响.

主要方法:

在患有牛硫酸大肠炎的小鼠中,在5天内诱导了阿片类药物耐受性.
视觉 nociception 通过视觉运动反应 (VMRs) 和结肠 afferent 神经活动进行测量.
使用尾部浸泡试验评估了体质热性 nociception;监测了心肺呼吸系统的影响.

主要成果:

在炎症性疼痛模型中,小鼠对芬太尼产生了耐受性,但对NFEPP没有.
与芬太尼尔观察到交叉耐受性,但与NFEPP没有.
与芬太尼尔治疗的小鼠不同的是,接受NFEPP治疗的小鼠在结肠 afferents和背部根结质神经元中显示了保留的MOR激动反应.

结论:

与芬太尼相比,NFEPP不会在炎症性疼痛环境中诱导耐受性.
这种缺乏耐受性可以消除在发育炎症期间需要剂量升级的需要.
NFEPP提供了一种潜在的策略,以减轻阿片类药物的副作用和成风险.

关键词:

它们的pH值为pH.这是一个宽容的宽容度.这是一种内在的感觉 (visceral nociception).μ-阿片类受体激活剂.

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