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阿替利珠单抗 - 一种口服 CGRP 拮抗剂 - 通过 CSD 减弱脑膜伤害感受器的激活。

Atogepant - an orally-administered CGRP antagonist - attenuates activation of meningeal nociceptors by CSD.

机构信息

Department of Anesthesia, Critical Care and Pain Medicine, Beth Israel Deaconess Medical Center.

Harvard Medical School, Boston, Massachusetts, USA.

出版信息

Cephalalgia. 2022 Aug;42(9):933-943. doi: 10.1177/03331024221083544. Epub 2022 Mar 25.

Abstract

BACKGROUND

This study investigated the mechanism of action of atogepant, a small-molecule CGRP receptor antagonist recently approved for the preventive treatment of episodic migraine, by assessing its effect on activation of mechanosensitive C- and Aδ-meningeal nociceptors following cortical spreading depression.

METHODS

Single-unit recordings of trigeminal ganglion neurons (32 Aδ and 20 C-fibers) innervating the dura was used to document effects of orally administered atogepant (5 mg/kg) or vehicle on cortical spreading depression-induced activation in anesthetized male rats.

RESULTS

Bayesian analysis of time effects found that atogepant did not completely prevent the activation of nociceptors at the tested dose, but it significantly reduced response amplitude and probability of response in both the C- and the Aδ-fibers at different time intervals following cortical spreading depression induction. For C-fibers, the reduction in responses was significant in the early phase (first hour), but not delayed phase of activation, whereas in Aδ-fibers, significant reduction in activation was apparent in the delayed phase (second and third hours) but not early phase of activation.

CONCLUSIONS

These findings identify differences between the actions of atogepant, a small molecule CGRP antagonist (partially inhibiting both Aδ and C-fibers) and those found previously for fremanezumab, a CGRP-targeted antibody (inhibiting Aδ fibers only) and onabotulinumtoxinA (inhibiting C-fibers only)- suggesting that these agents differ in their mechanisms for the preventive treatment of migraine.

摘要

背景

本研究通过评估其在皮质扩散性抑制后对机械敏感 C 和 Aδ 脑膜伤害感受器激活的影响,研究了小分子 CGRP 受体拮抗剂 atogepant(最近被批准用于预防性治疗阵发性偏头痛)的作用机制。

方法

使用记录三叉神经节神经元(32 个 Aδ 和 20 个 C 纤维)的单一单位,记录口服 atogepant(5mg/kg)或载体对麻醉雄性大鼠皮质扩散性抑制诱导激活的影响。

结果

时间效应的贝叶斯分析发现,atogepant 不能完全阻止在测试剂量下伤害感受器的激活,但它在皮质扩散性抑制诱导后不同时间间隔内显著降低了 C 和 Aδ 纤维的反应幅度和反应概率。对于 C 纤维,在早期(第一小时)反应明显减少,但在激活的延迟期(第二和第三小时)没有减少,而对于 Aδ 纤维,在激活的延迟期明显减少,但在早期没有减少。

结论

这些发现表明,atogepant(一种小分子 CGRP 拮抗剂)的作用与以前发现的 fremanezumab(一种 CGRP 靶向抗体)和 onabotulinumtoxinA(仅抑制 C 纤维)之间存在差异,这表明这些药物在预防偏头痛方面的作用机制不同。

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