Department of Psychiatry, University of Illinois at Chicago, 1601 W. Taylor Street (MC 912), Chicago, IL, 60612, USA.
Department of Pharmaceutical Sciences, University of Colorado Anschutz Medical Campus, Aurora, USA.
Sci Rep. 2020 Oct 19;10(1):17629. doi: 10.1038/s41598-020-74605-9.
Delta opioid receptor (DOR) agonists have been identified as a promising novel therapy for headache disorders. DORs are broadly expressed in several peripheral and central regions important for pain processing and mood regulation; and it is unclear which receptors regulate headache associated symptoms. In a model of chronic migraine-associated pain using the human migraine trigger, nitroglycerin, we observed increased expression of DOR in cortex, hippocampus, and striatum; suggesting a role for these forebrain regions in the regulation of migraine. To test this hypothesis, we used conditional knockout mice with DORs deleted from forebrain GABAergic neurons (Dlx-DOR), and investigated the outcome of this knockout on the effectiveness of the DOR agonist SNC80 in multiple headache models. In DOR loxP controls SNC80 blocked the development of acute and chronic cephalic allodynia in the chronic nitroglycerin model, an effect that was lost in Dlx-DOR mice. In addition, the anti-allodynic effects of SNC80 were lost in a model of opioid induced hyperalgesia/medication overuse headache in Dlx-DOR conditional knockouts. In a model reflecting negative affect associated with migraine, SNC80 was only effective in loxP controls and not Dlx-DOR mice. Similarly, SNC80 was ineffective in the cortical spreading depression model of migraine aura in conditional knockout mice. Taken together, these data indicate that forebrain DORs are necessary for the action of DOR agonists in relieving headache-related symptoms and suggest that forebrain regions may play an important role in migraine modulation.
德尔塔阿片受体(DOR)激动剂已被确定为治疗头痛疾病的一种有前途的新疗法。DOR 在几个对疼痛处理和情绪调节很重要的外周和中枢区域广泛表达;目前尚不清楚哪种受体调节与头痛相关的症状。在使用人类偏头痛触发物硝酸甘油的慢性偏头痛相关疼痛模型中,我们观察到 DOR 在皮质、海马体和纹状体中的表达增加;这表明这些前脑区域在偏头痛的调节中起作用。为了验证这一假设,我们使用了 DOR 从 forebrain GABAergic 神经元(Dlx-DOR)中缺失的条件性敲除小鼠,并研究了这种敲除对 DOR 激动剂 SNC80 在多种头痛模型中的效果的影响。在 DOR loxP 对照中,SNC80 阻断了慢性硝酸甘油模型中急性和慢性头面部痛觉过敏的发展,而这种作用在 Dlx-DOR 小鼠中消失了。此外,在阿片类药物诱导的痛觉过敏/过度用药性头痛模型中,SNC80 的抗痛觉过敏作用在 Dlx-DOR 条件性敲除小鼠中消失了。在一个反映与偏头痛相关的负面情绪的模型中,SNC80 仅在 loxP 对照中有效,而在 Dlx-DOR 小鼠中无效。同样,SNC80 在皮质扩散抑制模型中对偏头痛先兆无效。综上所述,这些数据表明,前脑 DOR 对于 DOR 激动剂缓解与头痛相关的症状的作用是必要的,并表明前脑区域可能在偏头痛的调节中发挥重要作用。