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仲丁基丙基乙酰胺(SPD)具有抗偏头痛特性。

sec-Butylpropylacetamide (SPD) has antimigraine properties.

作者信息

Kaufmann Dan, Bates Emily A, Yagen Boris, Bialer Meir, Saunders Gerald H, Wilcox Karen, White H Steve, Brennan K C

机构信息

Anticonvulsant Drug Development Program, Department of Pharmacology and Toxicology, University of Utah, USA Department of Neurology, University of Utah, USA.

Department of Pediatrics, University of Colorado Denver School of Medicine, USA.

出版信息

Cephalalgia. 2016 Sep;36(10):924-35. doi: 10.1177/0333102415612773. Epub 2015 Nov 13.

Abstract

BACKGROUND

Though migraine is disabling and affects 12%-15% of the population, there are few drugs that have been developed specifically for migraine prevention. Valproic acid (VPA) is a broad-spectrum antiepileptic drug (AED) that is also used for migraine prophylaxis, but its clinical use is limited by its side effect profile. sec-Butylpropylacetamide (SPD) is a novel VPA derivative, designed to be more potent and tolerable than VPA, that has shown efficacy in animal seizure and pain models.

METHODS

We evaluated SPD's antimigraine potential in the cortical spreading depression (CSD) and nitroglycerin (NTG) models of migraine. To evaluate SPD's mechanism of action, we performed whole-cell recordings on cultured cortical neurons and neuroblastoma cells.

RESULTS

In the CSD model, the SPD-treated group showed a significantly lower median number of CSDs compared to controls. In the NTG-induced mechanical allodynia model, SPD dose-dependently reduced mechanical sensitivity compared to controls. SPD showed both a significant potentiation of GABA-mediated currents and a smaller but significant decrease in NMDA currents in cultured cortical neurons. Kainic acid-evoked currents and voltage-dependent sodium channel currents were not changed by SPD.

CONCLUSIONS

These results demonstrate SPD's potential as a promising novel antimigraine compound, and suggest a GABAergic mechanism of action.

摘要

背景

尽管偏头痛会使人丧失能力,且影响12% - 15%的人口,但专门用于预防偏头痛的药物却很少。丙戊酸(VPA)是一种广谱抗癫痫药物(AED),也用于偏头痛预防,但其临床应用受到其副作用的限制。仲丁基丙基乙酰胺(SPD)是一种新型的VPA衍生物,设计得比VPA更有效且耐受性更好,已在动物癫痫和疼痛模型中显示出疗效。

方法

我们在偏头痛的皮质扩散性抑制(CSD)和硝酸甘油(NTG)模型中评估了SPD的抗偏头痛潜力。为了评估SPD的作用机制,我们对培养的皮质神经元和神经母细胞瘤细胞进行了全细胞记录。

结果

在CSD模型中,与对照组相比,SPD治疗组的CSD中位数显著更低。在NTG诱导的机械性异常性疼痛模型中,与对照组相比,SPD剂量依赖性地降低了机械敏感性。在培养的皮质神经元中,SPD既显著增强了GABA介导的电流,又使NMDA电流有较小但显著的降低。SPD对 kainic 酸诱发的电流和电压依赖性钠通道电流没有影响。

结论

这些结果证明了SPD作为一种有前景的新型抗偏头痛化合物的潜力,并提示了一种GABA能作用机制。

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sec-Butylpropylacetamide (SPD) has antimigraine properties.仲丁基丙基乙酰胺(SPD)具有抗偏头痛特性。
Cephalalgia. 2016 Sep;36(10):924-35. doi: 10.1177/0333102415612773. Epub 2015 Nov 13.

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