Antinociceptive potency of enkephalins and enkephalinase inhibitors in the mouse model of colorectal distension—proof‐of‐concept,Chemical Biology & Drug Design

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Antinociceptive potency of enkephalins and enkephalinase inhibitors in the mouse model of colorectal distension—proof‐of‐concept
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2018-03-30 , DOI: 10.1111/cbdd.13186
Adam Fabisiak ₁ , Małgorzata Sobocińska ₂ , Elżbieta Kamysz ₂ , Jakub Fichna ₁ , Marta Zielińska ₁

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Irritable bowel syndrome (IBS) is a chronic disease characterized by abdominal pain and changes in bowel habits. Patients with IBS comprise a significant portion of attendants at the outpatient clinics. Targeting intestinal opioid receptors was found successful in alleviating pain and diarrhea—two major symptoms of IBS. In this study, we aimed to evaluate a novel potential pharmacological option: the use of enkephalinase inhibitors in therapy of visceral pain occurring in the course of IBS. We thus assessed the antinociceptive efficacy of enkephalins: Leu‐enkephalin and Met‐enkephalin, and enkephalinase inhibitors: opiorphin and sialorphin in the mouse model of visceral pain induced by colorectal distension. Leu‐enkephalin, Met‐enkephalin, and sialorphin, but not opiorphin, at the dose of 1 mg/kg injected subcutaneously potently decreased the visceromotor response to colon distension as compared to control. To conclude, enkephalinase inhibitors are worth being considered as potential therapeutics in patients with chronic abdominal pain and/or changed bowel habits, that is, suffering from IBS.

中文翻译：

脑啡肽和脑啡肽酶抑制剂在结直肠扩张小鼠模型中的抗伤害感受力-概念验证

肠易激综合症（IBS）是一种慢性疾病，其特征在于腹痛和排便习惯的改变。患有IBS的患者在门诊中占很大比例。发现靶向肠阿片受体可成功缓解疼痛和腹泻，这是IBS的两个主要症状。在这项研究中，我们旨在评估一种新的潜在药理学选择：脑啡肽酶抑制剂在IBS过程中发生的内脏疼痛的治疗中的使用。因此，我们在大肠扩张引起的内脏痛的小鼠模型中评估了脑啡肽：亮脑啡肽和甲乙脑啡，以及脑啡肽酶抑制剂：阿片啡和唾液酸吗啡的镇痛作用。亮脑啡肽，蛋氨酸脑啡肽和唾液酸蛋白，但不包括鸦片蛋白，与对照组相比，以1 mg / kg的剂量皮下注射可有效降低对结肠扩张的内脏运动反应。总之，对于慢性腹痛和/或排便习惯改变（即患有IBS）的患者，脑啡肽酶抑制剂值得考虑作为潜在的治疗方法。

更新日期：2018-03-30

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