Introduction: Physical, chemical, thermal injuries along with infectious diseases lead to acute pain with associated inflammation, being the primary cause of hospital visits. Moreover, neuropathic pain associated with diabetes is a serious chronic disease leading to high morbidity and poor quality of life.
Objective: Earlier multiple sulphonamides have been reported to have an antinociceptive and antiallodynic profile. 4-Fluoro-N-(4-sulfamoylbenzyl) Benzene Sulfonamide (4-FBS), a synthetic sulfonamide with reported carbonic anhydrase inhibitory activity, was investigated for its potential effects in mice model of acute and diabetic neuropathic pain.
Methods and Results: 4-FBS was given orally (p.o.) one hour before the test and then mice were screened for antinociceptive activity by using the tail immersion test, which showed significant antinociceptive effect at both 20 and 40 mg/kg doses. To explore the possible mechanisms, thermal analgesia of 4-FBS was reversed by the 5HT₃ antagonist ondansetron 1mg/kg intraperitoneally (i.p.) and by the μ receptor antagonist naloxone (1 mg/kg i.p.), implying possible involvement of serotonergic and opioidergic pathways in the analgesic effect of 4-FBS. Diabetes was induced in mice by a single dose of streptozotocin (STZ) 200 mg/kg i.p. After two weeks, animals first became hyperalgesic and progressively allodynic in the fourth week, which was evaluated through behavioral parameters like thermal and mechanical tests. 4-FBS at 20 and 40 mg/kg p.o. significantly reversed diabetes-induced hyperalgesia and allodynia at 30, 60, 90, and 120 minutes.
Conclusion: These findings are significant and promising while further studies are warranted to explore the exact molecular mechanism and the potential of 4-FBS in diabetic neuropathic pain.

Keywords: sulfonamides, streptozotocin; STZ, antinociception, diabetes mellitus; DM, neuropathic pain, von Frey filaments


中文翻译：

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4-氟-N-(4-磺酰基苄基)苯磺酰胺在小鼠疼痛模型中的镇痛和抗异常疼痛作用

简介：物理、化学、热损伤以及传染病导致急性疼痛并伴有炎症，是就诊的主要原因。此外，与糖尿病相关的神经性疼痛是一种严重的慢性疾病，导致高发病率和低生活质量。
目的：早期已报道多种磺胺类药物具有镇痛和抗异常疼痛作用。4-氟-N-(4-氨磺酰苄基)苯磺酰胺 (4-FBS) 是一种合成磺酰胺，据报道具有碳酸酐酶抑制活性，研究了其对急性和糖尿病神经性疼痛小鼠模型的潜在影响。
方法与结果：试验前1小时口服4-FBS，然后通过尾部浸入试验筛选小鼠的镇痛活性，20和40mg/kg剂量均显示出显着的镇痛作用。为了探索可能的机制，5HT ₃拮抗剂昂丹司琼 1mg/kg 腹腔注射 (ip) 和 μ 受体拮抗剂纳洛酮 (1 mg/kg ip) 可逆转 4-FBS 的热镇痛作用，这意味着可能涉及血清素能和阿片能途径4-FBS 的镇痛作用。通过腹腔注射单剂量链脲佐菌素 (STZ) 200 mg/kg 诱导小鼠患糖尿病。两周后，动物首先出现痛觉过敏，并在第四周逐渐出现异常性疼痛，通过热和机械测试等行为参数进行评估。口服 20 和 40 mg/kg 4-FBS 在 30、60、90 和 120 分钟时可显着逆转糖尿病引起的痛觉过敏和异常性疼痛。
结论：这些发现意义重大且充满希望，同时需要进一步研究来探索 4-FBS 在糖尿病神经性疼痛中的确切分子机制和潜力。

关键词：磺胺类药物，链脲佐菌素；STZ、镇痛、糖尿病；DM、神经性疼痛、冯弗雷丝