DDD-028: 一种治疗糖尿病神经病变的有效、神经保护非阿片类化合物。
DDD-028: A Potent, Neuroprotective, Non-Opioid Compound for the Treatment of Diabetic Neuropathy.
发表日期：2023 Sep 08
作者：
Laura Micheli, Jagan Rajamoni, Lorenzo Di Cesare Mannelli, Parthasarathi Rajagopalan, Carla Ghelardini, Raghavan Rajagopalan
来源：
DIABETES & METABOLISM
摘要：
糖尿病神经病变（DN）是一种疼痛的慢性疾病，影响着全球糖尿病患者的大部分人口。目前的药物，例如普瑞巴林或度洛西汀，仅仅治疗与DN相关的疼痛症状，并不能改善神经损伤的根本问题。DDD-028（1）是一种小分子化合物，对于STZ诱导的DN啮齿动物模型具有强效的缓解疼痛活性。根据其他研究表明DDD-028能够抑制抗癌药物紫杉醇引起的星形胶质细胞增生和神经损伤，本研究认为DDD-028可以作为治疗DN的疾病改变性疗法的辅助选择。通过单晶X射线衍射确定了DDD-028的三维结构。版权所有 © 2023. Elsevier Ltd. 发布。
Diabetic neuropathy (DN) is a painful, chronic ailment that affects a large segment of diabetic population worldwide. Current medications such as pregabalin or duloxetine treat only the pain symptom associated with DN, but not the underlying nerve damage. DDD-028 (1) is a small molecule that displays potent pain-relieving activity in streptozotocin (STZ)-induced rodent model of DN. Combined with other studies indicating that DDD-028 suppresses astrogliosis and nerve damage induced by the anti-cancer drug, paclitaxel, the present study suggests that DDD-028 would be useful as a disease modifying therapeutic in the treatment of DN. The 3-dimensional structure of DDD-028 was confirmed by single crystal X-ray crystallography.Copyright © 2023. Published by Elsevier Ltd.