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Review Article

塞来昔布作为潜在抑制剂在炎症性疾病治疗中的作用 - 综述

卷 29, 期 17, 2022

发表于: 12 January, 2022

页: [3028 - 3049] 页: 22

弟呕挨: 10.2174/0929867328666210910125229

价格: $65

摘要

本文旨在回顾塞来昔布作为治疗炎症性疾病的潜在抑制剂。环加氧酶（COX）主要具有两种亚型，称为环加氧酶1（COX-1）和环加氧酶2（COX-2）。前者在肾脏和血小板中起与稳态效应相关的构成作用，而后者主要负责炎症作用的诱导。由于COX-2在炎症性疾病的发病机制中起重要作用，因此它已被指示为抗炎中间体规划的目标。许多开发和计划用于COX-2抑制的抑制剂对人体有副作用，主要是在胃肠道和/或心血管。因此，有必要设计新的潜在的COX-2抑制剂，这些抑制剂相对安全且无副作用。从这个意义上说，塞来昔布是唯一有效的选择性COX-2抑制剂，仍然在商业上可用（在“coxib”家族中）。因此，塞来昔布成为开发COX-2酶抗炎剂的商业化原型抑制剂。该评价提供了抑制重点，应为设计有前途的新型非甾体抗炎药（NSAIDs）提供结构基础，这些药物作为COX-2抑制剂，对人体的副作用较小。

关键词: 炎症，环氧合酶-2，非甾体抗炎药，塞来昔布，ADME，毒性。

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