A2B型腺苷受体拮抗剂的研究进展

Advances in the study of A_(2B) adenosine receptor antagonists

A2B腺苷受体参与激活肥大细胞和炎症细胞的活性功能,选择性A2B腺苷受体作为潜在的药物靶点正逐渐成为一个充满希望的研究热点。本文对近年来国内外有关A2B腺苷受体拮抗剂的文献资料进行了分析和归纳。首先介绍了选择性A2B腺苷受体拮抗剂药理学作用和开发意义;然后对选择性A2B腺苷受体拮抗剂的开发现状、构效关系及拮抗剂与受体相互作用情况作了深入讨论;最后,对选择性A2B腺苷受体拮抗剂研发前景进行了展望。

A2B adenosine receptor is involved in the control of mast cell degranulation, interleukin-8 synthesis and cell growth. A2B adenosine receptor antagonists may serve as novel drugs for asthma, Alzheimer＇s disease, cystic fibrosis and type-Ⅱ diabetes. Therefore, seeking for the highly selective A2B adenosine receptor antagonists has been one of great interest. The molecular basis, structure-activity relationship of selective A2B adenosine receptor antagonists and their interactions with A2B adenosine receptor were reviewed.