Linden J
University of Virginia Health Sciences Center, Charlottesville, 22908.
Trends Pharmacol Sci. 1994 Aug;15(8):298-306. doi: 10.1016/0165-6147(94)90011-6.
In this review, Joel Linden summarizes what is known about a new and intriguing member of the adenosine receptor family, the A3 receptor. This receptor exhibits unusually large differences in structure, tissue distribution and pharmacological properties between species. Rat A3 receptors are resistant to blockade by xanthine antagonists, but human and sheep A3 receptors can be potently blocked by certain xanthines, notably acidic 8-phenylxanthines. One function of the receptor is to facilitate degranulation of mast cells, and a role for mast cells and A3 receptors in mediating myocardial preconditioning has been proposed. Therefore, selective antagonists of A3 receptors have potential for the treatment of allergic, inflammatory and possibly ischaemic disorders.
在这篇综述中，乔尔·林登总结了关于腺苷受体家族的一个新的、有趣成员——A3受体的已知信息。该受体在不同物种之间的结构、组织分布和药理特性方面表现出异常大的差异。大鼠A3受体对黄嘌呤拮抗剂的阻断具有抗性，但人和绵羊的A3受体可被某些黄嘌呤有效阻断，尤其是酸性8-苯基黄嘌呤。该受体的一个功能是促进肥大细胞脱颗粒，并且有人提出肥大细胞和A3受体在介导心肌预处理中发挥作用。因此，A3受体的选择性拮抗剂具有治疗过敏、炎症以及可能的缺血性疾病的潜力。
