强效且具选择性的基于金刚烷的小分子P2X(7)受体拮抗剂/白细胞介素-1β抑制剂的发现。
Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors.
作者信息
Furber Mark, Alcaraz Lilian, Bent Janice E, Beyerbach Armin, Bowers Keith, Braddock Martin, Caffrey Moya V, Cladingboel David, Collington John, Donald David K, Fagura Malbinder, Ince Frank, Kinchin Elizabeth C, Laurent Celine, Lawson Mandy, Luker Timothy J, Mortimore Michael M P, Pimm Austen D, Riley Robert J, Roberts Nicola, Robertson Mark, Theaker Jill, Thorne Philip V, Weaver Richard, Webborn Peter, Willis Paul
机构信息
Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leics, U.K.
出版信息
J Med Chem. 2007 Nov 29;50(24):5882-5. doi: 10.1021/jm700949w. Epub 2007 Oct 27.
A novel series of antagonists of the human P2X7 receptor is described. Modification of substituents enabled identification of compounds selective for the rat P2X7 receptor and provides useful pharmacological tools for evaluation of the role of P2X7 in disease.
本文描述了一系列新型的人P2X7受体拮抗剂。通过取代基修饰能够鉴定出对大鼠P2X7受体具有选择性的化合物，并为评估P2X7在疾病中的作用提供了有用的药理学工具。
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