新型毒蕈碱受体变构调节剂的研发：拮抗剂AF-DX 384与六甲铵衍生物W84的杂合物
Development of a new type of allosteric modulator of muscarinic receptors: hybrids of the antagonist AF-DX 384 and the hexamethonio derivative W84.
作者信息
Mohr Marion, Heller Eberhard, Ataie Ameneh, Mohr Klaus, Holzgrabe Ulrike
机构信息
Institute of Pharmacy and Food Chemistry, Pharmaceutical Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany.
出版信息
J Med Chem. 2004 Jun 3;47(12):3324-7. doi: 10.1021/jm031095t.
Various fragments of the hexamethonio-type allosteric agent W84 were linked to the secondary amino group of the muscarinic M(2) acetylcholine receptor-preferring antagonist AF-DX 384 to increase the area of attachment with the allosteric site. Addition of only the phthalimido moiety of W84 gave an allosteric enhancer of NMS binding. Thus, a new lead structure for the development of allosteric enhancers of NMS binding has been discovered.
将六甲铵型变构剂W84的各种片段与毒蕈碱M(2)型乙酰胆碱受体选择性拮抗剂AF-DX 384的仲氨基相连，以增加与变构位点的结合面积。仅添加W84的邻苯二甲酰亚胺部分就得到了NMS结合的变构增强剂。因此，已发现一种用于开发NMS结合变构增强剂的新先导结构。
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