鉴定一系列新型非肽 NK3 受体拮抗剂。
Identification of a new series of non-peptidic NK3 receptor antagonists.
机构信息
Discovery Chemistry and DMPK, H. Lundbeck A/S, Valby, Denmark.
出版信息
Bioorg Med Chem Lett. 2011 Mar 1;21(5):1498-501. doi: 10.1016/j.bmcl.2010.12.135. Epub 2011 Jan 13.
PMID:21292483
Abstract
The identification and structure-activity relationships of 2-aminomethyl-1-aryl cyclopropane carboxamides as novel NK(3) receptor antagonists are reported. The compound series was optimized to give analogues with low nanomolar binding to the NK(3) receptor and brain exposure, leading to activity in vivo in the senktide-induced hypoactivity model in gerbils.
摘要
报告了 2-氨甲基-1-芳基环丙烷甲酰胺作为新型 NK(3)受体拮抗剂的鉴定和构效关系。该化合物系列经过优化，得到了对 NK(3)受体具有低纳摩尔结合亲和力和脑暴露的类似物，从而在沙土鼠的促啡肽诱导的低活性模型中具有体内活性。
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