新型2-氨基四氢萘和3-氨基苯并二氢吡喃衍生物作为选择性5-羟色胺5-HT7受体激动剂和拮抗剂

Novel 2-aminotetralin and 3-aminochroman derivatives as selective serotonin 5-HT7 receptor agonists and antagonists.

作者信息

Holmberg Pär, Sohn Daniel, Leideborg Robert, Caldirola Patrizia, Zlatoidsky Pavel, Hanson Sverker, Mohell Nina, Rosqvist Susanne, Nordvall Gunnar, Johansson Anette M, Johansson Rolf

机构信息

Organic Pharmaceutical Chemistry, Uppsala University, Uppsala Biomedical Centre, Box 574, SE-751 23 Uppsala, Sweden.

出版信息

J Med Chem. 2004 Jul 29;47(16):3927-30. doi: 10.1021/jm0498102.

DOI:10.1021/jm0498102

PMID:15267230

Abstract

The understanding of the physiological role of the G-protein coupled serotonin 5-HT(7) receptor is largely rudimentary. Therefore, selective and potent pharmacological tools will add to the understanding of serotonergic effects mediated through this receptor. In this report, we describe two compound classes, chromans and tetralins, encompassing compounds with nanomolar affinity for the 5-HT(7) receptor and with good selectivity. Within theses classes, we have discovered both agonists and antagonists that can be used for further understanding of the pharmacology of the 5-HT(7) receptor.

摘要

对G蛋白偶联血清素5-HT(7)受体生理作用的了解在很大程度上还处于初级阶段。因此，选择性和强效的药理学工具将有助于加深对通过该受体介导的血清素能效应的理解。在本报告中，我们描述了两类化合物，即色满类和四氢萘类，其中包含对5-HT(7)受体具有纳摩尔亲和力且选择性良好的化合物。在这些类别中，我们发现了可用于进一步了解5-HT(7)受体药理学的激动剂和拮抗剂。