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血清素 5-HT2B 受体的药物发现新兴机遇和关注点。

Emerging opportunities and concerns for drug discovery at serotonin 5-HT2B receptors.

机构信息

Departamento de Farmacología, Facultad de Farmacia. University of Santiago de Compostela. E-15782 Spain.

出版信息

Curr Top Med Chem. 2010;10(5):493-503. doi: 10.2174/156802610791111524.

DOI:10.2174/156802610791111524
PMID:20166944
Abstract

5-HT(2B) receptors have been reported to play an important role at cardiac, intestinal and central levels, as well as in bone marrow formation and growth. In the last decade, 5-HT(2B) receptors have also gained much attention as new targets in therapeutics, but also as off-targets because their activation along with the inhibition of serotonin transporters plays a significant role in the pathogenesis of 5-HT induced valvulopathy. Taking this into account, the present review focuses on the new therapeutic applications of 5-HT(2B) receptor ligands as well as on the potential concerns.

摘要

5-HT(2B)受体在心脏、肠道和中枢神经系统以及骨髓形成和生长中发挥着重要作用。在过去的十年中,5-HT(2B)受体也因其作为治疗靶点而备受关注,但也因其作为非靶点而备受关注,因为它们的激活以及 5-HT 诱导的瓣膜病发病机制中 5-羟色胺转运体的抑制作用发挥了重要作用。考虑到这一点,本综述重点介绍了 5-HT(2B)受体配体的新治疗应用以及潜在的关注点。

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