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Discovery of potent, orally bioavailable, selective 5-HT1A/B/DReceptor antagonists

Ward, Simon, Eddershaw, Peter J., Scott, Claire M., Gordon, Laurie J., Lovell, Peter J., Moore, Susan H., Smith, Paul W., Starr, Kathryn R., Thewlis, Kevin M. and Watson, Jeannette M. 2008. Discovery of potent, orally bioavailable, selective 5-HT1A/B/DReceptor antagonists. Journal of Medicinal Chemistry 51 (10) , pp. 2887-2890. 10.1021/jm8001444

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5-HT1 receptor antagonists have been discovered with good selectivity over the 5-HT transporter. This is the first report of highly potent, selective ligands for the 5-HT1A/B/D receptors with low intrinsic activity, which represent a useful set of molecules for further understanding the roles of the 5-HT1 receptor subtypes and providing new approaches for the treatment of depression.

Item Type: Article
Date Type: Published Online
Status: Published
Schools: Medicine
Publisher: ACS Publications
ISSN: 0022-2623
Last Modified: 21 Feb 2018 11:57

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