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Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists
journal contribution
posted on 2023-06-07, 23:08 authored by Simon E Ward, Peter J Eddershaw, Claire M Scott, Laurie J Gordon, Peter J Lovell, Susan H Moore, Paul W Smith, Kathryn R Starr, Kevin M Thewlis, Jeannette M Watson5-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.
History
Publication status
- Published
Journal
Journal of Medicinal ChemistryISSN
0022-2623Publisher
ElsevierExternal DOI
Issue
10Volume
51Page range
2887-2890Department affiliated with
- Chemistry Publications
Full text available
- No
Peer reviewed?
- Yes