Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.

Journal article

High-throughput screening of an array of biphenylmethylamines synthesised by high-throughput solid-phase chemistry resulted in the identification of compounds with high-affinity for the 5-ht5A receptor. The structure-activity relationship within this series and further array synthesis led to the identification of the biphenylmethylamine derivative 11, a potent and selective 5-ht5A receptor antagonist.

Authors: Corbett, D; Heightman, T; Moss, S; Bromidge, S; Coggon, SA

• Publication status: Published
• Journal: Bioorganic and medicinal chemistry letters
• Volume: 15
• Issue: 18
• Pages: 4014-4018
• Publication date: 2005-09-01
• DOI: 10.1016/j.bmcl.2005.06.024
• EISSN: 1464-3405
• ISSN: 0960-894X
• Language: English
• Keywords: Cell Line; Guanosine 5'-O-(3-Thiotriphosphate); Serotonin Antagonists; Structure-Activity Relationship; Guinea Pigs; Humans; Radioligand Assay; Receptors, Serotonin; Cricetinae; Animals; Drug Evaluation, Preclinical; Molecular Structure