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Literature DB >> 16002289

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

David F Corbett¹, Tom D Heightman, Stephen F Moss, Steven M Bromidge, Sara A Coggon, Mark J Longley, Ana Maria Roa, Jennifer A Williams, David R Thomas.

Abstract

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.

Entities: Chemical

Mesh：

Substances：

Year: 2005 PMID： 16002289 DOI： 10.1016/j.bmcl.2005.06.024

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

7 in total

1. The native serotonin 5-HT(5A) receptor: electrophysiological characterization in rodent cortex and 5-HT(1A)-mediated compensatory plasticity in the knock-out mouse.

Authors: Nathalie M Goodfellow; Craig D C Bailey; Evelyn K Lambe
Journal: J Neurosci Date: 2012-04-25 Impact factor: 6.167

2. The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.

Authors: Stephen P H Alexander; Helen E Benson; Elena Faccenda; Adam J Pawson; Joanna L Sharman; Michael Spedding; John A Peters; Anthony J Harmar
Journal: Br J Pharmacol Date: 2013-12 Impact factor: 8.739

3. Inactive and active state structures template selective tools for the human 5-HT_5A receptor.

Authors: Shicheng Zhang; He Chen; Chengwei Zhang; Ying Yang; Petr Popov; Jing Liu; Brian E Krumm; Can Cao; Kuglae Kim; Yan Xiong; Vsevolod Katritch; Brian K Shoichet; Jian Jin; Jonathan F Fay; Bryan L Roth
Journal: Nat Struct Mol Biol Date: 2022-07-14 Impact factor: 18.361

4. Structure-Based Design of a Chemical Probe Set for the 5-HT_5A Serotonin Receptor.

Authors: Anat Levit Kaplan; Ryan T Strachan; Joao M Braz; Veronica Craik; Samuel Slocum; Thomas Mangano; Vanessa Amabo; Henry O'Donnell; Parnian Lak; Allan I Basbaum; Bryan L Roth; Brian K Shoichet
Journal: J Med Chem Date: 2022-02-23 Impact factor: 8.039

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

1. The native serotonin 5-HT(5A) receptor: electrophysiological characterization in rodent cortex and 5-HT(1A)-mediated compensatory plasticity in the knock-out mouse.

2. The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.

3. Inactive and active state structures template selective tools for the human 5-HT_5A receptor.

4. Structure-Based Design of a Chemical Probe Set for the 5-HT_5A Serotonin Receptor.

5. (Biphenyl-4-yl)methylammonium chlorides: potent anticonvulsants that modulate Na+ currents.

6. Role of peripheral 5-HT_5A receptors in 5-HT-induced cardiac sympatho-inhibition in type 1 diabetic rats.

7. Antagonists of the serotonin receptor 5A target human breast tumor initiating cells.