Tricyclic pyridones as functionally selective human GABAA alpha 2/3 receptor-ion channel ligands |
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| Authors: | Crawforth James Atack John R Cook Susan M Gibson Karl R Nadin Alan Owens Andrew P Pike Andrew Rowley Michael Smith Alison J Sohal Bindi Sternfeld Francine Wafford Keith Street Leslie J |
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| Affiliation: | Department of Medicinal Chemistry, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK. james_crawforth@merck.com |
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| Abstract: | A series of tricyclic pyridones has been evaluated as benzodiazepine site ligands with functional selectivity for the alpha(3) over the alpha(1) containing subtype of the human GABA(A) receptor ion channel. This investigation led to the identification of a high affinity, functionally selective, orally bioavailable benzodiazepine site ligand that demonstrated activity in rodent anxiolysis models and reduced sedation relative to diazepam. |
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