Imidazo[1,2-b][1,2,4]triazines as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety |
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| Authors: | Jennings Andrew S R Lewis Richard T Russell Michael G N Hallett David J Street Leslie J Castro José L Atack John R Cook Susan M Lincoln Rachael Stanley Joanna Smith Alison J Reynolds David S Sohal Bindi Pike Andrew Marshall George R Wafford Keith A Sheppard Wayne F A Tye Spencer J |
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| Institution: | Neuroscience Research Centre, Merck Sharp and Dohme Research Laboratories, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK. andrew_jennings@merck.com |
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| Abstract: | Imidazo1,2-a]pyrimidines and imidazo1,2-b]1,2,4]triazines are ligands for the benzodiazepine binding site of GABA(A) receptors that are functionally selective for the alpha2/alpha3 subtypes over the alpha1 subtype. SAR studies to optimise this functional selectivity, pharmacokinetic and behavioural data are described. |
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