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Identification and structure-activity studies of novel ultrashort-acting benzodiazepine receptor agonists |
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| Authors: | Stafford Jeffrey A Pacofsky Gregory J Cox Richard F Cowan Jill R Dorsey George F Gonzales Stephen S Jung David K Koszalka George W McIntyre Maggie S Tidwell Jeffrey H Wiard Robert P Feldman Paul L |
| Affiliation: | GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA. |
| Abstract: | The synthesis and evaluation of novel ultrashort-acting benzodiazepine (USA BZD) agonists is described. A BZD scaffold was modified by incorporation of amino acids and derivatives. The propionate side chain of glutamic acid tethers an enzymatically labile functionality where the metabolite carboxylic acid displays markedly reduced BZD receptor affinity. The USA BZDs were characterized by full agonism profiles. Copyright2000 Elsevier Science Ltd. |
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