308242-39-9Relevant academic research and scientific papers
Identification and structure-activity studies of novel ultrashort-acting benzodiazepine receptor agonists
Stafford,, Jeffrey A.,Pacofsky,, Gregory J.,Cox, Richard F.,Cowan, Jill R.,Dorsey Jr., George F.,Gonzales, Stephen S.,Jung, David K.,Koszalka, George W.,McIntyre, Maggie S.,Tidwell, Jeffrey H.,Wiard, Robert P.,Feldman, Paul L.
, p. 3215 - 3218 (2002)
The synthesis and evaluation of novel ultrashort-acting benzodiazepine (USA BZD) agonists are 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.
SHORT-ACTING BENZODIAZEPINES
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Page/Page column 26; 27, (2008/06/13)
It has now been found that compounds of the present invention as described in Benzodiazepine derivatives of Formula (I) containing a carboxylic ester moiety and thereby capable of being inactivated by nonspecific tissue esterases in an organ-independent elimination mechanism and thereby providing a more predictable and reproducible pharmacodynamic profile. The compounds of the present invention are suitable for therapeutic purposes, including sedative-hypnotic, anxiolytic, muscle relaxant and anticonvulsant purposes and are useful to be administered intravenously in the following clinical settings: preoperative sedation, anxiolysis, and amnestic use for perioperative events; conscious sedation during short diagnostic, operative or endoscopic procedures; as a component for the induction and maintenance of general anesthesia, prior and/or concomitant to the administration of other anesthetic agents; ICU sedation.
