ABSTRACT
The majority of anxiolytic and hypnotic agents currently used in therapy belong to the 1,4-benzodiazepine (BDZ) class, representing among the most commonly prescribed medications worldwide. Due to their safety, 1,4-BDZs have largely supplanted other sedative drugs since their clinical introduction in the early 1960s. The extensive studies performed on this class of drugs led to an in-depth definition of both the structure–activity relationships and the function on their biological target, namely, the GABAA receptor. The success of these drugs remains nowadays unconditioned, although safe agents with different structures entered the market more recently.
