Azapirones: history of development.
The azapirones, a unique pharmacologic class that includes buspirone and gepirone appear to offer the promise of both antidepressant and anxiolytic activity. Their singular affinity for the serotonin (5-hydroxytryptamine [5-HT]) type 1A (5-HT1A) receptor subtype may be the factor responsible for the therapeutic activity of these agents. It is hoped that the distinctive characteristics of this new class of drugs will lead to effective therapy for the treatment of mood disorders without the adverse or ancillary effects associated with currently available agents such as the benzodiazepines. The development of drugs for the treatment of anxiety has gradually evolved from less selective agents, such as alcohol, opiates, and the bromides, to progressively more specific drugs, leading ultimately to the development of the benzodiazepine anxiolytics in 1959. The approval of the azapirone buspirone in 1986 marked a new era of psychotherapeutic drug therapy. There is now evidence that this new generation of anxiolytic drugs may offer antidepressant potential in addition to its anxiolytic properties.
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CNS Special Projects, Bristol-Myers Squibb Company, Wallingford, CT 06492-7660.
D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology; D001143:Arousal / Q000187:drug effects*; D001522:Behavior, Animal / Q000187:drug effects; D001921:Brain / Q000187:drug effects*; D002065:Buspirone / Q000266:history* / Q000494:pharmacology; D002621:Chemistry; D049673:History, 20th Century; D006801:Humans; D011743:Pyrimidines / Q000266:history* / Q000494:pharmacology; D011985:Receptors, Serotonin / Q000187:drug effects*; D013329:Structure-Activity Relationship
D014151:Anti-Anxiety Agents; D011743:Pyrimidines; D011985:Receptors, Serotonin; C039979:gepirone; D002065:Buspirone