Preclinical Pharmacology of Buspirone Hydrochloride

Buspirone is an azaspirodecanedione that has anxiolytic actions in man and anticonflict actions in experimental animals. In contrast to many commonly used anxiolytic agents, buspirone does not appear to have significant sedative, muscle relaxant or anticonvulsant actions. Consequently, it has been termed an “anxioselective” agent. The effects of buspirone and related compounds have been examined in a number of neurotransmitter systems that have been linked to the actions of other anxiolytic agents. Buspirone has been shown to affect dopaminergic, serotonergic and noradrenergic pathways, as well as the GABA‐benzodiazepine receptor chloride ionophore complex. Nonetheless, the doses (in vivo) and/or concentrations (in vitro) of buspirone (and related compounds) needed to affect these systems are not consistent with a causal relationship between the anxiolytic actions of buspirone and any of these systems. The neurochemical mechanism by which buspirone and related compounds exert both anticonflict and anxiolytic actions remains unknown. 1984 Pharmacotherapy Publications Inc.