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Buspirone as a midbrain modulator: Anxiolysis unrelated to traditional benzodiazepine mechanisms
Author(s) -
Eison Michael S.,
Eison Arlene S.
Publication year - 1984
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430040112
Subject(s) - buspirone , neurochemical , neuroscience , dopamine , anxiolytic , psychology , stereotypy , benzodiazepine , serotonergic , pharmacology , serotonin , amphetamine , medicine , anxiety , psychiatry , receptor
Abstract Buspirone is a clinically effective anxiolytic unrelated to the benzodiazepines in structure and pharmacological properties. Recent mechanism of action studies suggest that rather than working through traditional benzodiazepine mechanisms, buspirone affects diverse aspects of the brain's neurochemical circuitry. It acts as a presynaptic dopamine antagonist with little potency at postsynaptic dopamine sites. This action may synergize with a GABA antagonist component to its action to alter activities in diverse brain systems. These actions can be hypothesized to relate to buspirone's behavioral effects: GABA (catalepsy reversal), corticostriatal glutarnate (stereotypy), acetylcholine (EEG activation and enhanced psycho‐motor performance), and mesolimbic, mesocortical dopamine in addition to midbrain norepinephrine and serotonin (anxiolysis). A hypothetical scheme of buspirone's effects on the brain based upon already established elements of its mechanism of action is presented. This scheme suggests that buspirone's unique anxioselective profile is derived from complex polysynaptic actions and their ramifications upon multiple neural substrates that collectively mediate anxiety.