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Mechanisms of Action of Anxiolytics

    1. [1] University of Nantes
  • Localización: Psychiatry and Neuroscience Update: From Epistemology to Clinical Psychiatry – Vol. IV / Pascual Angel Gargiulo (ed. lit.), Humberto Luis Mesones Arroyo (ed. lit.), 2021, ISBN 978-3-030-61721-9, págs. 195-211
  • Idioma: inglés
  • Texto completo no disponible (Saber más ...)
  • Resumen
    • The discovery of benzodiazepine (BZD) receptors provided the impetus to discover and develop anxioselective anxiolytics. The beginning of an anxioselective mechanism of action was based on the γ-aminobutyric acid A (GABAA) receptor that resulted in clinical trials of multiple compounds. The BZD receptors were found to decrease brain serotonin (5HT) concentrations, so the second step was to find agonists or antagonists of 5HT receptors. Finally, serotonin reuptake inhibitors were used as anxiolytics. The serotonin receptors were explored to better understand the role of serotonin in the mechanism of action of anxiolytics. A part of this mechanism of action could be explained through glutamatergic action or neuropeptide regulation. The most studied neuropeptide was cholecystokinin which is a panicogenic agent, but unfortunately, to date there is no drug issued of this research. Other neuropeptides seem to play a role in anxiety disorders: corticotropin-releasing hormone, substance P and neurokinins, galanin, oxytocin, and atrial natriuretic peptide. Classic antidepressants, like tricyclics and SSRIs, have an anxiolytic activity which seems different from their antidepressant mechanism of action. The mechanism of action of anxiolytics is probably the result of the interaction of GABA and serotonin more or less modulated by neuropeptides. The role of glutamate is questionable as it regulates GABA activity. Adenosine interactions with serotonin and GABA could be an option.


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