Buspirone and related compounds as alternative anxiolytics

@article{Taylor1991BuspironeAR,
  title={Buspirone and related compounds as alternative anxiolytics},
  author={Duncan P. Taylor and Sandra L. Moon},
  journal={Neuropeptides},
  year={1991},
  volume={19},
  pages={15-19}
}

Anxiolytic effects of drugs acting on 5-HT receptor subtypes

Azapirones for the treatment of anxiety – an overview

Anxiety disorders belong to the most common psychiatric diagnosis. Over the years, benzodiazepines were considered the gold standard for pharmacological treatment of anxiety. They are effective

Augmentation of antipsychotic drug action by azapirone 5-HT1A receptor partial agonists: a meta-analysis.

5-HT1A partial agonists as adjunctive therapy improved overall psychopathology with a trend to improve positive symptoms in patients with schizophrenia.

Profile of action of 5-HT3 receptor antagonists, ondansetron and WAY 100289, in the elevated plus-maze test of anxiety of mice

It is suggested that the large within- and between-test variability observed with these compounds may indicate an action on mechanisms other than anxiety, as well as the enigmatic effects of 5-HT3 receptor antagonists in animal models of anxiety.

In vivo drug action of tandospirone at 5-HT1A receptor examined using positron emission tomography and neuroendocrine response

Despite the significant effect on growth hormone and body temperature, a clinical dose of tandospirone had a negligible effect on [11C]WAY 100635 binding, which indicates that the agonist produces a pharmacological effect without measurable occupancy, and a new index other than occupancy will be required for the in vivo evaluation of agonists.

References

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Buspirone, a new approach to the treatment of anxiety

  • Duncan P. Taylor
  • Biology, Psychology
    FASEB journal : official publication of the Federation of American Societies for Experimental Biology
  • 1988
Clinical studies have clearly demonstrated the efficacy of buspirone in the treatment of generalized anxiety disorder without the ancillary pharmacology of earlier anxiolytics, and recognize that action at 5‐HT1a receptors may be a viable approach to the pharmacotherapy of anxiety.

Serotonin Agents in Anxiety

  • Duncan P. Taylor
  • Psychology, Biology
    Annals of the New York Academy of Sciences
  • 1990
Investigation into Buspirone's mechanism of action revealed a key role for serotonin in the pharmacotherapy of anxiety, and a variety of serotonergic agents are now in preclinical and clinical development as anxiolytic agents, including 5-HT1A partial agonists,5-HT2 antagonists, and 5- HT3 antagonists.

Behavioral Models of Serotonin Receptor Activation

If functional relationships can be found, they may help provide answers regarding the mechanistic involvement of 5-HT both in normal and in abnormal behavior, and behavioral models may be applied to the discovery and further investigation of novel site-selective5-HT agonists and antagonists.

Autoradiographic localization of (3H) gepirone in the rat brain

Overall, the quantity of (3H)gepirone in each site correlated proportionally with known 5-HT{sub 1A} (in vitro) receptor binding.