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Notes:
- Buspirone decreases
dorsal raphe and hippocampal extracellular 5-HT concentrations via activation
of 5-HT1A somatodendritic autoreceptors in the dorsal raphe.
- Buspirone also
activates postsynaptic 5-HT1A receptors producing synaptic activity
that is independent of 5-HT, but may in part mimic the effects of 5-HT.
- Preclinical findings
predict that buspirone should have antidepressant activity, related
to partial agonism of 5-HT1A receptors.
- Chronic buspirone
administration desensitizes and down-regulates 5-HT1A somatodendritic
autoreceptors, which ultimately results in a recovery of the firing
activity of 5-HT neurons in the dorsal raphe.
- Buspirone
induces a partial 5-HT syndrome in rats.
- Buspirone
blocks 5-HT agonist-induced 5-HT syndrome.
- It acts in
rotational models of serotonergic activity.
- Buspirone
inhibits firing of dorsal raphe neurons while hyperpolarizing hippocampal
pyramidal cells.
- In behavioral
experiments with rats, buspirone reverses learned helplessness and
behavioral despair. Blier, 1994
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