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Buspirone is classified in the azapirone drug class. It has a strong affinity for serotonin 5HT1a receptors, where it acts as a partial agonist, which some researchers believe produces the preponderance of clinical effects.

It also has a weak affinity for serotonin 5HT2 receptors and acts as a weak antagonist on dopamine D2 autoreceptors. There is no effect on benzodiazepine GABA receptors.