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Buspirone hydrochloride, an azaspirodecanedione derivative (Figure 25–1), was synthesized in 1968 in the laboratories of Mead Johnson by Wu et al. (1969). Based on positive findings in conditioned-avoidance testing in rats, buspirone was originally studied clinically as a putative antipsychotic agent. It was projected to be largely devoid of the typical side effects of the antipsychotic class of drugs, but clinical trials failed to demonstrate usefulness in the treatment of schizophrenia (Sathananthan et al. 1975). Further study revealed that a single dose of buspirone had a marked taming effect in aggressive monkeys (Tompkins et al. 1980). In various behavioral models of anxiety in rodents, buspirone inhibited foot shock–induced fighting and prevented shock-induced suppression of drinking behavior, both screening tests predictive of anxiolytic effects (Riblet et al. 1982). At that time, minimal data were available on the molecular pharmacology of buspirone. However, Riblet et al. (1982) reported that buspirone displaced [3H]spiperone from dopamine D2 receptors in rat striatal membranes with an IC50 of 260 nM and demonstrated a right shift in binding activity in the presence of guanosine triphosphate (GTP), suggesting that it was a D2 agonist. Until the subsequent finding of high affinity binding to the newly discovered 5-HT1A receptor some 4 years later, the basis for the anxiolytic activity of buspirone was thought to be dopaminergic in origin.

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FIGURE 25–1. Chemical structure of buspirone.

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