Continuous administration (28 days) of gepirone, a potential anxiolytic, decreased rat cortical serotonin type 2 (5HT2) receptor density by 17 percent and reduced the frequency of head shakes induced by the serotonin agonist quipazine. These data support the results of previous studies confirming gepirone's involvement with brain serotonin systems, and suggest that in addition to its preclinical anxiolytic profile, gepirone exhibits pharmacological properties common to clinically effective antidepressants.