Ziprasidone (marketed as Geodon Zeldox by Pfizer and Zipwell by Actavis) was the fifth atypical antipsychotic to gain approval (February 2001) in the United States. It is approved by the U.S. Food and Drug Administration (FDA) for the treatment of schizophrenia and acute mania and mixed states associated with bipolar disorder. Its intramuscular injection form is approved for acute agitation in schizophrenic patients for whom treatment with just ziprasidone is appropriate. Ziprasidone is also used off-label for depression bipolar maintenance and PTSD.

For R&D use onlynot for drug household or other uses.

Ziprasidone(CP88059) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.IC50 valueTarget 5-HT receptor Dopamine receptorZiprasidone possesses an in vitro 5-HT2Adopamine D2 receptor affinity ratio higher than any clinically available antipsychotic agent. In vivo ziprasidone antagonizes 5-HT2A receptor-induced head twitch with 6-fold higher potency than for blockade of d-amphetamine-induced hyperactivity a measure of central dopamine D2 receptor antagonism.