Ziprasidone: a novel antipsychotic agent with a unique human receptor binding profile

Ziprasidone is a novel antipsychotic agent with a unique combination of pha rmacological activities at human receptors. Ziprasidone has high affinity f or human 5-HT receptors and for human dopamine D-2 receptors. Ziprasidone i s a 5-HT1A receptor agonist and an antagonist at 5-HT2A, 5-HT2C and 5-HT1B/ 1D receptors. Additionally, ziprasidone inhibits neuronal uptake of 5-HT an d norepinephrine comparable to the antidepressant imipramine. This unique p harmacological profile of ziprasidone may be related to its clinical effect iveness as a treatment for the positive, negative and affective symptoms of schizophrenia with a low propensity for extrapyramidal side effects, cogni tive deficits and weight gain. (C) 2001 Published by Elsevier Science B.V.