1. Academic Validation
  2. Ziprasidone: a novel antipsychotic agent with a unique human receptor binding profile

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

  • Eur J Pharmacol. 2001 Aug 17;425(3):197-201. doi: 10.1016/s0014-2999(01)01188-8.
A W Schmidt 1 L A Lebel H R Howard Jr S H Zorn
Affiliations

Affiliation

  • 1 CNS Discovery, Groton Laboratories, Pfizer Global Research and Development, MS 8220-4155, 558 Eastern Point Road, Groton, CT 06340-1596, USA. [email protected]
Abstract

Ziprasidone is a novel antipsychotic agent with a unique combination of pharmacological activities at human receptors. Ziprasidone has high affinity for human 5-HT receptors and for human dopamine D(2) receptors. Ziprasidone is a 5-HT(1A) receptor agonist and an antagonist at 5-HT(2A), 5-HT(2C) and 5-HT(1B/1D) receptors. Additionally, ziprasidone inhibits neuronal uptake of 5-HT and norepinephrine comparable to the antidepressant imipramine. This unique pharmacological profile of ziprasidone may be related to its clinical effectiveness as a treatment for the positive, negative and affective symptoms of schizophrenia with a low propensity for extrapyramidal side effects, cognitive deficits and weight gain.

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