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.

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.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Antipsychotic Agents / metabolism
  • Antipsychotic Agents / pharmacology*
  • Benzodiazepines
  • Binding Sites
  • Binding, Competitive / drug effects
  • Cell Line
  • Clozapine / metabolism
  • Clozapine / pharmacology
  • Dibenzothiazepines / metabolism
  • Dibenzothiazepines / pharmacology
  • Dopamine Antagonists / metabolism
  • Dopamine Antagonists / pharmacology
  • Haloperidol / metabolism
  • Haloperidol / pharmacology
  • Humans
  • Neurons / cytology
  • Neurons / metabolism
  • Norepinephrine / pharmacokinetics
  • Olanzapine
  • Piperazines / metabolism
  • Piperazines / pharmacology*
  • Pirenzepine / analogs & derivatives
  • Pirenzepine / metabolism
  • Pirenzepine / pharmacology
  • Quetiapine Fumarate
  • Rats
  • Receptors, Adrenergic, alpha / metabolism
  • Receptors, Dopamine / metabolism
  • Receptors, Serotonin / metabolism
  • Receptors, Serotonin, 5-HT1
  • Risperidone / metabolism
  • Risperidone / pharmacology
  • Serotonin / pharmacokinetics
  • Serotonin Antagonists / pharmacology
  • Thiazoles / metabolism
  • Thiazoles / pharmacology*

Substances

  • Antipsychotic Agents
  • Dibenzothiazepines
  • Dopamine Antagonists
  • Piperazines
  • Receptors, Adrenergic, alpha
  • Receptors, Dopamine
  • Receptors, Serotonin
  • Receptors, Serotonin, 5-HT1
  • Serotonin Antagonists
  • Thiazoles
  • Benzodiazepines
  • Quetiapine Fumarate
  • Serotonin
  • Pirenzepine
  • ziprasidone
  • Clozapine
  • Haloperidol
  • Risperidone
  • Olanzapine
  • Norepinephrine