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