Ziprasidone: a novel antipsychotic agent with a unique human receptor binding profile.
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.
Schmidt
A W
AW
CNS Discovery, Groton Laboratories, Pfizer Global Research and Development, MS 8220-4155, 558 Eastern Point Road, Groton, CT 06340-1596, USA. anne_w_schmidt@groton.pfizer.com
Lebel
L A
LA
Howard
H R
HR
Zorn
S H
SH
D000818:Animals; D014150:Antipsychotic Agents / Q000378:metabolism / Q000494:pharmacology*; D001569:Benzodiazepines; D001665:Binding Sites; D001667:Binding, Competitive / Q000187:drug effects; D002460:Cell Line; D003024:Clozapine / Q000378:metabolism / Q000494:pharmacology; D003987:Dibenzothiazepines / Q000378:metabolism / Q000494:pharmacology; D018492:Dopamine Antagonists / Q000378:metabolism / Q000494:pharmacology; D006220:Haloperidol / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D009474:Neurons / Q000166:cytology / Q000378:metabolism; D009638:Norepinephrine / Q000493:pharmacokinetics; D000077152:Olanzapine; D010879:Piperazines / Q000378:metabolism / Q000494:pharmacology*; D010890:Pirenzepine / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology; D000069348:Quetiapine Fumarate; D051381:Rats; D011942:Receptors, Adrenergic, alpha / Q000378:metabolism; D011954:Receptors, Dopamine / Q000378:metabolism; D011985:Receptors, Serotonin / Q000378:metabolism; D044263:Receptors, Serotonin, 5-HT1; D018967:Risperidone / Q000378:metabolism / Q000494:pharmacology; D012701:Serotonin / Q000493:pharmacokinetics; D012702:Serotonin Antagonists / Q000494:pharmacology; D013844:Thiazoles / Q000378:metabolism / Q000494:pharmacology*
D014150:Antipsychotic Agents; D003987:Dibenzothiazepines; D018492:Dopamine Antagonists; D010879:Piperazines; D011942:Receptors, Adrenergic, alpha; D011954:Receptors, Dopamine; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D012702:Serotonin Antagonists; D013844:Thiazoles; D001569:Benzodiazepines; D000069348:Quetiapine Fumarate; D012701:Serotonin; D010890:Pirenzepine; C092292:ziprasidone; D003024:Clozapine; D006220:Haloperidol; D018967:Risperidone; D000077152:Olanzapine; D009638:Norepinephrine