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Titolo:
ZIPRASIDONE (CP-88,059) - A NEW ANTIPSYCHOTIC WITH COMBINED DOPAMINE AND SEROTONIN RECEPTOR ANTAGONIST ACTIVITY
Autore:
SEEGER TF; SEYMOUR PA; SCHMIDT AW; ZORN SH; SCHULZ DW; LEBEL LA; MCLEAN S; GUANOWSKY V; HOWARD HR; LOWE JA; HEYM J;
Indirizzi:
PFIZER INC,DIV CENT RES,BOX 950,EASTERN POINT RD GROTON CT 06340
Titolo Testata:
The Journal of pharmacology and experimental therapeutics
fascicolo: 1, volume: 275, anno: 1995,
pagine: 101 - 113
SICI:
0022-3565(1995)275:1<101:Z(-ANA>2.0.ZU;2-G
Fonte:
ISI
Lingua:
ENG
Soggetto:
RAT CEREBRAL-CORTEX; ADENYLATE-CYCLASE ASSAY; PHARMACOLOGICAL CHARACTERIZATION; SCHIZOPHRENIC-PATIENTS; MUSCARINIC RECEPTORS; RITANSERIN R-55667; CHOROID-PLEXUS; BINDING-SITE; CLOZAPINE; BRAIN;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
63
Recensione:
Indirizzi per estratti:
Citazione:
T.F. Seeger et al., "ZIPRASIDONE (CP-88,059) - A NEW ANTIPSYCHOTIC WITH COMBINED DOPAMINE AND SEROTONIN RECEPTOR ANTAGONIST ACTIVITY", The Journal of pharmacology and experimental therapeutics, 275(1), 1995, pp. 101-113

Abstract

Ziprasidone (CP-88,059) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects in preclinical assayspredictive of antipsychotic activity. Whereas the compound is a dopamine antagonist in vitro and in vivo, its most potent action is antagonism of 5-HT2A receptors, where its affinity is an order of magnitude greater than that observed for dopamine D2 sites. Laboratory and clinical findings have led to a hypothesis that antagonism of 5-HT2A receptors in the brain limits the undesirable motor side effects associated with dopamine receptor blockade and improves efficacy against the negative symptoms of schizophrenia. Ziprasidone possesses an in vitro 5-HT2A/dopamine D2 receptor affinity ratio higher than any clinically available antipsychotic agent. In vivo, ziprasidone antagonizes 5-HT2A receptor-induced head twitch with 6-fold higher potency than for blockade of d-amphetamine-induced hyperactivity, a measure of central dopamine D2 receptor antagonism. Ziprasidone also has high affinity for the 5-HT1A, 5-HT1D and 5-HT2C receptor subtypes, which may further enhance its therapeutic potential. The prediction of antipsychotic efficacy without severe motor side effects is supported by the relatively weak potency of ziprasidone to produce catalepsy in animals, contrasted with its potent antagonism of conditioned avoidance responding and dopamine agonist-induced locomotor activation and stereotypy. The compound is well tolerated in animals at doses producing effective dopamine antagonism in the brain. Ziprasidone should be a valuable addition to the treatment of psychotic disorders.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/09/20 alle ore 12:37:40