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Titolo:
A PET STUDY OF 5-HT2 AND D-2 DOPAMINE-RECEPTOR OCCUPANCY INDUCED BY OLANZAPINE IN HEALTHY-SUBJECTS
Autore:
NYBERG S; FARDE L; HALLDIN C;
Indirizzi:
KAROLINSKA HOSP,DEPT CLIN NEUROSCI,PSYCHIAT SECT S-17176 STOCKHOLM SWEDEN
Titolo Testata:
Neuropsychopharmacology
fascicolo: 1, volume: 16, anno: 1997,
pagine: 1 - 7
SICI:
0893-133X(1997)16:1<1:APSO5A>2.0.ZU;2-J
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; NAIVE SCHIZOPHRENIC-PATIENTS; ANTIPSYCHOTIC-DRUGS; HUMAN-BRAIN; C-11; CLOZAPINE; BINDING; MEPHENYTOIN; RISPERIDONE; RACLOPRIDE;
Keywords:
POSITRON EMISSION TOMOGRAPHY; HUMAN; D-2 DOPAMINE RECEPTORS; 5-HT2 RECEPTORS; OLANZAPINE; ANTIPSYCHOTIC DRUGS; ATYPICAL;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
37
Recensione:
Indirizzi per estratti:
Citazione:
S. Nyberg et al., "A PET STUDY OF 5-HT2 AND D-2 DOPAMINE-RECEPTOR OCCUPANCY INDUCED BY OLANZAPINE IN HEALTHY-SUBJECTS", Neuropsychopharmacology, 16(1), 1997, pp. 1-7

Abstract

Olanzapine is a new antipsychotic drug with affinity for 5-HT2, D-2, D-1, and muscarinic receptors. Positron emission tomography and the radioligands [C-11]raclopride and [C-11]raclopride and [C-11]NSMP were used to measure D-2 and 5-HT2 receptor occupancy in three healthy subjects after 10 mg olanzapine orally. After seven hours D-2 receptor occupancy was 63%, 62% and 59%, respectively. After 9.5 hours 5-HT2 receptor occupancy was 74%, 86% and 92%. D-2 and 5-HT2 receptor occupancy was comparable to that found in patients continuously treated with clozapine. Clinical efficacy has been demonstrated for olanzapine in the dose range 5 to 15 mg per day. Extrapolation from our present observations after a 10 mg single-dose suggest, that at the lower end of the clinically examined dose range the D-2 and 5-HT2 receptor occupancy should be similar to that induced by standard doses of clozapine. Detailed evaluation of the dose-response characteristics of olanzapine and direct clinical comparison to clozapine will thus provide valuable leads to the clarification of atypical antipsychotic action. (C) 1997 American College of Neuropsychopharmacology.

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Documento generato il 21/01/20 alle ore 01:04:25