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Titolo:
In vivo olanzapine occupancy of muscarinic acetylcholine receptors in patients with schizophrenia
Autore:
Raedler, TJ; Knable, MB; Jones, DW; Lafargue, T; Urbina, RA; Egan, MF; Pickar, D; Weinberger, DR;
Indirizzi:
NIMH, Clin Brain Disorders Branch, NIH, DIRP, Bethesda, MD 20892 USA NIMHBethesda MD USA 20892 ders Branch, NIH, DIRP, Bethesda, MD 20892 USA Stanley Res Fdn, Bethesda, MD 20814 USA Stanley Res Fdn Bethesda MD USA 20814 ley Res Fdn, Bethesda, MD 20814 USA NIMH, Expt Therapeut Branch, DIRP, Bethesda, MD 20892 USA NIMH Bethesda MD USA 20892 Therapeut Branch, DIRP, Bethesda, MD 20892 USA
Titolo Testata:
NEUROPSYCHOPHARMACOLOGY
fascicolo: 1, volume: 23, anno: 2000,
pagine: 56 - 68
SICI:
0893-133X(200007)23:1<56:IVOOOM>2.0.ZU;2-C
Fonte:
ISI
Lingua:
ENG
Soggetto:
IN-VIVO; CHOLINERGIC RECEPTORS; DOUBLE-BLIND; RAT-BRAIN; CAUDATE-PUTAMEN; DOPAMINE; HALOPERIDOL; ANTAGONISM; BINDING; D-2;
Keywords:
muscarinic receptor; olanzapine; IQNB; SPECT; schizophrenia; antipsychotic;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
59
Recensione:
Indirizzi per estratti:
Indirizzo: Weinberger, DR NIMH, Clin Brain Disorders Branch, NIH, DIRP, 10 Ctr Dr,4S-235 MSC 1379, Bethesda, MD 20892 USA NIMH 10 Ctr Dr,4S-235 MSC 1379 Bethesda MD USA 20892 92 USA
Citazione:
T.J. Raedler et al., "In vivo olanzapine occupancy of muscarinic acetylcholine receptors in patients with schizophrenia", NEUROPSYCH, 23(1), 2000, pp. 56-68

Abstract

Olanzapine is an atypical antipsychotic with potent antimuscarinic properties in vitro (K-i = 2-25 nM). We studied in vivo muscarinic receptor occupancy by olanzapine at both low dose (5 mg/dy) and high dose (20 mg/dy) in several regions of cortex, striatum, thalamus and pons by analyzing [I-123]IQNB SPECT images of seven schizophrenia patients. Both low-dose and high-dose olanzapine studies revealed significantly lower [I-123]IQNB binding than that of drug-free schizophrenia patients (N = 12) in all regions except striatum. [I-123]IQNB binding was significantly lower at high-dose than low-dose in the same regions. Muscarinic occupancy by olanzapine ranged from 13% to 57% at 5 mg/dy and 26% to 79% at 20 mg/dy with an anatomical pattern indicating M-2 subtype selectivity. The [I-123]IQNB data indicate that olanzapine is a potent and subtype-selective muscarinic antagonist in vivo, perhaps explaining its low extrapyramidal side effect profile and low incidence of anticholinergic side effects. [Neuropsychopharmacology 23:56-68, 2000] Published by Elsevier Science Inc. on behalf of the American College of Neuropsychopharmacology.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/09/20 alle ore 09:30:55