| Autor: |
Raedler TJ; Clinical Brain Disorders Branch, DIRP, NIMH, 20892, Bethesda, MD 20892-1379, USA., Knable MB, Jones DW, Lafargue T, Urbina RA, Egan MF, Pickar D, Weinberger DR |
| Jazyk: |
angličtina |
| Zdroj: |
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology [Neuropsychopharmacology] 2000 Jul; Vol. 23 (1), pp. 56-68. |
| DOI: |
10.1016/S0893-133X(99)00162-1 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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