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Titolo:
Brain uptake and plasma metabolism of [C-11]vinpocetine: A preliminary PETstudy in a cynomolgus monkey
Autore:
Gulyas, B; Halldin, C; Karlsson, P; Chou, YH; Swahn, CG; Bonock, P; Paroczai, M; Farde, L;
Indirizzi:
Karolinska Inst, Dept Neurol, Div Brain Res, S-17177 Stockholm, Sweden Karolinska Inst Stockholm Sweden S-17177 Res, S-17177 Stockholm, Sweden Karolinska Inst, Dept Clin Neurosci, Psychiat Sect, S-17177 Stockholm, Sweden Karolinska Inst Stockholm Sweden S-17177 Sect, S-17177 Stockholm, Sweden Richter Gedeon Chem Works, Budapest, Hungary Richter Gedeon Chem Works Budapest Hungary hem Works, Budapest, Hungary
Titolo Testata:
JOURNAL OF NEUROIMAGING
fascicolo: 4, volume: 9, anno: 1999,
pagine: 217 - 222
SICI:
1051-2284(199910)9:4<217:BUAPMO>2.0.ZU;2-Y
Fonte:
ISI
Lingua:
ENG
Soggetto:
GATED NA+ CHANNELS; VINPOCETINE; RECEPTOR; POTENT; RAT; ISCHEMIA; BINDING; RELEASE;
Keywords:
positron emission tomography; brain; vinpocetine; metabolism;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Citazioni:
32
Recensione:
Indirizzi per estratti:
Indirizzo: Gulyas, B Karolinska Inst, Dept Neurol, Div Brain Res, S-17177 Stockholm, Sweden Karolinska Inst Stockholm Sweden S-17177 177 Stockholm, Sweden
Citazione:
B. Gulyas et al., "Brain uptake and plasma metabolism of [C-11]vinpocetine: A preliminary PETstudy in a cynomolgus monkey", J NEUROIMAG, 9(4), 1999, pp. 217-222

Abstract

Vinpocetine, a vinca alkaloid, is a widely used therapeutic agent in patients with acute and chronic stroke. To reveal the mechanisms of vinpocetine action in the brain, vinpocetine was labeled with C-11. Positron emission tomography (PET) was used to determine the uptake and distribution of [C-11]vinpocetine in brain regions and the trunk of a cynomolgous monkey in two independent measurements. The concentration of vinpocetine and its labeled metabolites was determined in blood and plasma using high-performance liquidchromatography (HPLC). Almost identical measurements were obtained in the two independent studies. After intravenous administration, following an initial peak, the total concentration of radioactivity in blood was relativelystable with time, whereas the concentration of the unchanged compound decreased with time in an exponential manner. The uptake of [C-11]vinpocetine in brain was rapid, and 5% of the radioactivity totally injected was presentin the brain 2 minutes after drug administration, indicating that the compound entered the brain readily. The radioactivity uptake was heterogeneously distributed among brain regions and was highest in the thalamus, the basal ganglia, and certain neocortical regions. The high brain uptake and the heterogeneous regional distribution indicate that direct central nervous system (CNS) effects of vinpocetine must be considered as explanation for the therapeutic effects. The detailed exploration of this suggestion requires further studies.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 07:14:33