Journal
JOURNAL OF THE NEUROLOGICAL SCIENCES
Volume 229, Issue -, Pages 219-223Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.jns.2004.11.032
Keywords
vinpocetine; PK11195; peripheral benzodiazepine binding site (PBBS); monkey brain; glia; positron emission tomography (PET)
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Vinpocetine, a synthetic derivative of the Vinca minor alkaloid vincamine, is a widely used drug in neurological practice. We tested the hypothesis that vinpocetine binds to peripheral benzodiazepine binding sites (PBBS) and is therefore a potential ligand of PBBS. Positron emission tomography (PET) measurements in two cynomolgous monkeys showed that pretreatment with vinpocetine markedly reduced the brain uptake of [11C]PK11195, a known PBBS radioligand. On the other hand, whereas pretreatment with PK11195 increased the brain uptake of [(11)C]vinpocetine due to the blockade of PBBS in the periphery, it significantly reduced the binding potential (BP) values of [(11)C]vinpocetine in the whole brain and in individual brain structures to PK11195. These findings indicate that, whereas the two ligands have different affinities to PBBS, vinpocetine is a potent ligand of PBBS, which in turn suggests that the pharmacological activity of vinpocetine may involve the regulation of glial functions. (c) 2004 Elsevier B.V. All rights reserved.
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