Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
9880417 | Journal of the Neurological Sciences | 2005 | 5 Pages |
Abstract
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 [11C]vinpocetine due to the blockade of PBBS in the periphery, it significantly reduced the binding potential (BP) values of [11C]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.
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Authors
Balázs Gulyás, Christer Halldin, Ádám Vas, Richard B. Banati, Evgeny Shchukin, Sjoerd Finnema, Jari Tarkainen, Károly Tihanyi, Géza Szilágyi, Lars Farde,