Gulyás Balázs, Halldin Christer, Vas Adám, Banati Richard B, Shchukin Evgeny, Finnema Sjoerd, Tarkainen Jari, Tihanyi Károly, Szilágyi Géza, Farde Lars
Karolinska Institute, Psychiatry Section, Department of Clinical Neuroscience, Karolinska Hospital, S-17176 Stockholm, Sweden.
J Neurol Sci. 2005 Mar 15;229-230:219-23. doi: 10.1016/j.jns.2004.11.032. Epub 2004 Dec 16.
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.
长春西汀是一种合成的长春花属小蔓长春花生物碱长春胺衍生物，是神经学实践中广泛使用的药物。我们验证了这样一个假设：长春西汀与外周苯二氮䓬结合位点（PBBS）结合，因此是PBBS的潜在配体。对两只食蟹猴进行的正电子发射断层扫描（PET）测量表明，用长春西汀预处理可显著降低已知的PBBS放射性配体[11C]PK11195的脑摄取量。另一方面，尽管用PK11195预处理由于外周PBBS的阻断而增加了[11C]长春西汀的脑摄取量，但它显著降低了[11C]长春西汀在全脑和各个脑结构中与PK11195的结合潜能（BP）值。这些发现表明，尽管这两种配体对PBBS的亲和力不同，但长春西汀是PBBS的有效配体，这反过来表明长春西汀的药理活性可能涉及神经胶质功能的调节。
