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[健康男性静脉注射[¹¹C]-长春西汀后脑摄取及区域分布:一项正电子发射断层扫描研究]

[Cerebral uptake and regional distribution of [11C]-vinpocetin after intravenous administration to healthy men: a PET study].

作者信息

Vas Adám, Sóvágó Judit, Halldin Christer, Sandell Johan, Karlsson Per, Kárpáti Egon, Kiss Béla, Cselényi Zsolt, Farde Lars, Gulyás Balázs

机构信息

Richter Gedeon Vegyészeti Gyár Rt., Budapest.

出版信息

Orv Hetil. 2002 Nov 24;143(47):2631-6.

Abstract

INTRODUCTION

Vinpocetine is a compound widely used in the prevention and treatment of cerebrovascular diseases. The exact mechanism of action of the drug is still not known. The objective of the present investigation was to determine the global uptake and regional distribution of radiolabelled vinpocetine in the human brain. Three healthy persons were examined with positron emission tomography (PET) and [11C]-vinpocetine.

RESULTS

The uptake of [11C]-vinpocetine in brain was rapid and on average as a maximum 3.7% of the total radioactivity injected was in the brain 2 minutes after radioligand administration. The uptake was heterogeneously distributed among brain regions. When compared with the cerebellum, an a priori reference region, the highest regional uptake was in the thalamus, the upper brain stem, the striatum and the cortex.

CONCLUSIONS

The brain regions showing increased uptake in the human brain correspond to those in which vinpocetine has previously been shown to induce elevated metabolism and blood flow by PET clinical studies in patients with chronic ischaemic post-stroke condition.

摘要

引言

长春西汀是一种广泛用于预防和治疗脑血管疾病的化合物。该药物的确切作用机制尚不清楚。本研究的目的是确定放射性标记的长春西汀在人脑中的整体摄取和区域分布。对三名健康受试者进行了正电子发射断层扫描(PET)和[11C] - 长春西汀检查。

结果

[11C] - 长春西汀在脑中的摄取迅速,给药后2分钟时,脑内摄取的放射性平均最高可达注入总放射性的3.7%。摄取在脑区中分布不均。与小脑(一个先验的参考区域)相比,区域摄取最高的是丘脑、脑桥上部、纹状体和皮质。

结论

在人脑中摄取增加的脑区与先前PET临床研究中显示长春西汀可使慢性缺血性中风后患者代谢和血流升高的脑区一致。

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PET studies on the brain uptake and regional distribution of [11C]vinpocetine in human subjects.
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Drug distribution in man: a positron emission tomography study after oral administration of the labelled neuroprotective drug vinpocetine.
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