Evaluation of the binding characteristics of [18F]fluoroproxyfan in the rat brain for in vivo visualization of histamine H3 receptor
Evaluation of the binding characteristics of [18F]fluoroproxyfan in the rat brain for in vivo visualization of histamine H3 receptor
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DOI：
10.1016/j.nucmedbio.2007.07.012
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发表时间：
2007-11-01
影响因子：
3.1
通讯作者：
Yanai, Kazuhiko
中科院分区：
文献类型：
--
作者：
Funaki, Yoshihito;Sato, Kimihiko;Yanai, Kazuhiko
组胺 H-3 受体在生物学功能中发挥着重要作用。本研究的目的是检查组胺 H3 受体是否可以在体内和体外用 [F-18]3-(1H-咪唑-4-基)丙基 4-氟苄基醚 (fluproxyfan) 可视化。使用[18F]苄基溴合成了具有高比活性的[F-18]氟丙醚。 [18F]氟丙醚与大鼠脑匀浆的结合在纹状体和丘脑中较高，在小脑中最低。体外放射自显影研究成功证明了[F-18]氟代凡与大鼠脑中H3受体的特异性结合。根据体外结合，[18F]氟代凡在大鼠脑中的体内分布是不均匀的。在阻断实验中，在存在大量氟丙苯的情况下，不均匀分布消失。这些数据表明，[18F]氟丙醚可能有助于通过正电子发射断层扫描对人脑中的组胺 H3 受体进行无创成像。 (c) 2007 Elsevier Inc. 保留所有权利。
Histamine H-3 receptors play an important role in biological functions. The aim of this research was to examine whether histamine H3 receptors can be visualized in vivo and in vitro with [F-18]3-(1H-imidazol-4-yl)propyI 4-fluorobenzyl ether (fluoroproxyfan). [F-18] Fluoroproxyfan was synthesized with high specific activity using [18F]benzyl bromide. The binding of [18F]fluoroproxyfan to rat brain homogenates was higher in the striatum and thalamus and was lowest in the cerebellum. The in vitro autoradiographic study successfully demonstrated the specific binding of [F-18]fluoroproxyfan to the H3 receptor in the rat brain. In accordance with the in vitro bindings, the in vivo distribution of [18F]fluoroproxyfan was heterogeneous in the rat brain. In the blocking experiments, the heterogeneous distribution disappeared in the presence of large amounts of fluoroproxyfan. These data suggest that [18F]fluoroproxyfan can be potentially useful to image histamine H3 receptor noninvasively in the human brain by positron emission tomography. (c) 2007 Elsevier Inc. All rights reserved.