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大鼠脑中[125I]R(+)反式-7-羟基-PIPAT结合位点的表征

Characterization of binding sites for [125I]R(+)trans-7-OH-PIPAT in rat brain.

作者信息

Kung M P, Chumpradit S, Frederick D, Garner S, Burris K D, Molinoff P B, Kung H F

机构信息

Department of Radiology, University of Pennsylvania, School of Medicine, Philadelphia 19104.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1994 Dec;350(6):611-7. doi: 10.1007/BF00169365.

DOI:10.1007/BF00169365
PMID:7708118
Abstract

Binding characteristics of a novel radioiodinated ligand, [125I]R(+)trans-7-hydroxy-2-(N-n-propyl-N-3'-iodo-2'-propenyl) aminotetralin ([125I]R(+)trans-7-OH-PIPAT), were evaluated using homogenate binding and autoradiographic techniques in rat brain. [125I]R(+)trans-7-OH-PIPAT bound to sites (dopamine receptors) in homogenates of rat basal forebrain (including caudate putamen, nucleus accumbens and olfactory tubercle) with a high affinity (Kd = 0.42 nM). A majority (70%) of the sites labeled by [125I]R(+)trans-7-OH-PIPAT in basal forebrain were GTP-sensitive. In rat hippocampal homogenates, specific and saturable binding of [125I]R(+)trans-7-OH-PIPAT to 5-HT1A receptors, with a Kd value of 1.4 nM and a Bmax value of 210 fmol/mg protein, was observed. Binding of [125I]R(+)trans-7-OH-PIPAT to sigma sites was also demonstrated in rat cerebellar homogenates. In the presence of GTP (to inhibit binding to D2 and 5-HT1A receptors) and DTG (to inhibit binding to sigma sites), dopamine D3 receptors could be selectively labeled with [125I]R(+)trans-7-OH-PIPAT. [125I]R(+)trans-7-OH-PIPAT offers several unique advantages, including high specific activity and high affinity binding, which make it an excellent probe for the investigation and characterization of the distribution of dopamine D3 receptors.

摘要

使用大鼠脑匀浆结合和放射自显影技术评估了一种新型放射性碘化配体[125I]R(+)反式-7-羟基-2-(N-正丙基-N-3'-碘-2'-丙烯基)氨基四氢萘([125I]R(+)反式-7-OH-PIPAT)的结合特性。[125I]R(+)反式-7-OH-PIPAT以高亲和力（Kd = 0.42 nM）与大鼠基底前脑（包括尾状壳核、伏隔核和嗅结节）匀浆中的位点（多巴胺受体）结合。基底前脑中被[125I]R(+)反式-7-OH-PIPAT标记的位点大部分（70%）对GTP敏感。在大鼠海马匀浆中，观察到[125I]R(+)反式-7-OH-PIPAT与5-HT1A受体有特异性和可饱和性结合，Kd值为1.4 nM，Bmax值为210 fmol/mg蛋白。在大鼠小脑匀浆中也证明了[125I]R(+)反式-7-OH-PIPAT与σ位点的结合。在存在GTP（抑制与D2和5-HT1A受体的结合）和DTG（抑制与σ位点的结合）的情况下，多巴胺D3受体可用[125I]R(+)反式-7-OH-PIPAT选择性标记。[125I]R(+)反式-7-OH-PIPAT具有几个独特的优点，包括高比活性和高亲和力结合，这使其成为研究和表征多巴胺D3受体分布的极佳探针。

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