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大鼠脑中[3H]3-羟基-PCP(1-(1-(3-羟基苯基)环己基)哌啶)结合位点的定量放射自显影定位

Quantitative autoradiographic localization of [3H]3-OH-PCP (1-(1(3-hydroxyphenyl)cyclohexyl)piperidine) binding sites in rat brain.

作者信息

Suzuki T, Yamamoto T, Hori T, Abe S, Moroji T, Shiraishi H, Ito T, Ho I K

机构信息

Department of Psychiatry, University of Tsukuba, Ibaraki, Japan.

出版信息

Brain Res Bull. 1995;37(4):431-5. doi: 10.1016/0361-9230(95)00005-4.

DOI:10.1016/0361-9230(95)00005-4
PMID:7620917
Abstract

Binding of a novel radioligand, [3H]3-OH-PCP (1(1(3-hydroxyphenyl) cyclohexyl)piperidine), to N-methyl-D-aspartate (NMDA) receptor-coupled and -uncoupled PCP sites was investigated in the rat brain. The highest densities of [3H]3-OH-PCP binding were observed in the hippocampal formation, notably in the stratum radiatum and oriens of CA1 region, and dentate gyrus. There were relatively high levels of binding in the olfactory system, superficial layer of cortices, the amygdala and the thalamus. In contrast, lower levels of binding were found in the globus pallidus, cerebellum, and brain stem, except for the superior colliculus. These findings demonstrate that [3H]3-OH-PCP binds to discrete regions within the rat brain. Its distribution is consistent with autoradiographic localization of [3H]TCP and [3H]MK-801 binding sites in the rat brain, suggesting that [3H]3-OH-PCP binds to NMDA/PCP ion-channel complexes in preference to sigma sites.

摘要

在大鼠脑中研究了一种新型放射性配体[3H]3 - OH - PCP(1(1(3 - 羟基苯基)环己基)哌啶)与N - 甲基 - D - 天冬氨酸(NMDA)受体偶联和未偶联的PCP位点的结合情况。在海马结构中观察到[3H]3 - OH - PCP结合的最高密度,特别是在CA1区的辐射层和海马下托,以及齿状回。在嗅觉系统、皮质表层、杏仁核和丘脑中存在相对较高水平的结合。相比之下,苍白球、小脑和脑干(除上丘外)的结合水平较低。这些发现表明[3H]3 - OH - PCP与大鼠脑内的离散区域结合。其分布与大鼠脑中[3H]TCP和[3H]MK - 801结合位点的放射自显影定位一致,表明[3H]3 - OH - PCP优先与NMDA/PCP离子通道复合物结合而非σ位点。

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