In vivo binding of [3H]d-N-allylnormetazocine and [3H]haloperidol to sigma receptors in the mouse brain.
In vivo binding of [3H]d-N-allylnormetazocine and [3H]haloperidol to sigma receptors in the mouse brain.
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[3H]d-N-烯丙去甲佐辛和[3H]氟哌啶醇与小鼠大脑中的σ受体的体内结合。
DOI：
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发表时间：
1990
影响因子：
2.8
通讯作者：
E. London
中科院分区：
文献类型：
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作者：
A. Weissman;E. Broussolle;E. London
使用 [3H]d-N-烯丙去甲佐辛 ([3H]d-NANM) 和 [3H]氟哌啶醇 ([3H]HAL) 作为配体，已在体外证明并表征了与 σ 位点的特异性结合。作为这些实验的延伸，我们检查了小鼠大脑中 [3H]d-NANM 和 [3H]HAL 的局部体内特异性结合。两种配体均观察到特异性体内 σ 结合；使用[3H]d-NANM和[3H]HAL，跨大脑区域特异性结合的平均估计值分别占大脑总放射性的54%和56%。两种配体在小脑、延髓脑桥和中脑中均显示出高水平的特异性结合，而在海马体中的特异性结合水平最低。估计[3H]d-NANM 与七个脑区苯环己哌啶 (PCP) 受体的平均结合仅占脑总放射性的 13%，并且显示出比 sigma 结合更均匀的区域分布。虽然[3H]d-NANM和[3H]HAL与σ位点的体内特异性结合的分布与体外获得的结果相当，但目前对体内[3H]d-NANM与PCP位点结合的估计与体外发现的PCP受体的分布并不相似。结果表明，放射性标记的 d-NANM 和 HAL 可用于体内 σ 结合位点成像。
Specific binding to sigma sites has been demonstrated and characterized in vitro using [3H]d-N-allylnormetazocine ([3H]d-NANM) and [3H]haloperidol ([3H]HAL) as ligands. As an extension of these experiments, we examined the regional in vivo specific binding of [3H]d-NANM and [3H]HAL in the mouse brain. Specific in vivo sigma binding was seen with both ligands; average estimates of specific binding across brain regions were 54 per cent and 56 per cent of total brain radioactivity, using [3H]d-NANM and [3H]HAL, respectively. Both ligands showed high levels of specific binding in the cerebellum, medulla-pons and midbrain, and lowest levels in the hippocampus. Estimated average [3H]d-NANM binding to phencyclidine (PCP) receptors across seven brain regions was only 13 per cent of total brain radioactivity, and showed a more uniform regional distribution than sigma binding. While the distributions of in vivo specific binding of [3H]d-NANM and [3H]HAL to sigma sites were comparable to findings obtained in vitro, the present estimates of in vivo [3H]d-NANM binding to PCP sites did not resemble the distribution of PCP receptors found in vitro. The results suggest that radiolabelled d-NANM and HAL may be useful for imaging sigma binding sites in vivo.