High correlation between the localization of [3H]TCP binding and NMDA receptors.
High correlation between the localization of [3H]TCP binding and NMDA receptors.
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[3H]TCP 结合定位与 NMDA 受体之间高度相关。
DOI：
10.1016/0014-2999(86)90703-x
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发表时间：
1986
影响因子：
5
通讯作者：
Young,AB
中科院分区：
文献类型：
--
作者：
Maragos,WF;Chu,DC;Greenamyre,JT;Penney,JB;Young,AB
氚化 N-(1-[2-噻吩基环己基)-3, 4-哌啶 ([3H] TCP) 是解离麻醉剂苯环己哌啶 (PCP) 的衍生物，最近已被证明可以与大鼠中枢神经系统内的阿片受体特异性结合（Sircar 和 Zukin，1985）。此类药物非竞争性抑制脊髓中 N-甲基-D-天冬氨酸 (NMDA)（一种谷氨酸类似物）的兴奋性（Martin 和 Lodge，1985），并抑制海马体的长时程增强（Stringer 等，1983）。这两种作用被认为是由 NMDA 敏感的谷氨酸受体介导的。 NMDA 受体与由 Mg 2÷ 门控的电压敏感阳离子通道偶联。正是于此。据信五氯苯酚和相关化合物发挥作用的通道位点。为了进一步描绘解离麻醉剂和 NMDA 受体之间的关系，我们使用定量放射自显影技术比较了大鼠中枢神经系统内 o 特异性化合物 [3H] TCP 和 NMDA 敏感的 [3H] 谷氨酸结合位点的区域结合分布。在大鼠前脑不同水平处采集的交替 20/μm 厚的载玻片切片上对每种受体类别进行放射标记。对于 [3H] TCP 结合，切片在冷 50 mM Tris-乙酸盐（pH 7.4）中预孵育 30 分钟，然后干燥。然后将切片在含有 1 mM 醋酸镁和 20 nM [3H] TCP（52.9 Ci/mmol，New England Nuclear Corp.）的相同缓冲液中在存在或不存在的情况下孵育 45 分钟。
Tritiated N-(1-[2-thienylcyclohexyl)-3, 4-piperidine ([3H] TCP), a derivative of the dissociative anesthetic phencyclidine (PCP), has recently been shown to bind specifically to a o-opiate receptor within the central nervous system of the rat (Sircar and Zukin, 1985). Drugs of this class noncompetitively inhibit the excitatory properties of N-methyl-D-aspartate (NMDA), a glutamate analogue, in the spinal cord (Martin and Lodge, 1985), and inhibit long-term potentiation in the hippocampus (Stringer et al., 1983). Both of these effects are thought to be mediated by NMDA-sensitive glutamate receptors. The NMDA receptor is coupled to a voltage-sensitive cation channel that is gated by Mg 2÷. It is at this. channel site that PCP and related compounds are believed to act. In order to further delineate the relationship between the dissociative anesthetics and NMDA receptors, we have compared the regional binding distribution of the o-specific compound [3H] TCP and NMDA-sensitive [3H] glutamate binding sites within the rat CNS using quantitative autoradiography.Radiolabelling of each receptor class was carried out on alternate 20/~ m thick slide mounted sections taken at various levels of rat forebrain. For [3H] TCP binding, sections were preincubated for 30 min in cold 50 mM Tris-acetate, pH 7.4 and then dried. Sections were then incubated for 45 min in the same buffer with 1 mM magnesium acetate and 20 nM [3H] TCP (52.9 Ci/mmol, New England Nuclear Corp.) in the presence or ab-
在体外，苯环己哌啶和环佐辛可阻断长时程增强作用。
影响因子：
5
作者：
J. L. Stringer;J. T. Hackett;P. G. Guyenet
通讯作者：
P. G. Guyenet