Sircar R, Zukin S R
Brain Res. 1985 Sep 30;344(1):142-5. doi: 10.1016/0006-8993(85)91198-9.
The anatomical localization of phencyclidine (PCP)/sigma-opiate receptors in rat brain was determined by quantitative light microscopy autoradiography using the new ligand N-(1-[2-thienyl]cyclohexyl) [3H]piperidine ([3H]TCP). TCP is a potent analog of PCP which possesses a higher affinity for PCP/sigma-opiate receptor than does PCP itself. The highest level of [3H]TCP binding was detected in the hippocampus. Intermediate levels were found in frontal cortex, striatum, amygdala and cerebellum. Specific [3H]TCP binding was undetectable in anterior commissure and corpus callosum. The distribution pattern of [3H]TCP binding sites is similar to the pattern obtained with [3H]PCP but more sharply defined. On the basis of its greater potency and specificity, [3H]TCP may prove superior to [3H]PCP as a molecular probe for the study of brain sigma opiate/phencyclidine receptors.
利用新型配体N-(1-[2-噻吩基]环己基)[3H]哌啶([3H]TCP)，通过定量光学显微镜放射自显影法确定了大鼠脑中苯环利定(PCP)/σ-阿片受体的解剖定位。TCP是PCP的一种强效类似物，它对PCP/σ-阿片受体的亲和力比PCP本身更高。在海马体中检测到最高水平的[3H]TCP结合。在额叶皮质、纹状体、杏仁核和小脑中发现中等水平。在前连合和胼胝体中未检测到特异性[3H]TCP结合。[3H]TCP结合位点的分布模式与[3H]PCP获得的模式相似，但更清晰明确。基于其更强的效力和特异性，[3H]TCP可能被证明是一种比[3H]PCP更优越的用于研究脑σ-阿片/苯环利定受体的分子探针。
