Sircar R, Zukin S R
Life Sci. 1983;33 Suppl 1:259-62. doi: 10.1016/0024-3205(83)90492-7.
Specific [3H]phencyclidine (PCP)-binding studies were carried out in homogenates prepared from different regions of post-mortem human brains derived from subjects free of any neurological disease. Scatchard analysis revealed a single class of [3H]PCP-binding sites. Binding was found to be stereospecific i.e. markedly greater ability of the potent PCP agonist dexoxadrol to displace specifically bound 10 nM [3H]PCP as compared to its behaviorally inactive enantiomer levoxadrol. Stereospecific binding was abolished by preincubation of homogenate with trypsin or by heating the homogenate to 90 degrees C for 15 min. Various sigma opiates displaced specifically bound [3H]PCP binding in a rank order similar to that seen in rat brain. Thus a baseline has been established to enable future elucidation of the possible role of these sites in psychiatric illnesses.
在取自无任何神经疾病受试者的死后人类大脑不同区域制备的匀浆中进行了特异性[3H]苯环己哌啶（PCP）结合研究。Scatchard分析显示存在一类[3H]PCP结合位点。发现结合具有立体特异性，即与行为上无活性的对映体左吗喃相比，强效PCP激动剂右吗喃特异性取代10 nM [3H]PCP特异性结合的能力明显更强。通过将匀浆与胰蛋白酶预孵育或通过将匀浆加热至90摄氏度15分钟，立体特异性结合被消除。各种σ阿片类药物以与在大鼠脑中观察到的相似的顺序特异性取代[3H]PCP结合。因此已经建立了一个基线，以便将来阐明这些位点在精神疾病中可能的作用。
