Quirion R, Hammer R P, Herkenham M, Pert C B
Proc Natl Acad Sci U S A. 1981 Sep;78(9):5881-5. doi: 10.1073/pnas.78.9.5881.
[3H]Phencyclidine ([3H]PCP) binds specifically to an apparently single class of binding sites on slide-mounted sections of rat olfactory bulb (Kd = 46 nM; Bmax = 10.5 fmol per slice). Bound [3H]PCP can be displaced by nonradioactive PCP and a series of its analogs with relative potencies that correlate closely (P less than 0.001) with values determined in a rat discrimination test that utilized PCP as a cue. Although morphine, naloxone, and opiate peptides do not displace bound [3H]PCP, psychotomimetic benzomorphans, classed as "sigma opiates," are quite potent displacers in vitro and have PCP-like behavioral properties in vivo. These results suggest that phencyclidine and the sigma opiates act at the same sites. [3H]PCP binding sites were visualized by using tritium-sensitive LKB film analyzed by computerized densitometry and color coding. The [3H]PCP binds most densely to cortical areas, diffusely in neocortex, and somewhat heterogeneously in the laminae of the hippocampal formation and dentate gyrus. Most of the brainstem and spinal cord show low specific [3H]PCP binding, with gray matter generally showing more binding than white.
[3H]苯环己哌啶（[3H]PCP）特异性结合于大鼠嗅球载玻片标本上一类明显单一的结合位点（解离常数Kd = 46 nM；最大结合量Bmax = 每片10.5 fmol）。结合的[3H]PCP可被非放射性PCP及其一系列类似物取代，其相对效力与在以PCP为线索的大鼠辨别试验中测定的值密切相关（P < 0.001）。虽然吗啡、纳洛酮和阿片肽不能取代结合的[3H]PCP，但被归类为“σ阿片类药物”的拟精神病苯吗喃类在体外是相当有效的取代剂，且在体内具有类似PCP的行为特性。这些结果表明苯环己哌啶和σ阿片类药物作用于相同位点。通过使用氚敏感的LKB胶片，并经计算机密度测定和颜色编码分析来观察[3H]PCP结合位点。[3H]PCP在皮质区域结合最密集，在新皮质中呈弥散性结合，在海马结构和齿状回层中结合有些不均匀。脑干和脊髓的大部分区域显示低特异性[3H]PCP结合，灰质的结合通常比白质更多。
