Quirion R, Pert C B
Prog Neuropsychopharmacol Biol Psychiatry. 1983;7(4-6):451-6. doi: 10.1016/0278-5846(83)90010-6.
[3H]Phencyclidine (PCP, Angel Dust) receptors have been characterized using a rat brain binding section technique. [3H]PCP labels a single class of site in rat brain (KD = 46 nM; Bmax = 10.5 fmol/slice). Ligand selectivity pattern strongly suggests that [3H]PCP binds to sites relevant for its pharmacological actions. Chronic PCP treatment (10 mg/kg/day for 14 days) decreases the number of sites (Bmax) for [3H]PCP and [3H]spiperone binding but not for [3H]dihydromorphine. These modifications could be related to the development of tolerance and dependence to PCP. Visualization of [3H]PCP binding sites shows high densities of receptors in cortical areas and hippocampus. Lower densities are observed in caudate-putamen, nucleus accumbens, and amygdala. Negligible quantities of receptors are seen in brain stem and over white matter. The presence of specific [3H]PCP binding sites in rat brain suggests the possible existence of an endogenous ligand for this unique receptor.
已使用大鼠脑结合切片技术对[3H]苯环己哌啶（PCP，天使粉）受体进行了表征。[3H]PCP标记大鼠脑中的单一类位点（KD = 46 nM；Bmax = 10.5 fmol/切片）。配体选择性模式强烈表明[3H]PCP与与其药理作用相关的位点结合。慢性PCP治疗（10 mg/kg/天，持续14天）可减少[3H]PCP和[3H]螺哌隆结合的位点数量（Bmax），但不影响[3H]二氢吗啡的结合位点数量。这些改变可能与对PCP耐受性和依赖性的发展有关。[3H]PCP结合位点的可视化显示皮质区域和海马体中受体密度较高。在尾状核-壳核、伏隔核和杏仁核中观察到较低的密度。在脑干和白质中可见到可忽略不计数量的受体。大鼠脑中存在特异性[3H]PCP结合位点表明可能存在这种独特受体的内源性配体。
