Vincent J P, Kartalovski B, Geneste P, Kamenka J M, Lazdunski M
Proc Natl Acad Sci U S A. 1979 Sep;76(9):4678-82. doi: 10.1073/pnas.76.9.4678.
[3H]Phencyclidine binds to synaptic membranes from rat brain in a saturable, reversible, and selective fashion, with a dissociation constant Kd of 0.25 microM and a maximal binding capacity of 2.4 pmol/mg of membrane protein--i.e., 250 pmol/g of brain. The binding activity is concentrated in synaptosomal fractions, is higher in cerebral cortex and corpus striatum than in other parts of the rat brain, and is not detectable in the spinal cord. Only molecules of the phencyclidine series and ketamine are able to bind to the phencyclidine receptor. [3H]Phencyclidine bound to its receptor is not displaced by the classical neurotransmitters or neuromodulators. There is a good correlation between the apparent affinities of a series of phencyclidine analogs for the phencyclidine receptor and the pharacological activities of these analogs as measured by the rotarod assay.
[3H]苯环己哌啶以可饱和、可逆且具有选择性的方式与大鼠脑突触膜结合，解离常数Kd为0.25微摩尔，最大结合容量为2.4皮摩尔/毫克膜蛋白，即250皮摩尔/克脑。结合活性集中在突触体部分，在大脑皮层和纹状体中比在大鼠脑的其他部位更高，在脊髓中无法检测到。只有苯环己哌啶系列分子和氯胺酮能够与苯环己哌啶受体结合。与苯环己哌啶受体结合的[3H]苯环己哌啶不会被经典神经递质或神经调节剂取代。一系列苯环己哌啶类似物对苯环己哌啶受体的表观亲和力与通过转棒试验测量的这些类似物的药理活性之间存在良好的相关性。
