Interaction of phencyclidine ("angel dust") with a specific receptor in rat brain membranes.
Interaction of phencyclidine ("angel dust") with a specific receptor in rat brain membranes.
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苯环己哌啶（“天使之尘”）与大鼠脑膜中特定受体的相互作用。
DOI：
10.1073/pnas.76.9.4678
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发表时间：
1979
影响因子：
11.1
通讯作者：
M. Lazdunski
中科院分区：
文献类型：
--
作者：
J. Vincent;B. Kartalovski;P. Geneste;J. Kamenka;M. Lazdunski
苯环利定以可饱和的、可逆的和选择性的方式与大鼠脑突触膜结合，其解离常数Kd为0.25微米，最大结合容量为2.4pmol/mg膜蛋白--即250pmol/g脑。结合活性集中在突触体组分，大脑皮层和纹状体的结合活性高于大鼠脑的其他部分，在脊髓中检测不到。只有苯环利定系列分子和氯胺酮能够与苯环利定受体结合。与其受体结合的苯环利定不会被经典的神经递质或神经调节剂取代。一系列苯环利定类似物对苯环利定受体的表观亲和力与用旋转棒试验测得的药理活性之间有很好的相关性。
[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.