Specific [3H]phencyclidine binding in rat central nervous system.
Specific [3H]phencyclidine binding in rat central nervous system.
复制标题
大鼠中枢神经系统中的特异性[3H]苯环己哌啶结合。
DOI：
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发表时间：
1979
影响因子：
11.1
通讯作者：
R. Zukin
中科院分区：
文献类型：
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作者：
S. Zukin;R. Zukin
[3H]苯环利定（Phencyclidine， PCP）在大鼠脑膜制剂中具有特异性和高亲和力（Kd = 0.15微米，pH 7.4）结合到单一饱和类结合位点。特异性结合在0℃时约占总结合的70%，在37℃（10 nM [3H]PCP）时约占总结合的33%。结合的[3H]PCP可被非放射性PCP、其一系列衍生物和拟精神阿片类药物n -烯丙基去环唑嗪（SKF 10,047）取代，其相对效力与动物行为试验中测定的结果密切相关。毒蕈碱胆碱能配体抑制[3H]PCP结合，但仅在0.1 mM，且与毒蕈碱位点结合或药理学效力的等级不同。其他药物，包括SKF 10047以外的阿片类药物，在0.1 mM处不能取代特异性结合的[3H]PCP。[3H]PCP结合在粗突触体亚细胞部分最富集，海马（密度最高的区域）的含量约为脊髓（密度最低的区域）的3倍。胰蛋白酶和Pronase降低了特异性[3H]PCP结合。因此，PCP可能通过结合特定的脑受体部位对中枢神经系统产生影响。
[3H]Phencyclidine (PCP) bound specifically and with high affinity (Kd = 0.15 microM at pH 7.4) to a single saturable class of binding sites in rat brain membrane preparations. Specific binding constituted approximately 70% of total binding at 0 degrees C and 33% of total binding at 37 degrees C (at 10 nM [3H]PCP). Bound [3H]PCP could be displaced by nonradioactive PCP, a series of its derivatives, and the psychotomimetic opiate N-allylnorcyclazocine (SKF 10,047) with relative potencies that closely paralleled those determined in animal behavioral tests. Muscarinic cholinergic ligands inhibited [3H]PCP binding, but only at 0.1 mM and in rank order at variance with that for binding to muscarinic sites or for pharmacological potencies. Other drugs, including opiates other than SKF 10,047, were unable to displace specifically bound [3H]PCP at 0.1 mM. [3H]PCP binding was most enriched in crude synaptosomal subcellular fractions, and was about three times higher in hippocampus (region of highest density) than in cervical spinal cord (region of lowest density). Trypsin and Pronase reduced specific [3H]PCP binding. Thus, PCP may exert its effects on the central nervous system via binding to specific brain receptor sites.