(+)-[3H]MK-801 binding sites in postmortem human brain.
(+)-[3H]MK-801 binding sites in postmortem human brain.
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( )-[3H]MK-801 死后人脑中的结合位点。
DOI：
10.1111/j.1471-4159.1990.tb01944.x
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发表时间：
1990
影响因子：
4.7
通讯作者：
Weber,E
中科院分区：
文献类型：
--
作者：
Quarum,ML;Parker,JD;Keana,JF;Weber,E
通过使用（+）-[3 H]MK-801的结合研究，确定了人死后脑组织中N-甲基-D-天冬氨酸受体相关5-甲基-10，11-二氢-5H-二苯并[a，d]环庚烯-5，10-亚胺马来酸盐（MK-801）结合位点的药理学特异性和区域分布。Scatchard分析显示了高亲和力（KD= 0.9 ± 0.2 nM，Bmax= 499 ± 33 fmol/mg蛋白质）和低亲和力（KD= 3.6 ± 0.9 nM，Bmax= 194 ± 44 fmol/ mg蛋白质）结合位点。与低亲和力结合位点（小脑>脑干）相比，高亲和力位点显示出不同的受体密度区域分布（皮质>海马>纹状体）。高亲和力（皮质）和低亲和力（小脑）结合位点的秩序药理学特异性和立体选择性相同。然而，所有测试的化合物在皮质中的高亲和力位点显示出更大的效力。结果表明，（+）[3 H]MK-801在人死后脑组织中的结合具有药理学和区域特异性。
The pharmacological specificity and the regional distribution of theN‐methyl‐D‐aspartate receptor‐associated 5‐methyl‐10,11‐dihydro‐5H‐dibenzo[a,d]cyclohepten‐5, 10‐imine maleate (MK‐801) binding sites in human postmortem brain tissue were determined by binding studies using (+)‐[3H]MK‐801. Scatchard analysis revealed a high‐affinity (KD= 0.9 ± 0.2 nM,Bmax= 499 ± 33 fmol/mg of protein) and a low‐affinity (KD= 3.6 ± 0.9 nM,Bmax= 194 ± 44 fmol/ mg of protein) binding site. The high‐affinity site showed a different regional distribution of receptor density (cortex > hippocampus > striatum) compared to the low‐affinity binding site (cerebellum > brainstem). The rank order pharmacological specificity and stereoselectivity of the high‐(cortex) and low‐(cerebellar) affinity binding sites were identical. However, all compounds tested showed greater potency at the high‐affinity site in cortex. The results indicate that (+)[3H]MK‐801 binding in human postmortem brain tissue shows pharmacological and regional specificity.