Computer-assisted analysis of receptor-binding studies of [3H]-naloxone and [3H]-DADL: a reinterpretation of the Na+ effect.
Computer-assisted analysis of receptor-binding studies of [3H]-naloxone and [3H]-DADL: a reinterpretation of the Na+ effect.
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DOI：
10.1016/0024-3205(83)90469-1
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发表时间：
1983
期刊：
影响因子：
6.1
通讯作者：
Gilda H. Leow;L. Toll;C. Keys
中科院分区：
文献类型：
--
作者：
Gilda H. Leow;L. Toll;C. Keys
在存在和不存在100 mM NaCl的情况下，对[3 H]-纳洛酮、[3 H-DADL、吗啡和哌替啶的竞争性结合研究进行了计算机辅助分析。结果与阿片受体的3位点模型最一致，表明在存在Na+时，纳洛酮从μ特异性（81%）变为κ特异性更强（63%）的配体。发现三种激动剂（DADL、吗啡和哌替啶）抑制[3 H]-纳洛酮的IC 50变化较大，不是由于在任何受体位点的亲和力降低，而是由于存在Na+时这些激动剂在“κ”处的亲和力较低。
Computer-assisted analysis of competitive binding studies of [3H]-naloxone, [3H-DADL, morphine and meperidine in the presence and absence of 100 mM NaCl have been made. The results are most consistent with a 3-site model of opiate receptors and indicate that in the presence of Na+naloxone changes from a μ-specific (81%) to a more κ-specific (63%) ligand. The large IC50shift in inhibition of [3H]-naloxone by three agonists, DADL, morphine and meperidine is found not to be due to a decrease in affinity at any receptor site but rather to a low affinity of these agonists at “κ” in the presence of Na+.