Binding of naloxone to human T lymphocytes.
Binding of naloxone to human T lymphocytes.
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DOI：
10.1016/0006-2952(87)90567-3
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发表时间：
1987-12
影响因子：
5.8
通讯作者：
J. Madden;Robert M. Donahoe;Jan Zwemer-Collins;David A. Shafer;Arthur Falek
中科院分区：
文献类型：
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作者：
J. Madden;Robert M. Donahoe;Jan Zwemer-Collins;David A. Shafer;Arthur Falek
纯化的T淋巴细胞与阿片类拮抗剂纳洛酮有特定的结合部位。该位点的KD为50.6±2.4 nM，Hill系数(N)为1.67±0.16，表明配体结合具有正协同作用。结合的纳洛酮可被多种阿片激动剂部分取代，包括吗啡(56%)、β-内啡肽(61%)、脑啡肽和亮氨酸脑啡肽(各40%)、脑啡肽(78%)和脑啡胺(66%)。在细胞超声裂解后，几乎所有的结合能力都在颗粒膜组分中恢复。样本之间的Bmax存在很大的个体间差异，这可能是不同个体之间药物作用差异的可能机制基础。
Purified T lymphocytes have a specific binding site for naloxone, the opiate antagonist. TheKDfor the site was 50.6 ± 2.4 nM, while the Hill coefficient (n) was 1.67 ± 0.16, indicating a degree of positive cooperativity of ligand binding. The bound naloxone was partially displaceable by various opiate agonists including morphine (56%), β-endorphin (61%), met5- and leu5-enkephalin (40% each), [dala2,dleu5]-enkephalin (78%) and [dala2,dleu5]-enkephalinamide (66%). Virtually all of the binding capacity was recovered in the particulate membrane fraction after sonic lysis of the cells. There was great interindividual variability inBmaxbetween samples, suggesting a possible mechanistic basis for the variability in drug action seen between different individuals.