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锌离子对脑啡肽与阿片受体结合的抑制作用:在大脑中可能具有的生理重要性。

Inhibition of enkephalin binding to opiate receptors by zinc ions: possible physiological importance in the brain.

作者信息

Stengaard-Pedersen K

出版信息

Acta Pharmacol Toxicol (Copenh). 1982 Mar;50(3):213-20. doi: 10.1111/j.1600-0773.1982.tb00964.x.

DOI:10.1111/j.1600-0773.1982.tb00964.x
PMID:6283789
Abstract

Zinc ions can totally block stereospecific binding of 3H-met-enkephalinamide (2-D-ala-5-L-methionine) to opiate receptor sites in synaptic membranes of the hippocampus, the cerebral cortex and the basal ganglia of the rat brain. Analysis of binding isotherms indicates that this inhibitory effect involves a decrease in both receptor affinity and the number of binding sites. Our data also suggest that the zinc ions react with essential SH-groups of the opiate receptor. The endogenous concentrations of zinc ions in the hippocampus, the cerebral cortex and the basal ganglia are compatible with the concentrations needed to inhibit opiate receptor binding in vitro. Especially the hippocampus contains a high concentration of zinc ion, which are localized exclusively in the giant boutons of the mossy fibers. Further, the hippocampal distribution of enkephalin and zinc ions is identical and confined to the mossy fiber zone. Hence, zinc ions may represent important modulators of opiate receptor binding in the central nervous system, particularly in the hippocampal mossy fiber zone.

摘要

锌离子能够完全阻断3H-甲硫氨酸脑啡肽酰胺(2-D-丙氨酸-5-L-甲硫氨酸)与大鼠脑海马、大脑皮层及基底神经节突触膜上阿片受体位点的立体特异性结合。结合等温线分析表明,这种抑制作用涉及受体亲和力和结合位点数量的降低。我们的数据还表明,锌离子与阿片受体的必需巯基发生反应。海马、大脑皮层及基底神经节中锌离子的内源性浓度与体外抑制阿片受体结合所需的浓度相符。尤其是海马中含有高浓度的锌离子,这些锌离子仅定位于苔藓纤维的巨大终扣中。此外,脑啡肽和锌离子在海马中的分布是相同的,且局限于苔藓纤维区。因此,锌离子可能是中枢神经系统中阿片受体结合的重要调节剂,尤其是在海马苔藓纤维区。

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Inhibition of enkephalin binding to opiate receptors by zinc ions: possible physiological importance in the brain.锌离子对脑啡肽与阿片受体结合的抑制作用:在大脑中可能具有的生理重要性。
Acta Pharmacol Toxicol (Copenh). 1982 Mar;50(3):213-20. doi: 10.1111/j.1600-0773.1982.tb00964.x.
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Inhibition of opiate receptor binding by zinc ions: possible physiological importance in the hippocampus.锌离子对阿片受体结合的抑制作用:在海马体中的潜在生理重要性。
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[Interaction of D-Ala2-[Tyr-3,5-3H]enkephalin(5-D-Leu) with opiate receptors of rat brain].[D-丙氨酸2-[酪氨酸-3,5-3H]脑啡肽(5-D-亮氨酸)与大鼠脑阿片受体的相互作用]
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Modulation of mu, delta and kappa opioid receptors in rat brain by metal ions and histidine.金属离子和组氨酸对大鼠脑内μ、δ和κ阿片受体的调节作用。
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