Nongenomic regulation of the kinetics of exocytosis by estrogens.
Nongenomic regulation of the kinetics of exocytosis by estrogens.
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雌激素胞吐动力学的非基因组调节。
DOI：
10.1124/jpet.301.2.631
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发表时间：
2002
期刊：
影响因子：
--
通讯作者：
R. Borges
中科院分区：
文献类型：
--
作者：
J. Machado;C. Alonso;A. Morales;José F. Gómez;R. Borges
在大鼠肾上腺灌注和培养的牛嗜铬细胞中研究了雌激素对引起的儿茶酚胺分泌和胞吐动力学的非基因组作用的作用。17 β-雌二醇以及雌激素受体调节剂雷洛昔芬和LY 117018，但不是17 α-雌二醇，在微摩尔范围内抑制乙酰胆碱或高钾引起的儿茶酚胺输出。然而，这些药物未能改变分泌引起的高钙（2+）与离子载体A-23187（calcimycin）处理的腺体，这表明雌激素没有直接作用于分泌机制。在单细胞水平上，雌激素在纳摩尔范围内改变了胞吐动力学。除17 α-雌二醇外，所有试验药物均能显著减缓胞吐作用，如安培法所测。LY 117018还降低了颗粒中的儿茶酚胺含量。17 β-雌二醇降低细胞内游离Ca（2+），但仅在微摩尔浓度下，而纳摩尔浓度增加cAMP水平。这些作用用非渗透性药物17 β-雌二醇-辣根过氧化物酶重现，并用纳摩尔浓度的抗雌激素ICI 182，780（氟维司群）拮抗。我们的数据表明，存在的膜网站，调节细胞外吞现象和总的儿茶酚胺释放高和低的亲和力，分别。
The role of nongenomic action of estrogens on elicited catecholamine secretion and exocytosis kinetics was studied in perfused rat adrenals and in cultured bovine chromaffin cells. 17beta-Estradiol as well as the estrogen receptor modulators raloxifene and LY117018, but not 17alpha-estradiol, inhibited at the micromolar range the catecholamine output elicited by acetylcholine or high potassium. However, these agents failed to modify the secretion elicited by high Ca(2+) in glands treated with the ionophore A-23187 (calcimycin), suggesting that estrogens did not directly act on the secretory machinery. At the single cell level, estrogens modified the kinetics of exocytosis at nanomolar range. All of the drugs tested except 17alpha-estradiol produced a profound slowing down of the exocytosis as measured by amperometry. LY117018 also reduced the granule content of catecholamines. 17beta-Estradiol reduced the intracellular free Ca(2+) but only at micromolar concentrations, whereas nanomolar concentrations increased the cAMP levels. These effects were reproduced with the nonpermeable drug 17beta-estradiol-horseradish peroxidase and antagonized with nanomolar concentrations of the antiestrogen ICI 182,780 (fulvestrant). Our data suggest the presence of membrane sites that regulate both the exocytotic phenomenon and the total catecholamine release with high and low affinity, respectively.
类固醇 17-α-雌二醇对肾上腺儿茶酚胺释放的膜介导作用。
DOI：
--
发表时间：
1991
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Lopez,MG;Abad,F;Sancho,C;dePascual,R;Borges,R;Maroto,R;Dixon,W;Garcia,AG
通讯作者：
Garcia,AG