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钒酸盐抑制激动剂与D2多巴胺受体的结合。

Vanadate inhibits agonist binding to D2 dopamine receptor.

作者信息

Elazar Z, Fuchs S

机构信息

Department of Chemical Immunology, Weizmann Institute of Science, Rehovot, Israel.

出版信息

J Mol Neurosci. 1991;3(1):1-6. doi: 10.1007/BF02896843.

DOI:10.1007/BF02896843
PMID:1679343
Abstract

Orthovanadate (in the micromolar range) inhibits the high-affinity binding of the D2 dopamine receptor to specific agonists (apomorphine and N-propylnorapomorphine), while it does not affect the binding to D2 antagonists (spiperone and haloperidol). These effects of vanadate resemble those observed with guanine nucleotides or their analogs. However, in contrast to the guanine nucleotides, vanadate does not induce dissociation of the D2 dopamine receptor from its related G proteins, suggesting that vanadate and guanine nucleotides may exert their effect on the D2 dopamine receptor via different mechanisms. The effect of vanadate on agonist binding was shown to be ATP dependent and correlated with increased protein phosphorylation.

摘要

原钒酸盐(在微摩尔范围内)可抑制D2多巴胺受体与特定激动剂(阿扑吗啡和N-丙基去甲阿扑吗啡)的高亲和力结合,而不影响其与D2拮抗剂(螺哌隆和氟哌啶醇)的结合。钒酸盐的这些作用类似于用鸟嘌呤核苷酸或其类似物所观察到的作用。然而,与鸟嘌呤核苷酸不同的是,钒酸盐不会诱导D2多巴胺受体与其相关G蛋白解离,这表明钒酸盐和鸟嘌呤核苷酸可能通过不同机制对D2多巴胺受体发挥作用。已证明钒酸盐对激动剂结合的作用是ATP依赖性的,且与蛋白质磷酸化增加相关。

相似文献

1
Vanadate inhibits agonist binding to D2 dopamine receptor.钒酸盐抑制激动剂与D2多巴胺受体的结合。
J Mol Neurosci. 1991;3(1):1-6. doi: 10.1007/BF02896843.
2
Characterization of high-affinity dopamine D2 receptors and modulation of affinity states by guanine nucleotides in cholate-solubilized bovine striatal preparations.
J Neurochem. 1986 Nov;47(5):1493-502. doi: 10.1111/j.1471-4159.1986.tb00784.x.
3
Chronic haloperidol does not alter agonist affinity for dopamine receptors in vitro.慢性给予氟哌啶醇不会在体外改变激动剂对多巴胺受体的亲和力。
Eur J Pharmacol. 1985 Mar 12;109(3):389-94. doi: 10.1016/0014-2999(85)90400-5.
4
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Stimulation of high-affinity adenosine A2 receptors decreases the affinity of dopamine D2 receptors in rat striatal membranes.刺激高亲和力腺苷A2受体可降低大鼠纹状体膜中多巴胺D2受体的亲和力。
Proc Natl Acad Sci U S A. 1991 Aug 15;88(16):7238-41. doi: 10.1073/pnas.88.16.7238.
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Dopamine D2 receptors in the anterior pituitary: a single population without reciprocal antagonist/agonist states.垂体前叶中的多巴胺D2受体:单一群体,不存在相互拮抗/激动状态。
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本文引用的文献

1
Dopamine receptors in brain and periphery.大脑和外周的多巴胺受体。
Neurochem Int. 1987;10(1):1-25. doi: 10.1016/0197-0186(87)90167-7.
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Dopamine inhibits 32P incorporation into phosphatidylinositol in the anterior pituitary gland of the rat.
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Insulin stimulates the phosphorylation of the 95,000-dalton subunit of its own receptor.胰岛素刺激其自身受体95,000道尔顿亚基的磷酸化。
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Changes in pH sensitivity of adenylate cyclase specifically induced by fluoride and vanadate.
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Vanadate, epidermal growth factor and the stimulation of DNA synthesis.钒酸盐、表皮生长因子与DNA合成的刺激作用
Biochem Biophys Res Commun. 1981 Oct 30;102(4):1115-21. doi: 10.1016/s0006-291x(81)80127-1.
6
Insulin-like effect of vanadate on adipocyte glycogen synthase and on phosphorylation of 95,000 dalton subunit of insulin receptor.钒酸盐对脂肪细胞糖原合酶及胰岛素受体95000道尔顿亚基磷酸化的胰岛素样作用。
Biochem Biophys Res Commun. 1983 May 31;113(1):80-6. doi: 10.1016/0006-291x(83)90434-5.
7
Vanadium ions stimulate DNA synthesis in Swiss mouse 3T3 and 3T6 cells.钒离子可刺激瑞士小鼠3T3和3T6细胞中的DNA合成。
Proc Natl Acad Sci U S A. 1983 Oct;80(20):6162-6. doi: 10.1073/pnas.80.20.6162.
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Identification, purification, and characterization of phosphotyrosine-specific protein phosphatases from cultured chicken embryo fibroblasts.从培养的鸡胚成纤维细胞中鉴定、纯化和表征磷酸酪氨酸特异性蛋白磷酸酶。
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Pharmacological characterization of the D2 dopamine receptor negatively coupled with adenylate cyclase in rat anterior pituitary.大鼠垂体前叶中与腺苷酸环化酶负偶联的D2多巴胺受体的药理学特性
Mol Pharmacol. 1983 May;23(3):576-84.
10
Inhibition of membrane phosphotyrosyl-protein phosphatase activity by vanadate.钒酸盐对膜磷酸酪氨酸蛋白磷酸酶活性的抑制作用。
Biochem Biophys Res Commun. 1982 Aug;107(3):1104-9. doi: 10.1016/0006-291x(82)90635-0.