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十钒酸盐具有α-肾上腺素能激动剂活性,且具有与去甲肾上腺素反式-β形式相同的结构基序。

Decavanadate possesses alpha-adrenergic agonist activity and a structural motif common with trans-beta form of noradrenaline.

作者信息

Venkataraman B V, Ravishankar H N, Rao A V, Kalyani P, Sharada G, Namboodiri K, Gabor B, Ramasarma T

机构信息

Department of Biochemistry, Indian Institute of Science, Bangalore, India.

出版信息

Mol Cell Biochem. 1997 Apr;169(1-2):27-36. doi: 10.1023/a:1006882408983.

DOI:10.1023/a:1006882408983
PMID:9089628
Abstract

Decavanadate, an inorganic polymer of vanadate, produced contraction of rat aortic rings at a relatively high concentration compared to phenylephrine, an agonist of alpha-adrenergic receptor. This effect was blocked by two known alpha-adrenergic receptor antagonists, prazosin and phenoxybenzamine. Decavanadate, formed by possible dimerization of V5 under acid conditions, possessed a structural feature of two pairs of unshared oxygen atoms at a distance of 3.12 A, not found in its constituents of V4 or V5. A structural motif of O..O..O using such oxygen atoms is recognized in decavanadate. This matches with a similar motif of N..O..O that uses the essential amino and hydroxyl groups of the side-chain and the m-hydroxyl group in trans-beta form of noradrenaline. The interaction of such a structural motif with the membrane receptor is likely to be the basis of the unusual noradrenaline-mimic action of decavanadate.

摘要

十钒酸盐是钒酸盐的一种无机聚合物,与α-肾上腺素能受体激动剂去氧肾上腺素相比,它在相对较高的浓度下能使大鼠主动脉环收缩。这种效应被两种已知的α-肾上腺素能受体拮抗剂哌唑嗪和酚苄明阻断。十钒酸盐可能是在酸性条件下由V5二聚形成的,具有两对非共享氧原子,其间距为3.12 Å的结构特征,这在其V4或V5成分中未发现。在十钒酸盐中可识别出使用此类氧原子的O..O..O结构基序。这与使用去甲肾上腺素反式β形式侧链的必需氨基和羟基以及间羟基的类似N..O..O基序相匹配。这种结构基序与膜受体的相互作用可能是十钒酸盐异常的去甲肾上腺素模拟作用的基础。

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Decavanadate possesses alpha-adrenergic agonist activity and a structural motif common with trans-beta form of noradrenaline.十钒酸盐具有α-肾上腺素能激动剂活性,且具有与去甲肾上腺素反式-β形式相同的结构基序。
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本文引用的文献

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Contractile effects of vanadate on aorta rings from virgin and pregnant rats.钒酸盐对未孕和孕鼠主动脉环的收缩作用。
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Role of calcium ions in the regulation of intramitochondrial metabolism. Properties of the Ca2+-sensitive dehydrogenases within intact uncoupled mitochondria from the white and brown adipose tissue of the rat.钙离子在调节线粒体内代谢中的作用。大鼠白色和棕色脂肪组织完整解偶联线粒体中钙敏感脱氢酶的特性。
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Mechanism of vanadate-induced contraction of airways smooth muscle of the guinea-pig.钒酸盐诱导豚鼠气道平滑肌收缩的机制。
Br J Pharmacol. 1983 Sep;80(1):163-72. doi: 10.1111/j.1476-5381.1983.tb11062.x.
10
Does vanadium play a role in cellular regulation?钒在细胞调节中起作用吗?
Curr Top Cell Regul. 1981;20:247-301. doi: 10.1016/b978-0-12-152820-1.50011-0.