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幼年和成年仓鼠胰岛中α2-肾上腺素能受体及非肾上腺素能咪唑克生结合位点的鉴定

Identification of alpha 2-adrenoceptors and of non-adrenergic idazoxan binding sites in pancreatic islets from young and adult hamsters.

作者信息

Lacombe C, Viallard V, Paris H

机构信息

INSERM U 317, Institut Louis Bugnard, CHU Rangueil, Toulouse, France.

出版信息

Int J Biochem. 1993 Jul;25(7):1077-83. doi: 10.1016/0020-711x(93)90124-w.

Abstract
  1. The current study was undertaken to investigate the characteristics of alpha 2-adrenoceptors and to search for the presence of NAIBS in hamster pancreatic islets. 2. Pancreatic islets were isolated from young (6-7 weeks) and adult (14-15 weeks) animals. 3. The identification of alpha 2-adrenoceptors using [3H]RX821002 indicated that adults exhibited higher number of alpha 2-adrenoceptors than the young animals (194 +/- 20 vs 105 +/- 16 fmol/mg protein) while the Kd value was unchanged. 4. Glucose-evoked insulin release was completely inhibited by the alpha 2-agonist clonidine (0.1 microM) whatever the age of the animals. Agonist inhibition curves showed the following rank order of potency: clonidine > UK14304 > adrenaline. 5. Blockade of UK14304-elicited inhibition by various antagonists indicated that yohimbine has a low affinity for the receptor supporting the conclusion that the receptor is of the alpha 2-D subtype. 6. Binding experiments with [3H]idazoxan under conditions allowing to discriminate between alpha 2-adrenoceptors and NAIBS showed that hamster pancreatic islets express a high number of NAIBS. The density of NAIBS was similar in young and adult hamsters (1550 +/- 245 and 1342 +/- 332 fmol/mg protein).
摘要
  1. 本研究旨在调查α2 - 肾上腺素能受体的特征,并探寻仓鼠胰岛中是否存在非典型α2 - 肾上腺素能结合位点(NAIBS)。2. 从幼年(6 - 7周)和成年(14 - 15周)动物中分离出胰岛。3. 使用[3H]RX821002鉴定α2 - 肾上腺素能受体表明,成年动物的α2 - 肾上腺素能受体数量高于幼年动物(194±20对105±16 fmol/mg蛋白),而解离常数(Kd)值不变。4. 无论动物年龄如何,α2 - 激动剂可乐定(0.1μM)均可完全抑制葡萄糖诱发的胰岛素释放。激动剂抑制曲线显示出以下效力顺序:可乐定>UK14304>肾上腺素。5. 各种拮抗剂对UK14304引起的抑制作用的阻断表明,育亨宾对该受体的亲和力较低,支持该受体为α2 - D亚型的结论。6. 在能够区分α2 - 肾上腺素能受体和NAIBS的条件下,用[3H]咪唑克生进行的结合实验表明,仓鼠胰岛表达大量的NAIBS。幼年和成年仓鼠中NAIBS的密度相似(1550±245和1342±332 fmol/mg蛋白)。

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