幼鼠和成年仓鼠胰岛α 2-肾上腺素受体和非肾上腺素能性咪唑嗪结合位点的鉴定。

C Lacombe, V Viallard, H Paris
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引用次数: 16

摘要

1. 本研究旨在探讨- 2肾上腺素受体的特征,并在仓鼠胰岛中寻找NAIBS的存在。2. 从幼龄动物(6-7周龄)和成年动物(14-15周龄)中分离胰岛。3.用[3H]RX821002对α 2-肾上腺素受体进行鉴定表明,成年鼠α 2-肾上腺素受体的数量高于幼年鼠(194 +/- 20 vs 105 +/- 16 fmol/mg protein),而Kd值不变。4. 无论动物的年龄大小,α 2激动剂可乐定(0.1微米)都能完全抑制葡萄糖诱发的胰岛素释放。激动剂抑制曲线效价顺序为:可乐定> UK14304 >肾上腺素。5. 多种拮抗剂阻断uk14304引起的抑制表明育亨宾对该受体具有低亲和力,支持该受体为α 2-D亚型的结论。6. 在区分α 2-肾上腺素受体和NAIBS的条件下,与[3H]咪唑嗪的结合实验表明,仓鼠胰岛表达大量的NAIBS。NAIBS在幼鼠和成年仓鼠体内的密度相似,分别为1550 +/- 245和1342 +/- 332 fmol/mg蛋白。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Identification of alpha 2-adrenoceptors and of non-adrenergic idazoxan binding sites in pancreatic islets from young and adult hamsters.

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).

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