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Imidazoline receptors in rat liver cells: a novel receptor or a subtype of alpha 2-adrenoceptors?大鼠肝细胞中的咪唑啉受体：一种新型受体还是α2肾上腺素能受体的一个亚型？
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Presynaptic imidazoline receptors and non-adrenoceptor [3H]-idazoxan binding sites in human cardiovascular tissues.人类心血管组织中的突触前咪唑啉受体和非肾上腺素能受体[3H]-咪唑克生结合位点
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Imidazolinic radioligands for the identification of hamster adipocyte alpha 2-adrenoceptors.用于鉴定仓鼠脂肪细胞α2-肾上腺素能受体的咪唑啉类放射性配体。
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Non-adrenergic sites for imidazolines are not directly involved in the alpha 2-adrenergic antilipolytic effect of UK 14304 in rat adipocytes.咪唑啉的非肾上腺素能位点不直接参与 UK 14304 在大鼠脂肪细胞中的α2 肾上腺素能抗脂解作用。
Biochem Pharmacol. 1990 Aug 1;40(3):437-45. doi: 10.1016/0006-2952(90)90541-r.

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Effect of a 7-day treatment with idazoxan and its 2-methoxy derivative RX 821002 [correction of RX 821001] on alpha 2-adrenoceptors and non-adrenoceptor idazoxan binding sites in rabbits.咪唑克生及其2-甲氧基衍生物RX 821002 [纠正为RX 821001] 对兔α2-肾上腺素能受体和非肾上腺素能受体咪唑克生结合位点的7天治疗效果。
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Protein measurement with the Folin phenol reagent.使用福林酚试剂进行蛋白质测定。
J Biol Chem. 1951 Nov;193(1):265-75.
2
METABOLISM OF ISOLATED FAT CELLS. I. EFFECTS OF HORMONES ON GLUCOSE METABOLISM AND LIPOLYSIS.分离脂肪细胞的代谢。I. 激素对葡萄糖代谢和脂肪分解的影响。
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High affinity 3H-cimetidine binding in guinea-pig tissues.豚鼠组织中高亲和力的3H-西咪替丁结合
Life Sci. 1980 Jul 21;27(3):199-206. doi: 10.1016/0024-3205(80)90138-1.
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Alpha 2-adrenergic inhibition of lipolysis and respiration in rat brown adipocytes.α2-肾上腺素能对大鼠棕色脂肪细胞脂解和呼吸的抑制作用。
Biochem Pharmacol. 1983 Oct 15;32(20):3117-20. doi: 10.1016/0006-2952(83)90259-9.
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Adrenergic regulation of adipocyte metabolism.脂肪细胞代谢的肾上腺素能调节
J Lipid Res. 1983 Aug;24(8):945-66.
6
Preponderance of alpha 2- over beta 1-adrenergic receptor sites in human fat cells is not predictive of the lipolytic effect of physiological catecholamines.人体脂肪细胞中α2 - 肾上腺素能受体位点多于β1 - 肾上腺素能受体位点，并不能预测生理性儿茶酚胺的脂解作用。
J Lipid Res. 1983 Apr;24(4):429-40.
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The alpha 2-adrenergic receptor of human fat cells: comparative study of alpha 2-adrenergic radioligand binding and biological response.人类脂肪细胞的α2-肾上腺素能受体：α2-肾上腺素能放射性配体结合与生物学反应的比较研究
J Physiol (Paris). 1982;78(3):279-87.
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Solubilization of a [3H]cimetidine binding site from rat brains. A clonidine-sensitive H-2 receptor subtype?大鼠脑内[3H]西咪替丁结合位点的增溶作用。一种对可乐定敏感的H-2受体亚型？
Mol Pharmacol. 1981 Sep;20(2):240-3.
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A postsynaptic alpha 2-receptor: the alpha-adrenergic receptor of hamster white fat cells.一种突触后α2受体：仓鼠白色脂肪细胞的α-肾上腺素能受体。
Experientia. 1980 Dec 15;36(12):1413-4. doi: 10.1007/BF01960132.
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Identification of alpha 2-adrenergic receptors in human fat cell membranes by [3H]chlonidine binding.通过[3H]可乐定结合鉴定人脂肪细胞膜中的α2-肾上腺素能受体。
Eur J Pharmacol. 1980 Oct 31;67(4):481-4. doi: 10.1016/0014-2999(80)90191-0.

[3H]-咪唑克生以高亲和力与仓鼠脂肪细胞上的两个位点结合：一个α2-肾上腺素能受体位点和一个非肾上腺素能受体位点。

[3H]-idazoxan binds with high affinity to two sites on hamster adipocytes: an alpha 2-adrenoceptor and a non-adrenoceptor site.

作者信息

MacKinnon A C, Brown C M, Spedding M, Kilpatrick A T

机构信息

Department of Pharmacology, Syntex Research Centre, Heriot-Watt University Research Park, Riccarton, Edinburgh.

出版信息

Br J Pharmacol. 1989 Dec;98(4):1143-50. doi: 10.1111/j.1476-5381.1989.tb12658.x.

DOI:10.1111/j.1476-5381.1989.tb12658.x
PMID:2558757
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1854795/
Abstract
  1. [3H]-idazoxan labels a single population of high affinity sites (Kd 2.26 +/- 0.02 nM; Bmax 372 +/- 25 fmol mg-1 protein) in hamster adipocyte membranes. In the presence of 1 microM yohimbine to preclude binding to alpha 2-adrenoceptors, the density of [3H]-idazoxan binding sites was reduced (287 +/- 18 fmol mg-1 protein) without an apparent decrease in the affinity (Kd 2.19 +/- 0.24 nM) of the radioligand. 2. Displacement studies indicate that alpha-adrenoceptor ligands with an imidazoline side chain completely inhibit [3H]-idazoxan binding to hamster adipocyte membranes; in contrast, the alpha 2-adrenoceptor antagonists yohimbine, rauwolscine, BDF 6143 and phentolamine inhibited only 20-30% of the specific binding with affinity values consistent with an interaction at alpha 2-adrenoceptors. 3. The low potency of noradrenaline and adrenaline in displacing [3H]-idazoxan binding to the second site on hamster adipocyte membranes indicates that it is unlikely that this site is a type of adrenoceptor. 4. These results suggest that [3H]-idazoxan binds with high affinity to two sites in hamster adipocytes: an alpha 2-adrenoceptor and a non-adrenoceptor imidazoline site.
摘要
  1. [3H]-咪唑克生标记仓鼠脂肪细胞膜中单一的高亲和力位点群体（解离常数Kd为2.26±0.02纳摩尔；最大结合量Bmax为372±25飞摩尔/毫克蛋白）。在存在1微摩尔育亨宾以防止与α2 -肾上腺素能受体结合的情况下，[3H]-咪唑克生结合位点的密度降低（287±18飞摩尔/毫克蛋白），而放射性配体的亲和力（Kd为2.19±0.24纳摩尔）没有明显下降。2. 置换研究表明，具有咪唑啉侧链的α-肾上腺素能受体配体完全抑制[3H]-咪唑克生与仓鼠脂肪细胞膜的结合；相比之下，α2 -肾上腺素能受体拮抗剂育亨宾、萝芙素、BDF 6143和酚妥拉明仅抑制20 - 30%的特异性结合，其亲和力值与在α2 -肾上腺素能受体处的相互作用一致。3. 去甲肾上腺素和肾上腺素在置换[3H]-咪唑克生与仓鼠脂肪细胞膜上第二个位点结合方面效力较低，这表明该位点不太可能是一种肾上腺素能受体类型。4. 这些结果表明，[3H]-咪唑克生以高亲和力与仓鼠脂肪细胞中的两个位点结合：一个α2 -肾上腺素能受体和一个非肾上腺素能咪唑啉位点。