[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.
Abstract
- [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
- [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。
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