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Comparison of [H-3]tamsulosin and [H-3]prazosin binding to wild-type and constitutively active alpha(1B)-adrenoceptors

机译：[H-3]坦索罗辛和[H-3]哌唑嗪与野生型和组成型活性α（1B）肾上腺素受体的结合的比较

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We have tested the hypothesis that smaller alpha(1B)-adrenoceptor labeling by [H-3]tamsulosin compared to [H-3]prazosin is related to differential recognition of agonist low affinity states. Paired saturation binding experiments with [H-3]prazosin and [H-3]tamsulosin were performed in membrane preparations from rat liver and Rat-1 fibroblasts stably transfected with wild-type hamster alpha(1B)-adrenoceptors or a constitutively active mutant thereof. In all three settings [H-3]tamsulosin labeled significantly fewer alpha(1B)-adrenoceptors than [H-3]prazosin. In noradrenaline competition binding experiments, the percentage of agonist low affinity sites was smallest for the constitutively active alpha(1B)-adrenoceptor but the percentage of agonist low affinity sites recognized by [H-3]tamsulosin and [H-3]prazosin did not differ significantly. We conclude that [H-3]tamsulosin labels fewer alpha(1B)-adrenoceptors than [H-3]prazosin but this is not fully explained by a poorer labeling of agonist low affinity sites. (C) 2000 Elsevier Science Inc, All rights reserved. [References: 13]
机译：我们已经测试了以下假设，即与[H-3]吡唑嗪相比，由[H-3]坦索罗辛标记的α（1B）-肾上腺素受体较小，与激动剂低亲和力状态的差异识别有关。在稳定转染了野生仓鼠α（1B）-肾上腺素受体或其组成型活性突变体的大鼠肝脏和成年大鼠成纤维细胞的膜制剂中，进行了[H-3]普拉唑嗪和[H-3]坦索罗辛的成对饱和结合实验。在所有三个设置中，[H-3]坦索罗辛标记的α（1B）-肾上腺素受体明显少于[H-3]吡唑嗪。在去甲肾上腺素竞争结合实验中，组成型活性α（1B）-肾上腺素受体激动剂低亲和力位点的百分比最小，但[H-3]坦索罗辛和[H-3]普拉唑嗪识别的激动剂低亲和力位点的百分比没有差异很大。我们得出的结论是[H-3]坦索罗辛比[H-3] Prazosin标记更少的alpha（1B）-肾上腺素能受体，但这不能由激动剂低亲和力部位的较差标记完全解释。 （C）2000 Elsevier Science Inc，保留所有权利。 [参考：13]

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