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首页> 外文期刊>American Journal of Physiology >Alpha1-adrenoceptor subtypes on rat afferent arterioles assessed by radioligand binding and RT-PCR.
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Alpha1-adrenoceptor subtypes on rat afferent arterioles assessed by radioligand binding and RT-PCR.

机译：通过放射性配体结合和RT-PCR评估大鼠传入小动脉上的Alpha1-肾上腺素受体亚型。

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摘要

We utilized [3H]prazosin saturation and competition radioligand binding studies to characterize the expression of alpha1-adrenoceptors in preglomerular vessels. mRNA for adrenoceptor subtypes was assayed using RT-PCR. The vessels were isolated using an iron oxide-sieving method. [3H]prazosin bound to a single class of binding sites (Kd 0.087 +/- 0.012 nM, Bmax 326 +/- 56 fmol/mg protein). Phentolamine displaced [3H]prazosin (0.2 nM) with a pK(i) of 8.37 +/- 0.09. Competition with the selective alpha1A-adrenoceptor antagonist 5-methylurapidil fit a two-site model (pK(i) 9.38 +/- 0.21 and 7.04 +/- 0.15); 59 +/- 3% of the sites were high-affinity, and 41 +/- 3% were low-affinity binding sites. Competition with the alpha1D-adrenoceptor antagonist 8-(2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl)-8-azaspiro[4.5]decane-7,9-d ione dihydrochloride (BMY-7378) fit a one-site model with low affinity (pK(i) 6.83 +/- 0.03). The relative contents of alpha1A-, alpha1B-, and alpha1D-adrenoceptor mRNAs were 64 +/- 5, 25 +/- 5, and 11 +/- 1%, respectively. Thus there was a very good correlation between mRNA and receptor binding for the subtypes. These data indicate a predominance of the alpha1A-adrenoceptor subtype in rat renal resistance vessels, with smaller densities of alpha1B- and alpha1D-adrenoceptors.
机译：我们利用[3H] prazosin饱和度和竞争放射性配体结合研究来表征肾小球前血管中α1-肾上腺素受体的表达。使用RT-PCR测定肾上腺素能受体亚型的mRNA。使用氧化铁筛分法分离容器。 [3H] prazosin与单类结合位点结合（Kd 0.087 +/- 0.012 nM，Bmax 326 +/- 56 fmol / mg蛋白）。苯酚酚胺取代的[3H]吡唑嗪（0.2 nM），pK（i）为8.37 +/- 0.09。与选择性α1A-肾上腺素受体拮抗剂5-甲基尿嘧啶的竞争符合两点模型（pK（i）9.38 +/- 0.21和7.04 +/- 0.15）; 59 +/- 3％的位点是高亲和力，而41 +/- 3％是低亲和力的结合位点。与alpha1D-肾上腺素受体拮抗剂8-（2- [4-（2-甲氧基苯基）-1-哌嗪基]乙基）-8-氮杂螺[4.5]癸烷-7,9-d离子二盐酸盐（BMY-7378）的竞争低亲和力的单站点模型（pK（i）6.83 +/- 0.03）。 α1A-，α1B-和α1D-肾上腺素受体mRNA的相对含量分别为64 +/- 5、25 +/- 5和11 +/- 1％。因此，亚型的mRNA和受体结合之间具有非常好的相关性。这些数据表明，在大鼠肾脏抗性血管中，α1A-肾上腺素受体亚型占主导地位，α1B-和α1D-肾上腺素受体的密度较小。

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