Expression of renal alpha 1-adrenergic receptor subtypes in established hypertension.
Expression of renal alpha 1-adrenergic receptor subtypes in established hypertension.
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已确诊的高血压中肾α1-肾上腺素能受体亚型的表达。
DOI：
10.1097/00005344-199206000-00003
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发表时间：
1992
影响因子：
3
通讯作者：
Insel,PA
中科院分区：
文献类型：
--
作者：
Jackson,CA;Michel,MC;Insel,PA
在血压正常和高血压大鼠的肾膜中进行放射性配体结合研究，以检验遗传性高血压动物的肾[α] 1-肾上腺素能亚型存在改变的假设。最初的研究表明，高选择性竞争化合物（+）-尼古地平在区分大鼠肾膜中的ala和alb位点时具有比5-甲基乌拉地尔更高的选择性，之后，该化合物被用于区分高亲和力（[alpha] 1a）和低亲和力（[alpha] 1b）位点。与自发性高血压大鼠血压的显着差异（[DELTA] BP= 74 mm Hg）相反，肾脏[alpha] 1-肾上腺素能受体密度没有差异。自发性高血压大鼠（SHR）全肾细胞膜上有31%的[α] 1a和69%的[α] 1b位点，（+）-尼古地平的-log（Ki）值分别为10.0+/-0.3和7.1+/-0.1。然而，这些值与从血压正常的Wistar-Kyoto（WKY）大鼠的肾膜获得的值没有不同。这些结果表明，尽管在高血压的建立阶段血压升高，但[alpha] 1a和[alpha] lb的数量、亲和力和比例似乎与该阶段高血压的表现无关。
Radioligand binding studies were undertaken in renal membranes of normotensive and hypertensive rats in order to test the hypothesis that there are alterations in renal [alpha] 1-adrenergic subtypes of genetic hypertensive animals. The highly selective competitive compound,(+)-niguldipine, was used to distinguish high-affinity ([alpha] 1a) from low-affinity ([alpha] 1b) sites, after initial studies demonstrated that this compound had greater selectivity than 5-methylurapidil in distinguishing ala and alb sites in rat renal membranes. In contrast to the significant difference in the blood pressure of the spontaneously hypertensive rats ([DELTA] BP= 74 mm Hg), there was no difference in the renal [alpha] 1-adrenergic receptor density. Membranes from the whole kidneys of spontaneously hypertensive rats (SHRs) possessed 31%[alpha] 1a and 69%[alpha] 1b sites with-log (Ki) values of 10.0+/-0.3 and 7.1+/-0.1, respectively, for (+)-niguldipine. However, these values were not different from those obtained from renal membranes of the normotensive Wistar-Kyoto (WKY) rats. These results indicate that in spite of the elevated blood pressure during the established phase of hypertension, the number, the affinity, and the ratio of the [alpha] 1a and [alpha] lb appear not to be responsible for the manifestation of hypertension during this phase.