| 大鼠前列腺α1-肾上腺素受体亚型分析 |
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| 引用本文： | 彭明强 张幼怡 吕志珍 薛兆英 韩启德. 大鼠前列腺α1-肾上腺素受体亚型分析[J]. 中国药理学与毒理学杂志, 1997, 11(4): 253-256 |
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| 作者姓名： | 彭明强 张幼怡 吕志珍 薛兆英 韩启德 |
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| 作者单位： | 北京医科大学第三医院血管医学研究所，北京医科大学泌尿外科研究所 |
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| 基金项目： | 国家自然科学基金,美国中华医学基金 |
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| 摘 要： | 用离体组织收缩功能实验和放射配体结合实验, 分析大鼠前列腺α1-肾上腺素受体(α1-AR)三种亚型的分布及其介导的收缩效应. 结果显示: 标本经用氯乙基可乐定(CEC)预处理后,去氧肾上腺素(PE)介导的最大收缩效应无明显下降, α1-AR亚型选择性拮抗剂5-MU, WB4101, 萘哌地尔, 尼古地平, BMY7378抑制PE介导前列腺收缩的pA2值与克隆α1A-AR亚型的Ki值呈高度相关(r=0.91). 在放射配体结合实验中, 标本经CEC预处理后, ［125I］BE与α1-AR的最大结合容量由1.09±0.32 nmol·g-1蛋白质明显下降至0.33±0.08 nmol·g-1蛋白质. α1A-, α1B- , α1D-AR密度分别约占总受体密度的15%, 65%和20%. 结果提示大鼠前列腺中尽管α1-AR三种亚型均有分布, 但引起平滑肌收缩的功能性α1-AR以α1A-AR为主.
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| 关 键 词： | 受体,肾上腺素,α 受体亚型 肾上腺素受体阻滞剂 大鼠 前列腺 |
| 收稿时间： | 1996-07-01 |
Analysis of α1-adrenoceptor subtypes on the rat prostate |
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| PENG Ming-Qiang, ZHANG You-Yi, LU Zhi-Zhen, XUE Zhao-Ying, HAN Qi-De. Analysis of α1-adrenoceptor subtypes on the rat prostate[J]. Chinese Journal of Pharmacology and Toxicology, 1997, 11(4): 253-256 |
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| Authors: | PENG Ming-Qiang ZHANG You-Yi LU Zhi-Zhen XUE Zhao-Ying HAN Qi-De |
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| Affiliation: | (Instititute of Vascular Medicine, Third Hospital, Beijing Medical University, Beijing 100083; 2. Institute of Urology, Beijing Medical University, Beijing 100034) |
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| Abstract: | The distribution of α1-adrenoceptor(α1- AR) subtypes and the functional role in Wistar rat prostates were studied by using functional experiment and radioligand binding assay. The results showed that the maximal contraction induced by phenylephrine (PE) was not decreased obviously after pretreatment with chloroethylclonidine (CEC). The pA2 values of α1-AR selective antagonists, 5-methylurapidil, WB4101, naftopidil, (+) niguldipine and BMY7378, for antagonizing PE-induced prostate contraction had a high correlative association with the p Ki values for cloned bovine α1A-AR (r=0.91). In the radioligand binding assay, the maximal binding capacity of ［125I］BE and α1-AR decreased obviously after pretreatment with CEC, which were 1.09±0.32 nmol·g-1 protein and 0.33±0.08 nmol·g-1 protein, respectively. The percentage of α1A-, α1B-and α1D-AR was approximately 15%, 65% and 20%. These results indicate that the functional α1-AR subtype inducing prostatic muscle contraction is α1A- AR although there are three subtypes in rat prostate. |
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| Keywords: | receptor adrenergic alpha receptor subtypes adrenergic receptor blockaders rats prostate |
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