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±０．３２ｎｍｏｌ·ｇ－１蛋白质明显下降至０．３３±０．０８ｎｍｏｌ·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．
The distribution of α 1 adrenoceptor(α 1 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 pA 2 values of α 1 AR selective antagonists, 5 methylurapidil, WB4101, naftopidil, (+) niguldipine and BMY7378, for antagonizing PE induced prostate contraction had a high correlative association with the pK i values for cloned bovine α 1A AR (r=0.91). In the radioligand binding assay, the maximal binding capacity of [ 125 I]BE and α 1 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 α 1A , α 1B and α 1D AR was approximately 15%, 65% and 20%. These results indicate that the functional α 1 AR subtype inducing prostatic muscle contraction is α 1A AR although there are three subtypes in rat prostate.
出处
《中国药理学与毒理学杂志》
CAS
CSCD
北大核心
1997年第4期253-256,共4页
Chinese Journal of Pharmacology and Toxicology
基金
国家自然科学基金
美国中华医学基金
关键词
前列腺
肾上腺素受体
亚型
α1-AR
receptor,adrenergic,alpha
receptor subtypes
adrenergic receptor blockaders
rats
prostate
