文章基本信息

标题：Alterations of Binding Characteristics of α1-, β1-Adrenoceptors and Ca2+ Binding Sites in the Myocardium of Spontaneously Hypertensive Rats (SHR) by Chronically Administered Bunazosin, Atenolol, Ketanserin and Verapamil
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作者：Kenichi WATANABE ; Akira SHIBATA ; Hiroyuki WAKABAYASHI 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1993
卷号：16
期号：5
页码：480-482
DOI：10.1248/bpb.16.480
出版社：The Pharmaceutical Society of Japan
摘要：The effects of chronic treatment with bunazosin, atenolol, ketanserin and verapamil on the myocardium of the spontaneously hypertensive rat (SHR) were examined by the radioligand binding assay method using [³H]prazosin, [<125>I]iodocyanopindolol and [³H]nitrendipine binding to α₁- and β₁-adrenergic receptors and Ca²⁺ binding sites. The norepinephrine concentration in the rat myocardium was also determined. (1) All of these drugs lowered the elevated blood pressure of the SHR. (2) Only ketanserin administration increased the K_d value of the α₁-adrenoceptor in the SHR. (3) Administration of atenolol and ketanserin to the SHR decreased the B_max value of the β₁-adrenoceptor. (4) Verapamil, bunazosin and atenolol also lowered the B_max values of the Ca²⁺ binding sites of SHRs. (5) All drugs except for atenolol lowered the norepinephrine concentration in the myocardium of the SHR. These findings suggest that the SHR has an abnormality of the α₁ and β₁-adrenoceptors and Ca²⁺ binding site of the myocardium, that the drugs had a beneficial effect on these receptors, that the drugs could also lower the high norepinephrine content in the myocardium of the SHR and that some of these drugs also affected the binding characteristics of other types of membrane receptors.
关键词：alpha1-adrenoceptor;beta1-adrenoceptor;calcium ion binding site;norepinephrine;spontaneously hypertensive rat (SHR);adrenergic blocking agent