Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
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
渡辺 賢一柴田 昭若林 広行嶋田 健次土橋 洋史長友 孝文
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1993 年 16 巻 5 号 p. 480-482

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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 Kd value of the α1-adrenoceptor in the SHR. (3) Administration of atenolol and ketanserin to the SHR decreased the Bmax value of the β1-adrenoceptor. (4) Verapamil, bunazosin and atenolol also lowered the Bmax 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.

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