Beta-receptor blocking potencies of the three newly synthesized .BETA.-adrenergic antagonists (S-596,K-351,N-696) as assessed with the radioligand binding assay method in rat cardiac muscle membrane treated with neuraminidase.
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概要
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To assess the β-blocking potencies of three newly synthesized β-blockers, i.e., S-596: dl-2 (3'-t-butylamino-2'-hydroxypropylthio)-4-(5'-carbamoyl-2'-thienyl)-thiazole hydrochloride, K-351: 3, 4-dihydro-8-(2-hydroxy-3-isopropyl-aminopropoxy)-3-nitroxy-2H-1-benzopyran, and N-696: 4, 3-(tert-butylamino)-2-hydroxypropoxy)-N-methylisocarbostyril hydrochloride, values of K<SUB>i</SUB> (inhibition constant) were obtained by the radioligand binding assay method using rat heart membrane treated with neuraminidase. The pA<SUB>2</SUB> values of these blockers as antagonists against the positive chronotropic and inotropic actions of isoproterenol were also determined by pharmacological methods using guinea pig atria. To assess the selectivity of these β-blockers, pA<SUB>2</SUB> values were also obtained in the isolated trachea using isoproterenol as an agonist. The order of potencies as assessed by K<SUB>i</SUB> and pA<SUB>2</SUB> values were S-596>K-351>N-696. When the K<SUB>i</SUB> values were plotted against the pA<SUB>2</SUB> values together with the K<SUB>i</SUB> and pA<SUB>2</SUB> values of our previous study (Horii et al., 1974; Nakazawa et al., 1978; Nakagawa et al., 1980; Nakagawa et al., 1983; Nagatomo et al., 1983), straight lines were obtained with r values of 0.93 (P<0.001) (positive chronotropic action) and 0.91 (P<0.001) (positive inotropic action), respectively. Thus, the validity of using the β-adrenoceptor binding assay method developed in this laboratory using cardiac membrane treated with neuraminidase for assessment of the potencies of β-adrenoceptor blockers in cardiac muscle was further substantiated.
- 公益社団法人 日本薬理学会の論文
著者
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Imai Shoichi
Department Of Phamacology Niigata University School Of Medicine
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Nagatomo Takafumi
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
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SASAKI Miyuki
Department of Pharmacology, Niigata College of Pharmacy
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Nakagawa Yoshito
Department Of Pharmacology Niigata University School Of Medicine
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Tsuchihashi Hiroshi
Department Of Pharmacology Niigata College Of Pharmacy
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NAKAHARA Hajime
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Kyoto University
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