Studies on a New Beta-adrenoceptor Blocker, 6-(2-Hydroxy-3-isopropylamino) propoxy Benzothiazole Succinate (KF-577)
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概要
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Beta-adrenoceptor blocking activity of a newly synthesized benzothiazole derivative, 6-(2-hydroxy-3-isopropylamino) propoxybenzothiazole succinate (KF-577) was investigated. In in vitro preparation of the guinea pig trachea and the atrium it was approximately 1/100 and 1/10 as potent as propranolol, respectively, in competitively blocking the betareceptors : some cardioselectivity was seen. Like propranolol, it is devoid of intrinsic beta-stimulating activity. In urethane-anesthetized rats KF-577 and propranolol both exhibited a pressor effect at lower doses, while at higher doses both caused a sharp fall in blood pressure. The depressor and positive chronotropic effects of isoproterenol were both blocked by either KF-577 or propranolol. Mechanisms of this pressor effect were explored using vagotomized, adrenalectomized, reserpinized rats, and the results were subjected to discussion. KF-577 had a surface anesthetic potency 1/20 that of propranolol (guinea pig cornea) and a conduction anesthetic potency comparable to propranolol (frog sciatic nerve). KF-577 was thus shown to be a beta-adrenoceptor blocker having some selectivity.
- 社団法人日本薬学会の論文
- 1977-08-25
著者
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粕谷 豊
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Hoshi University
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渡辺 稔
Department of Toxicology and Pharmacology, Faculty of Pharmaceutical Sciences, The University of Tok
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粕谷 豊
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Hoshi University
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粕谷 豊
東京大学薬学部
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渡辺 稔
Department of Toxicology and Pharmacology, Faculty of Pharmaceutical Sciences, The University of Tokyo
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