STUDIES ON MODE OF ANTAGONISM BETWEEN ADRENERGIC β-MIMETICS AND β-BLOCKING AGENTS (I). β-BLOCKING ACTION OF MESCALINE AND ITS DERIVATIVES
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概要
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In order to clarify whether or not trimetoquinol (TMQ) and isoproterenol (ISO) interact with the same receptor, the pA<SUB>2</SUB> values of propranolol (PR) and certain trimethoxybenzene derivatives were measured, using isolated guinea pig tracheal chains. Each of PR, mescaline (MES) and its derivatives gave almost the same pA<SUB>2</SUB> values for TMQ and ISO. Introduction of an alkyl group into the N atom of MES increased the affinity to the receptor in the order of methyl and isopropyl as well as the structure-activity relationship of catecholamines, while that of hydroxyl group in the β-position of the side chain decreased pA<SUB>2</SUB> values. The slopes of the regression lines for anti-TMQ action of MES derivatives as well as PR were almost one, but those for their anti-ISO action were less than 0.3. 3, 4, 5-Trimethoxyaniline and 3, 4, 5-trimethoxy-benzoic acid had little activity as β-blocking agents. These results suggest the possibility that TMQ and ISO would interact with the same receptor sites. The importance of the trimethoxybenzene and the phenethylamine moieties in the MES-derivatives for anti-TMQ action is discussed.
- 公益社団法人 日本薬理学会の論文
著者
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OHASHI Motoaki
Pharmacological Research Laboratory Tanabe Seiyaku Co., Ltd.
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Iwasawa Yoshio
Pharmacological Research Laboratory Tanabe Seiyaku Co. Ltd.
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KIYOMOTO Akio
Pharmacological Research Laboratory, Tanabe Seiyaku Co., Ltd.
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SAITO Seiichi
Organic Chemical Research Laboratory, Tanabe Seiyaku Co., Ltd.
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YAMAMURA Shiro
Organic Chemical Research Laboratory, Tanabe Seiyaku Co., Ltd.
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IWASAWA YOSHIO
Pharmacological Research Laboratory, Tanabe Seiyaku Co., Ltd.
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