Antitussive effect of RU-20201 - Central and peripheral actions.

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概要

• 論文の詳細を見る

• The antitussive effect of the new compound 1, 2, 3, 4a, 9b-hexahydro-8, 9b-dimethyl-4-[3-(4-methyl-piperazine-1-yl) propionamide] dibenzofuran-3-one dihydrochloride (RU-20201) was investigated in dogs and guinea pigs, including its sites of action. The antitussive effect of RU-20201 was about 1/10 as potent as that of codeine phosphate in dogs with the puncture electrode-induced cough (PEC) method and about 1/12 and 1/4 as potent as that of codeine phosphate in guinea pigs with the PEC and chemical stimulation methods, respectively. When RU-20201 was administered in a dose range of 1 to 10 mg into the vertebral artery toward the brain in lightly anesthetized dogs, no antitussive effect was observed against the coughing elicited by electrical stimulation of the central cut end of the superior laryngeal nerve. However, a stimulative effect on respiration, especially on respiratory rate occurred. The peripheral effect of RU-20201 on the cough was investigated using the <I>in situ</I> upper trachea perfusion preparation which allows a direct drug administration to the local site around the tracheal mucosa, this site being electrically stimulated to induce coughing. A close i.a. infusion of RU-20201 in doses of 1 and 3 mg/min into the tracheal vascular bed for 5 min inhibited the cough response elicited by mucosal stimulation. The above findings suggest that RU-20201 has a significant antitussive activity, the site of action being probably, at least, at the cough receptor level.

• 公益社団法人 日本薬理学会の論文

著者

• MISAWA Miwa

  Department of Pharmacology, School of Pharmacy, Hoshi University

• Misawa Miwa

  Department Of Applied Pharmacology Hoshi University

• Kamei Junzo

  Department Of Pathophysilology & Therapeutics Faculty Of Pharmaceutical Sciences Hoshi Universit

• Yanaura Saizo

  Department Of Applied Pharmacology School Of Pharmacy Hoshi University

• Hosokawa Tomokazu

  Department of Medicinal Plant Science, Hoshi University

• KITAGAWA Harumi

  Department of Pharmacology, Hoshi College of Pharmacy

• KITAGAWA Harumi

  Department of Pharmacology, School of Pharmacy, Hoshi University

• FUJIKURA Hideaki

  Department of Pharmacology, School of Pharmacy, Hoshi University

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