Different modes of inhibition of rat gastric mucosal 6-keto-PGF1.ALPHA. production by indomethacin, aspirin and aminopyrine.

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概要

• 論文の詳細を見る

• The actions of aminopyrine on rat gastric mucosal cyclooxygenase activity in vitro were investigated and compared with those of the cyclooxygenase inhibitors indomethacin and aspirin. Aminopyrine is a phenyl-pyrazolone derivative with potent analgesic and antipyretic properties, but is weakly ulcerogenic, while indomethacin and aspirin are known to cause considerable ulcerogenesis. Aminopyrine was less potent in its ability to inhibit cyclooxygenase activity. The inhibition by all three drugs decreased with an increase in the substrate concentration. Pre-incubation with the enzymes greatly increased the inhibitory action of indomethacin and aspirin, but only slightly increased that of aminopyrine. The inhibitory action of aminopyrine was reversible, whereas those of indomethacin and aspirin were irreversible. These findings are discussed in relation to the low incidence of gastrointestinal irritation caused by aminopyrine.

• 公益社団法人 日本薬理学会の論文

著者

• Shimizu Shin-ichiro

  Department Of Applied Physics Tokyo University Of Agriculture And Technology

• Nishikawa Takashige

  Department Of Applied Pharmacology Kagoshima University Graduate School Of Medical And Dental Scienc

• SHIMIZU Shin-ichiro

  Department of Pharmacology, Kagoshima University Dental School

• TOMORI Yuichi

  First Department of Oral and Maxillofacial Surgery, Kagoshima University Dental School

• YAMASHITA Sukehide

  First Department of Oral and Maxillofacial Surgery, Kagoshima University Dental School

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• Different modes of inhibition of rat gastric mucosal 6-keto-PGF1.ALPHA. production by indomethacin, aspirin and aminopyrine.

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