Studies on a new antiallergic pyridinecarboxamide TA-5707F and its sodium salt (TA-5707) I. Inhibition of IGE-induced passive cutaneous anaphylaxis (PCA) in rats.
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概要
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Effects of TA-5707F [6-methyl-<I>N</I>-(1<I>H</I>-tetrazol-5-yl)-2-pyridinecarboxamide] and its sodium salt (TA-5707) on IgE-induced homologous PCA in rats were investigated. 1. Both TA-5707 and TA-5707F were found to be orally effective inhibitors of rat PCA. Maximum activity by oral administration was obtained when they were administered 5 min before the challenge. Their ID50's under these conditions were both approximately 1 mg/kg. Administration 5 min after the challenge was no longer effective. 2. TA-5707 was also effective by intravenous administration, and its I D50, <I>ca</I>. 0.1 mg/kg, was less than that of disodium cromoglycate (DSCG). 3. The PCA-inhibitory activity of TA-5707 was not affected by adrenalectomy and adrenomedullectomy. 4. Daily administration of TA-5707 or TA-5707F for 8 days did not induce drug tolerance. 5. Tachyphylaxis and cross -tachyphylaxis were observed when the PCA-inhibitory activities of TA-5707 and DSCG were tested after intravenous pretreatment with a large dose (<I>ca</I>. 30 times the ID50) of either drug, but not after oral pretreatment with a therapeutic dose of TA-5707 or TA-5707F.
- 公益社団法人 日本薬理学会の論文
著者
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TAKEYAMA SHIGEYUKI
Biological Research Laboratory, Tanabe Seiyaku Co., Ltd.
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TSUZURAHARA Kei
Biological Research Laboratory and Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.
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ISHIKAWA Setsuko
Biological Research Laboratory and Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.
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MURATA Takashi
Biological Research Laboratory and Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.
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DATE Tadamasa
Biological Research Laboratory and Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.
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TAKEYAMA Shigeyuki
Biological Research Laboratory and Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.
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