Immunopharmacological studies on TBX, a new antiallergic drug. (3). Inhibitory effects on histamine release from lung fragments and bronchoconstriction in guinea pigs.
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- YANAGIHARA Yukiyoshi
- Clinical Research Center for Allergy, National Sagamihara Hospital
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- KASAI Hiroshi
- Research Laboratories, Tokyo Tanabe Pharmaceutical Co., Ltd.
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- MATSUI Shizuo
- Research Laboratories, Tokyo Tanabe Pharmaceutical Co., Ltd.
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- NINOMIYA Kenji
- Research Laboratories, Tokyo Tanabe Pharmaceutical Co., Ltd.
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The effects of 9-methyl-3-(lH-tetrazol-5-yl)-4H-pyrido[1, 2-a]pyrimidin-4-one potassium salt (TBX), a new antiallergic drug, on histamine release from lung fragments, experimental asthma and isolated tracheal muscle were investigated in guinea pigs. TBX (10-7 to 10-4 g/ml) dose-dependently inhibited antigen-induced histamine release from lung fragments of guinea pigs passively sensitized with homologous IgE serum. Antigen inhalation-induced experimental asthma in passively sensitized animals was inhibited in a dose-dependent fashion by i.v. (1 to 5 mg/kg) and p.o. (10 to 100 mg/kg) administrations of TBX. In vivo bronchoconstriction by platelet-activating factor (PAF, i.v.) was also inhibited by TBX (0.3 to 10 mg/kg, i.v.). However, high concentrations of TBX (more than 3 x 10-4 g/ml) were needed to inhibit PAF-induced platelet aggregation in vitro. With regard to the effect on isolated tracheal muscle, TBX itself at concentrations higher than 10-5 g/ml induced dose-dependent reduction in the resting tonus, which was not affected by pretreatment with propranolol. Neither the leukotriene D4-induced contraction nor the prostaglandin F2α-Induced one was specifically antagonized by TBX. The results obtained indicate that TBX is an antiasthmatic agent effective in inhibiting both IgE- and PAF-induced bronchoconstriction, possibly by interfering with mediator release.
収録刊行物
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- Jpn.J.Pharmacol.
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Jpn.J.Pharmacol. 51 (1), 83-92, 1989
公益社団法人 日本薬理学会
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詳細情報 詳細情報について
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- CRID
- 1390282679267681920
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- NII論文ID
- 130000832582
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- NII書誌ID
- AA00691188
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- COI
- 1:CAS:528:DyaL1MXls1KqtLk%3D
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- ISSN
- 13473506
- 00215198
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- PubMed
- 2478743
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- Crossref
- PubMed
- CiNii Articles
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- 使用不可