A Tiaramide Derivative, 5-Chloro-3-(4-hydroxypiperadinocarbonylmethyl) benzothiazoline-2-one (HPR-611), a Potent Inhibitor of Anaphylactic Chemical Mediator Release-A Distinctive Feature from Disodium Cromoglycate
スポンサーリンク
概要
- 論文の詳細を見る
Effects of a tiaramide derivative, 5 chloro-3-(4-hydroxypiperadinocarbonylmethyl) benzothiazoline-2-one (HPR-611), on anaphylactic chemical mediator release from rat peritoneal exudate cells (RPEC), guinea pig lung fragments (GPLF) and human lung fragments (HLF) were investigated in comparison with those of tiaramide and disodium cromoglycate (DSCG). HPR-611 at 10^<-6>-10^<-4> g/ml showed a concentration-dependent inhibition of the histamine release from RPEC regardless of its pretreatment time. Tiaramide also inhibited the release with slightly less potency than HPR-611. The treatment of DSCG 1 min before antigen challenge markedly prevented the release but the inhibitory potency was clearly deteriorated by prolongation of the pretreatment time. Tiaramide tended to influence the anaphylactic release of histamine from GPLF with only 20% inhibition of the release at either 10^<-5> or 10^<-4> g/ml, whereas HPR-611 at 10^<-5> and 10^<-4> g/ml significantly suppressed the release in a concentration-dependent fashion. DSCG was not effective on that even at higher concentrations. Anaphylactic release of not only histamine but also immunoreactive leukotriene B_4 (i-LTB_4) and i-LTC_4 from HLF was markedly inhibited by 10^<-8>-10^<-4> g/ml of HPR-611. Tiaramide inhibited the release to a somewhat less extent than HPR-611,while nominal or no inhibitions by DSCG were found. From these results, it is clearly apparent that anti-allergic actions of HPR-611 are quite different from those of DSCG.
- 公益社団法人日本薬学会の論文
著者
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Yamamura H
Department Of Pharmacology Kyoto Pharmaceutical University
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Ohata Katsuya
Department Of Pharmacology Kyoto Pharmaceutical University:department Of Pneumology Ogaki Municipal
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Horiba Michiaki
Department Of Pharmacology Kyoto Pharmaceutical University:department Of Pneumology Ogaki Municipal
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MATSUBARA Shigeki
Department of Obstetrics and Gynecology, Jichi Medical University School of Medicine
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Matsubara Shigeki
Department Of Obstetrics And Gynecology Jichi Medical School
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NABE Takeshi
Department of Pharmacology, Kyoto Pharmaceutical University
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YAMAMURA Hideki
Department of Pharmacology, Kyoto Pharmaceutical University
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Yasui Kiyoshi
Department of Paediatrics, Yokohama City University Medical Center
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Yamamura H
Kyoto Pharmaceytical Univ. Kyoto Jpn
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Matsubara Shigeki
Department Of Pharmacology Kyoto Pharmaceutical University:department Of Pneumology Ogaki Municipal
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Nabe Takeshi
Department Of Pharmacology Kyoto Pharmaceutical University
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HASHII Hiroshi
Department of Pharmacology, Kyoto Pharmaceutical University
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WATANABE KOHNO
Department of Pharmacology, Kyoto Pharmaceutical University
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Watanabe Kohno
Department Of Pharmacology Kyoto Pharmaceutical University:department Of Pneumology Ogaki Municipal
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Hashii Hiroshi
Department Of Pharmacology Kyoto Pharmaceutical University:department Of Pneumology Ogaki Municipal
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Yasui K
Department Of Pharmacology Kyoto Pharmaceutical University:department Of Pneumology Ogaki Municipal
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Yasui Kiyoshi
Department Of Molecular Genetics National Institute Of Genetics
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Yamamura Hideki
Department Of Anatomy Hiroshima University School Of Medicine
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Yamamura Hisao
Department Of Molecular And Cellular Pharmacology Graduate School Of Pharmaceutical Sciences Nagoya
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Yamamura Hisao
Department Of Molecular And Cellular Pharmacology Graduate School Of Pharmaceutical Sciences Nagoya
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Yamamura H
Kyoto Pharmaceutical Univ. Kyoto Jpn
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Matsubara Shigeki
Department Of Obstetrics And Gynecology And Jichi Perinatal Education Center
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Horiba Michiaki
Department Of Pharmacology Kyoto Pharmaceutical University:department Of Pneumology Ogaki Municipal
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Nabe T
Department Of Pharmacology Kyoto Pharmaceutical University
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