Journal of Pharmacobio-Dynamics
Online ISSN : 1881-1353
Print ISSN : 0386-846X
ISSN-L : 0386-846X
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
Takeshi NABEHiroshi HASHIIShigeki MATSUBARAKiyoshi YASUIHideki YAMAMURAMichiaki HORIBAShigekatsu WATANABE KOHNOKatsuya OHATA
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Keywords: histamine
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1992 Volume 15 Issue 12 Pages 673-679

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Abstract

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 B4 (i-LTB4) and i-LTC4 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.

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© The Pharmaceutical Society of Japan
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