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Mechanism of action of MY-1250, a main metabolite of repirinast (MY-5116), in inhibiting histamine release from rat, mast cells

We have previously reported that MY-1250, a main metabolite of reprinast (MY-5116), markedly inhibited antigen induced histamine release from rat peritoneal exudate cel is with IC50 value of 4.9×10^-8 g/ml. In the present study we investigatesssub investigated the effect of MY-1250 or phophohorylati...

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Bibliographic Details
Published in:Japanese Journal of Pharmacology 1988, Vol.46 (suppl), p.62-62
Main Authors: Noboru Yamada, Kazuo Suzuki, Shuichiro Kadowaki, Kazuo Takahashi, Susumu Mizogami
Format: Article
Language:Japanese
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Summary:We have previously reported that MY-1250, a main metabolite of reprinast (MY-5116), markedly inhibited antigen induced histamine release from rat peritoneal exudate cel is with IC50 value of 4.9×10^-8 g/ml. In the present study we investigatesssub investigated the effect of MY-1250 or phophohorylation of a mast cell protein. Incubation of purified rat mast, cel Is with MY-1250 in the presence of radioactive phosphate result eesluted in a rapid phosphory1ation of 78K-dalton protein, which had been previously reported in the case of DSCG. Dibutyry-cGMP also induced phosphorylation of this protein, but dibutyryl cAMP did not. Phosphorylation occureder manner at more than 10^-6 g/ml of MY-1250 and dephosphorylation occured by continuous treatment with MY-1250, which is consistent with the tachyphylaxis observed in the inhibition of histamine release. These findings suggest that phosphory1ation of 78K-dalton protein is much related to the inhibitory action of MY-1250 against histamine release from mast cells.
ISSN:0021-5198