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MY-1250, a major metabolite of the anti-allergic drug repirinast, induces phosphorylation of a 78-kDa protein in rat mast cells.
Biochem Pharmacol. 1992 Sep 25; 44(6):1211-3.BP

Abstract

Repirinast (MY-5116; isoamyl 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano [3,2-c]quinoline-2-carboxylate) is an anti-allergic drug of demonstrated effectiveness for treating bronchial asthma in humans. MY-1250 (5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano [3,2-c]quinoline-2-carboxylic acid), the major active metabolite of repirinast, inhibits antigen-induced histamine release from sensitized rat peritoneal exudate cells (PEC). When purified rat mast cells were treated with MY-1250 (2.5 x 10(-5) M) for 1 min, phosphorylation of a specific mast cell protein of apparent molecular mass of 78 kDa was observed as previously reported for sodium cromoglycate (SCG). Phosphorylation of this protein induced by MY-1250 and SCG occurred in a concentration-dependent manner with IC50 values of 2.0 x 10(-7) and 1.4 x 10(-5) M, respectively. MY-1250 did not inhibit calcium ionophore A23187 (1 microgram/mL)-induced histamine release from rat PEC. In the presence of calcium ionophore A23187 (1 microgram/mL), phosphorylation of this protein induced by MY-1250 was not evident. In conclusion, MY-1250 induced phosphorylation of a 78-kDa protein in rat mast cells and MY-1250 may inhibit histamine release by regulating phosphorylation of this protein in rat mast cells.

Authors+Show Affiliations

Pharmaceuticals Laboratory, Mitsubishi Kasei Corporation, Yokohama, Japan.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

1358073

Citation

Yamada, N, et al. "MY-1250, a Major Metabolite of the Anti-allergic Drug Repirinast, Induces Phosphorylation of a 78-kDa Protein in Rat Mast Cells." Biochemical Pharmacology, vol. 44, no. 6, 1992, pp. 1211-3.
Yamada N, Kadowaki S, Takahashi K, et al. MY-1250, a major metabolite of the anti-allergic drug repirinast, induces phosphorylation of a 78-kDa protein in rat mast cells. Biochem Pharmacol. 1992;44(6):1211-3.
Yamada, N., Kadowaki, S., Takahashi, K., & Umezu, K. (1992). MY-1250, a major metabolite of the anti-allergic drug repirinast, induces phosphorylation of a 78-kDa protein in rat mast cells. Biochemical Pharmacology, 44(6), 1211-3.
Yamada N, et al. MY-1250, a Major Metabolite of the Anti-allergic Drug Repirinast, Induces Phosphorylation of a 78-kDa Protein in Rat Mast Cells. Biochem Pharmacol. 1992 Sep 25;44(6):1211-3. PubMed PMID: 1358073.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - MY-1250, a major metabolite of the anti-allergic drug repirinast, induces phosphorylation of a 78-kDa protein in rat mast cells. AU - Yamada,N, AU - Kadowaki,S, AU - Takahashi,K, AU - Umezu,K, PY - 1992/9/25/pubmed PY - 1992/9/25/medline PY - 1992/9/25/entrez SP - 1211 EP - 3 JF - Biochemical pharmacology JO - Biochem Pharmacol VL - 44 IS - 6 N2 - Repirinast (MY-5116; isoamyl 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano [3,2-c]quinoline-2-carboxylate) is an anti-allergic drug of demonstrated effectiveness for treating bronchial asthma in humans. MY-1250 (5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano [3,2-c]quinoline-2-carboxylic acid), the major active metabolite of repirinast, inhibits antigen-induced histamine release from sensitized rat peritoneal exudate cells (PEC). When purified rat mast cells were treated with MY-1250 (2.5 x 10(-5) M) for 1 min, phosphorylation of a specific mast cell protein of apparent molecular mass of 78 kDa was observed as previously reported for sodium cromoglycate (SCG). Phosphorylation of this protein induced by MY-1250 and SCG occurred in a concentration-dependent manner with IC50 values of 2.0 x 10(-7) and 1.4 x 10(-5) M, respectively. MY-1250 did not inhibit calcium ionophore A23187 (1 microgram/mL)-induced histamine release from rat PEC. In the presence of calcium ionophore A23187 (1 microgram/mL), phosphorylation of this protein induced by MY-1250 was not evident. In conclusion, MY-1250 induced phosphorylation of a 78-kDa protein in rat mast cells and MY-1250 may inhibit histamine release by regulating phosphorylation of this protein in rat mast cells. SN - 0006-2952 UR - https://www.unboundmedicine.com/medline/citation/1358073/MY_1250_a_major_metabolite_of_the_anti_allergic_drug_repirinast_induces_phosphorylation_of_a_78_kDa_protein_in_rat_mast_cells_ L2 - https://linkinghub.elsevier.com/retrieve/pii/0006-2952(92)90387-X DB - PRIME DP - Unbound Medicine ER -