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Mechanism of action of MY-1250, an active metabolite of Repirinast, in inhibiting histamine release from rat mast cells.
Br J Pharmacol. 1992 Mar; 105(3):587-90.BJ

Abstract

1. When MY-1250 (3.6 x 10(-5) M) was added to mast cells, it caused a rapid increase in adenosine 3':5'-cyclic monophosphate (cyclic AMP) and decrease in adenosine 5'-triphosphate (ATP), both of which recovered to their original levels within 2 min. The accumulation of cyclic AMP was maximal at 20 s after challenge with MY-1250. The minimum level of ATP was observed at 20 s after addition of MY-1250. 2. The initial rise in [Ca2+]i and the histamine release induced by DNP-AS antigen (40 micrograms ml-1) was most strongly inhibited at 20 s after incubation of the mast cells with MY-1250. 3. MY-1250 strongly and dose-dependently inhibited the histamine release from rat mast cells induced by antigen. Moreover, MY-125 strongly inhibited calcium ion mobilization from the intracellular Ca(2+)-store. 4. These results suggested that the inhibitory mechanism of MY-1250 on the initial rise in [Ca2+]i and histamine release induced by antigen was due to the inhibition of ATP-dependent Ca(2+)-release from the intracellular Ca(2+)-stores.

Authors+Show Affiliations

Department of Pharmacology, Tokushima Bunri University, Japan.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

1378339

Citation

Takei, M, et al. "Mechanism of Action of MY-1250, an Active Metabolite of Repirinast, in Inhibiting Histamine Release From Rat Mast Cells." British Journal of Pharmacology, vol. 105, no. 3, 1992, pp. 587-90.
Takei M, Endo K, Takahashi K. Mechanism of action of MY-1250, an active metabolite of Repirinast, in inhibiting histamine release from rat mast cells. Br J Pharmacol. 1992;105(3):587-90.
Takei, M., Endo, K., & Takahashi, K. (1992). Mechanism of action of MY-1250, an active metabolite of Repirinast, in inhibiting histamine release from rat mast cells. British Journal of Pharmacology, 105(3), 587-90.
Takei M, Endo K, Takahashi K. Mechanism of Action of MY-1250, an Active Metabolite of Repirinast, in Inhibiting Histamine Release From Rat Mast Cells. Br J Pharmacol. 1992;105(3):587-90. PubMed PMID: 1378339.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Mechanism of action of MY-1250, an active metabolite of Repirinast, in inhibiting histamine release from rat mast cells. AU - Takei,M, AU - Endo,K, AU - Takahashi,K, PY - 1992/3/1/pubmed PY - 1992/3/1/medline PY - 1992/3/1/entrez SP - 587 EP - 90 JF - British journal of pharmacology JO - Br J Pharmacol VL - 105 IS - 3 N2 - 1. When MY-1250 (3.6 x 10(-5) M) was added to mast cells, it caused a rapid increase in adenosine 3':5'-cyclic monophosphate (cyclic AMP) and decrease in adenosine 5'-triphosphate (ATP), both of which recovered to their original levels within 2 min. The accumulation of cyclic AMP was maximal at 20 s after challenge with MY-1250. The minimum level of ATP was observed at 20 s after addition of MY-1250. 2. The initial rise in [Ca2+]i and the histamine release induced by DNP-AS antigen (40 micrograms ml-1) was most strongly inhibited at 20 s after incubation of the mast cells with MY-1250. 3. MY-1250 strongly and dose-dependently inhibited the histamine release from rat mast cells induced by antigen. Moreover, MY-125 strongly inhibited calcium ion mobilization from the intracellular Ca(2+)-store. 4. These results suggested that the inhibitory mechanism of MY-1250 on the initial rise in [Ca2+]i and histamine release induced by antigen was due to the inhibition of ATP-dependent Ca(2+)-release from the intracellular Ca(2+)-stores. SN - 0007-1188 UR - https://www.unboundmedicine.com/medline/citation/1378339/Mechanism_of_action_of_MY_1250_an_active_metabolite_of_Repirinast_in_inhibiting_histamine_release_from_rat_mast_cells_ L2 - https://onlinelibrary.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0007-1188&date=1992&volume=105&issue=3&spage=587 DB - PRIME DP - Unbound Medicine ER -