Ethacrynic acid inhibition of histamine release from rat mast cells: effect on cellular ATP levels and thiol groups.
The experiments concerned the effect of ethacrynic acid (0.5 mM) on the adenosine triphosphate (ATP) content of rat mast cells and the effect on histamine release induced by the ionophore A23187 (10 microM). Ethacrynic acid decreased the ATP level of the cells in presence of antimycin A and glucose as well as in presence of 2-deoxyglucose. A23187-induced histamine release was inhibited by ethacrynic acid, and this inhibition was completely reversed by dithiothreitol. These observations may indicate that ethacrynic acid inhibits glycolytic and respiratory energy production in rat mast cells. Furthermore, the inhibition of histamine release occurred mainly through interaction with thiol groups, although inhibition of cellular energy production may have been an additional mechanism.
D000255:Adenosine Triphosphate / Q000032:analysis*; D000818:Animals; D000001:Calcimycin / Q000037:antagonists & inhibitors; D002470:Cell Survival / Q000187:drug effects; D004229:Dithiothreitol / Q000494:pharmacology; D004976:Ethacrynic Acid / Q000494:pharmacology*; D006636:Histamine Release / Q000187:drug effects*; D008297:Male; D008407:Mast Cells / Q000032:analysis / Q000187:drug effects* / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D013438:Sulfhydryl Compounds / Q000378:metabolism*
D013438:Sulfhydryl Compounds; D000001:Calcimycin; D000255:Adenosine Triphosphate; D004976:Ethacrynic Acid; D004229:Dithiothreitol