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Econazole Depleted Calcium Release-Activated Calcium (CRAC) Current Through Blockade of Voltage_Dependent Ca2+Channels

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Econazole is an azole antifungal agent which can block the calcium release-activated calcium (CRAC) current in human leukaemic T cell line. The phenomenon is also possible to occur in mast cell such as RBL-2H3 (rat basophilic leukemia) cells, a tumor analog of mast into the cells, a tumor analog of mast cells. In the study, we investigated effect of econazole on 45 Ca 2+ uptake into the cells in response to thaspigargin an ATP-dependent Ca 2+ (SERCA) inhibitor, by direct measurement of radiolabelled Ca 2+ uptake in cells. The mechanism underriying this effect of econazole was studied using molecular modelling. In present study, econazole inhibited 45Ca2+ influx into mast cells in absence of Mast cells inducer+ thapsigargin. Morever, econazole potently suppressed the 45Ca2+ influx thapsigarging. Moreover, econazole potently suppressed the 45Ca2+ influx thapsigargin. Moreover, econazole potently supprssed the 45Ca2+ influx induced by thapsigarging. It was supported that econazole also inhibited Ca2+-induced tracheal contraction. The increase of Ca2+ was stimulated by transigarging. It was supported that econazole alsoinibited Ca2+ influx induced by thapsigargin. It was supported that enconazole also inhibited Ca2+- induced tracheal contraction. The increase of Ca2+ was stimulated by the opening of voltage-dependent Ca2+ channels activated by KCI-induced membrane depolarization. Based on molecular docking study, score of interaction (equal to energy of intraction) of 3FGO, a man protein target on Ca2+-ATPase, ATPase, with netive lign, thapsigargin and enconazole were-76.941, -117.205, and -92. 277, respectively. The interaction of thapsigargin and Ca2+-ATPase was more stabel tahn this of econazole and Ca2+-ATPase. It suggests that it would be difficul for econazole to block the interaction of thapsigargin with Ca2+-Atpase to increase intracellular Ca2+involving the blokade of voltage-dependendent Ca2+channels, but not involving the Ca2+-ATPase pathway.

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Majalah Farmasi Indonesia:22(2)2011: 128-136:

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Yogyakarta : Fakultas Farmasi UGM., 2011

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English

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0126-1037

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