BHQ is a selective inhibitor of sarco-endoplasmic reticulum Ca2+-ATPase (SERCA).
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The importance of the Ca2+-ATPases of the surface and endoplasmic reticulum membranes in regulating the intracellular Ca2+ concentrations in living cells has been recognized as a result of the development of biophysical techniques and finding of useful pharmacological tool drugs[1]. BHQ is a potent and selective inhibitor of the sarco-endoplasmic reticulum Ca2+-ATPase (SERCA). In rat tail artery myocytes, BHQ reduced ICa(L) in a concentration- and voltage-dependent manner with an IC50 of 66.7 μM[2]. In rat basophilic leukaemia (RBL-2H3) cells under whole cell voltage clamp, a maximal blockade of inward current was obtained within 6 min after perfusion with 10 μM BHQ which caused depolarization of the cell which would affect Ca2+ influx[3].
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