| 19904006 |
Al-Mousa F, Michelangeli F: Commonly used ryanodine receptor activator, 4-chloro-m-cresol (4CmC), is also an inhibitor of SERCA Ca2+ pumps. Pharmacol Rep. 2009 Sep-Oct;61(5):838-42.
4-Chloro-m-cresol (4CmC) is an extensively used activator of ryanodine receptors (RyRs). Studies have shown that 4CmC, at a concentration of 1 mM, is sufficient to cause Ca (2+) release through RyRs. Here, we show that mM concentrations of 4CmC also inhibit the sarcoplasmic-endoplasmic reticulum Ca (2+)-ATPase (SERCA), (IC (50) 2-3mM) and cause Ca (2+) release. 4CmC also causes increased intracellular [Ca (2+)] levels in COS-7 cells, which lack functional RyRs. Thus, any increase in [Ca (2+)] levels associated with use of 4CmC (> or= 1mM) could lead to non-specific Ca (2+) changes due to SERCA inhibition rather than RyR activation. |
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