L-type calcium channel blockers at therapeutic concentrations are not linked to CRAC channels and heart failure
Gary S Bird1, Yu-Ping Lin2, Charles J Tucker3
1Molecular and Cellular Biology Laboratory, National Institute of Environmental Health Sciences, NIH, Research Triangle Park, NC, USA.
Abstract:
Amlodipine has been used as a front-line anti-hypertensive therapy for decades by virtue of blocking voltage-operated calcium channels with high affinity and specificity. Recently, the safety of amlodipine has been questioned, as it was reported to activate Ca2+ release-activated Ca2+ (CRAC) channels and increase the risk of heart failure. Here we show, using a variety of approaches, that amlodipine does not activate CRAC channels at therapeutic concentrations. Combined with our previous meta-analysis, our study should reassure physicians that amlodipine should continue to be prescribed for treating hypertension.
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