BAPTA-AM

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Background

BAPTA-AM is a selective calcium chelator [1].
Ca2+ is one of the most ubiquitous and versatile intracellular signaling molecules that control numerous cellular processes such as neurotransmitter release, contraction of all muscle cell types and fertilization [4].
BAPTA-AM is a selective and membrane permeable calcium chelator. In the human leukemia cell lines HL-60 and U937, BAPTA/AM (10 μM) induced internucleosomal DNA cleavage and classic apoptotic morphology. Also, BAPTA/AM increased Ca2+ in intracellular and downregulated c-jun [1]. In bovine chromaffin cells, APTA-AM (50 μM) rapidly and reversibly inhibited Ca2+-activated K+ (I(KCa)) and voltage-gated K+ (I(K)) by 50% [2]. In HEK 293 cells, BAPTA-AM inhibited hERG (Kv11.1), hKv1.3 and hKv1.5 channels with IC50 values of 1.3, 1.45 and 1.23 μM respectively in a concentration dependent way, which was dependent on channel opening [3].
In swiss mice, BAPTA-AM inhibited locomotor stimulation produced by ethanol and reversed ethanol-induced hypnotic effects. In male C57BL/6J mice, BAPTA-AM reduced ethanol consumption in a dose-dependent way [4].

[1]. Grant S, Freemerman AJ, Gregory PC, et al. Induction of apoptotic DNA fragmentation and c-jun downregulation in human myeloid leukemia cells by the permeant Ca2+ chelator BAPTA/AM. Oncol Res, 1995, 7(7-8): 381-392.
[2]. Urbano FJ, Buño W. BAPTA-AM blocks both voltage-gated and Ca2+-activated K+ currents in cultured bovine chromaffin cells. Neuroreport, 1998, 9(15): 3403-3407.
[3]. Tang Q, Jin MW, Xiang JZ, et al. The membrane permeable calcium chelator BAPTA-AM directly blocks human ether a-go-go-related gene potassium channels stably expressed in HEK 293 cells. Biochem Pharmacol, 2007, 74(11): 1596-1607.
[4]. Baliño P, Monferrer L, Pastor R, et al. Intracellular calcium chelation with BAPTA-AM modulates ethanol-induced behavioral effects in mice. Exp Neurol, 2012, 234(2): 446-453.