2-Aminoethyl diphenylborinate (2-APB) is a modulator of intracellular calcium levels and transient receptor potential (TRP) channels.
1,2 It inhibits calcium release induced by inositol-1,4,5-triphosphate (IP
3) in rat cerebellar microsomes (IC
50 = 42 μM) without affecting IP
3 binding to its receptor.
1 2-APB inhibits store-operated calcium entry (SOCE) in DT40 cells (IC
50 = 4.8 μM), as well as inhibits TRP canonical 6 (TRPC6) and TRP melastatin 8 (TRPM8) and activates TRP vanilloid 1 (TRPV1), TRPV2, and TRPV3
in vitro.
2,3 It also inhibits calcium transients induced by the sarcoplasmic/endoplasmic reticulum Ca
2+-ATPase (SERCA) inhibitor thapsigargin (Item No.
10522) in DDT1 MF-2 cells when used at a concentration of 75 μM.
1 2-APB inhibits differentiation of primary mouse brown adipocytes when used at concentrations ranging from 30 to 300 μM and reduces adipocyte triglyceride levels at 100 μM.
4 It also increases the expression of
Ucp1 and
Pparg in primary mouse brown adipocytes. 2-APB (10 mg/kg) reduces protein levels of TRP melastatin 2 (TRPM2) in the rat hippocampus and improves learning and memory deficits induced by amyloid-β (25-35) in rats.
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