A modulator of intracellular calcium levels and TRP channels
2-APB is an antagonist of Ins(1,4,5) P3-induced Ca2+ release with IC50 value of 42 μM [1].
Myo-Ins(1,4,5) P3 receptors (IP3R) mediates the mobilization of internal Ca2+. IP3R is involved in Ca2+ waves and Ca2+ oscillations.
2-APB is an antagonist of Ins(1,4,5) P3-induced Ca2+ release. 2APB inhibited Ins(1,4,5)-P3-induced Ca2+ release from rat cerebellar microsomal with IC50 value of 42 μM. Addition of 2APB to the extracellular inhibited the cytosolic Ca2+ rise in human platelets and neutrophils stimulated by thrombin. Also, 2APB inhibited the contraction of thoracic aorta induced by angiotensin II (AII) [1]. In HEK-293 cells, 2-APB in the extracellular blocked human TRPC5 channels with IC50 value of 20 μM. Also, 2-APB blocked TRPC6 and TRPM3. In cells overexpressing TRPC5, 2-APB inhibited cell proliferation [2]. In the mouse pancreatic acinar cell, 2-APB significantly inhibited store-operated Ca2+ (SOC)-mediated Ca2+ entry at low concentrations. In permeabilized acinar cell, 2-APB inhibited direct stimulation of Ca2+ release and InsP3-induced Ca2+ release at high concentrations [3].
In rats with I/R-induced testicular injury, 2-APB significantly increased superoxide dismutase (SOD), total antioxidant capacity (TAC) and glutathione (GSH) and reduced malondialdehyde (MDA) and DNA fragmentation, which suggested the antiapoptotic and antioxidative effects of 2-APB [4].
2-APB是一种Ins(1,4,5)P3受体拮抗剂，其IC50值为42μM[1]。
肌醇(1,4,5)三磷酸受体（IP3R）介导内部Ca2+的释放。IP3R参与了Ca2+波和Ca2+振荡。
2-APB是Ins(1,4,5)P3诱导的Ca2+释放的拮抗剂。2-APB抑制了大鼠小脑微粒体中Ins(1,4,5)P3诱导的Ca2+释放，其IC50值为42μM。在血小板和中性粒细胞中，2-APB的加入可抑制血栓素诱导的细胞内Ca2+升高。此外，2-APB还可抑制血管紧张素II(AII)诱导的主动脉收缩[1]。在HEK-293细胞中，2-APB在胞外能够阻断人类TRPC5通道，其IC50值为20μM。此外，2-APB还可阻断TRPC6和TRPM3。在过表达TRPC5的细胞中，2-APB抑制了细胞增殖[2]。在小鼠胰腺腺泡细胞中，2-APB显著抑制了低浓度下存储诱导的Ca2+进入，而在高浓度下抑制了直接的Ca2+释放和InsP3诱导的Ca2+释放[3]。
在I/R诱导的睾丸损伤的大鼠中，2-APB显著增加了超氧化物歧化酶(SOD)、总抗氧化能力(TAC)和谷胱甘肽(GSH)，并减少了丙二醛(MDA)和DNA断裂，这表明2-APB具有抗凋亡和抗氧化作用[4]。
参考文献:
[1].? Maruyama T, Kanaji T, Nakade S, et al. 2APB, 2-aminoethoxydiphenyl borate, a membrane-penetrable modulator of Ins(1,4,5)P3-induced Ca2+ release. J Biochem, 1997, 122(3): 498-505.
[2].? Xu SZ, Zeng F, Boulay G, et al. Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect. Br J Pharmacol, 2005, 145(4): 405-414.
[3].? Choi KJ, Kim KS, Kim SH, et al. Caffeine and 2-Aminoethoxydiphenyl Borate (2-APB) Have Different Ability to Inhibit Intracellular Calcium Mobilization in Pancreatic Acinar Cell. Korean J Physiol Pharmacol, 2010, 14(2): 105-111.
[4].? Sari E, Aksit H, Erken HA, et al. Protective effect of 2-APB on testicular ischemia-reperfusion injury in rats. J Urol, 2015, 193(3): 1036-1041.
动态评分
0.0