DCPIB

DCPIB is an inhibitor of volume-regulated anion channels (VRAC).¹ It inhibits the swelling-induced chloride current (I_Cl,swell) in bovine pulmonary artery endothelial cells (IC₅₀ = 4.1 µM). DCPIB inhibits the VRAC subunit leucine-rich containing 8A (LRRC8A; IC₅₀ = 20.9 µM) and inhibits sphingosine-1-phosphate-induced cGAMP uptake by LRRC8A in telomerase-immortalized human microvascular endothelial (TIME) cells when used at a concentration of 20 µM.^2,3 It also inhibits the two-pore domain potassium channels K_2P18.1/TRESK, K_2P3.1/TASK1, and K_2P9.1/TASK3 in COS-7 cells expressing the human channels (IC₅₀s = 0.14, 0.95, and 50.72 µM, respectively).⁴ DCPIB (10 µM) activates K_2P2.1/TREK1 and K_2P4.1/TRAAK channels in COS-7 cells expressing the human channels. Intracisternal administration of DCPIB (20 µg/kg) reduces infarct area and neurological deficit scores in a rat model of cerebral ischemia induced by middle cerebral artery occlusion (MCAO).⁵

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1. Decher, N., Lang, H.J., Nilius, B., et al. DCPIB is a novel selective blocker of ICl,swell and prevents swelling-induced shortening of guinea-pig atrial action potential duration. Br. J. Pharmacol. 134(7), 1467-1479 (2001).

2. Qiu, Z., Dubin, A.E., Mathur, J., et al. SWELL1, a plasma membrane protein, is an essential component of volume-regulated anion channel. Cell 157(2), 447-458 (2014).

3. Lahey, L.J., Mardjuki, R.E., Wen, X., et al. LRRC8A:C/E heteromeric channels are ubiquitous transporters of cGAMP. Mol. Cell. 80(4), 578-591 (2020).

4. Lv, J., Liang, Y., Zhang, S., et al. DCPIB, an inhibitor of volume-regulated anion channels, distinctly modulates K2P channels. ACS Chem. Neurosci. 10(6), 2786-2793 (2019).

5. Zhang, Y., Zhang, H., Feustel, P.J., et al. DCPIB, a specific inhibitor of volume regulated anion channels (VRACs), reduces infarct size in MCAo and the release of glutamate in the ischemic cortical penumbra. Exp. Neurol. 210(2), 514-520 (2008).