Table 1.
Evidence for different activation mechanisms of Panx1 channels
Activation mechanism and stimulationModel systemElectrophysiologyATP releaseDye permeationReference
Pressure or stretch      
Negative pressure (∼40 mbar) Recombinant PANX1 in Xenopus oocytes Single-channel recording; inhibitor NA NA NA Bao et al., 2004  
Pressure Native PANX1 in human erythrocytes Single-channel recording; inhibitor NA NA NA Locovei et al., 2006a  
Stretch (15 or 30 cmH2O) Native Panx1 in rat bladders NA CBX (100 µM); BB FCF (100 µM) NA Beckel et al., 2015  
Hypotonicity Native PANX1 in human erythrocytes NA CBX (100 µM) Inhibitor NA Locovei et al., 2006a  
Hypotonicity Native PANX1 in human bronchial epithelial cells NA CBX (10 µM); 10Panx1 (30 µM) CBX (10 µM); 10Panx1 (30 µM) Seminario-Vidal et al., 2011  
Hypotonicity Native PANX1 in A549 cells NA PANX1 siRNA PANX1 siRNA Seminario-Vidal et al., 2011  
Hypotonicity Native Panx1 in mouse tracheas NA Panx1−/− Panx1−/− Seminario-Vidal et al., 2011  
Hypotonicity Native PANX1 in CN-LM1A and MDA-LM2 cellsa NA CBX (500 µM)b NA Furlow et al., 2015  
Hypotonicity and 75 mM extracellular K+ Native Panx1 in mouse erythrocytes NA Probenecid (1 mM); Panx1−/−±probenecid Panx1−/− Qiu et al., 2011  
Extracellular K+      
20∼150 mM K+ Recombinant Panx1 in Xenopus oocytes Whole-cell current; CBX (100 µM); probenecid (1 mM) CBX (100 µM); probenecid (100 or 500 µM) NA Silverman et al., 2009; Wang et al., 2014  
150 mM K+ Recombinant Panx1 in Xenopus oocytes Single-channel recording; inhibitor NA CBX (100 µM) NA Wang et al., 2014  
? mM K+ Recombinant Panx1 in Xenopus oocytes NA BB FCF (10 µM) NA Wang et al., 2013  
50 mM K+ Native PANX1 in 1321N1 cells NA NA Panx1 shRNA Silverman et al., 2009  
10 mM K+ Native Panx1 in mouse hippocampal slides NA Mefloquine (100 nM); Panx1−/− Mefloquine (100 nM); Panx1−/− Santiago et al., 2011  
10 mM K+ Native Panx1 in mouse astrocytes Whole-cell current; Panx1−/− Panx1−/− Panx1−/− Suadicani et al., 2012  
75 mM extracellular K+ and hypotonicity Native Panx1 in mouse erythrocytes NA Probenecid (1 mM); Panx1−/−±probenecid Panx1−/− Qiu et al., 2011  
Intracellular Ca2+      
Ca2+ (0.1 µM∼10 mM) Recombinant PANX1 in Xenopus oocytes Inside-out macropatch; single-channel recording; inhibitor NA NA NA Locovei et al., 2006b  
A23187 (200 µM) Recombinant Panx1 in Xenopus oocytes Whole-cell current; inhibitor NA NA NA Locovei et al., 2006b  
Ionomycin (10 µM) Recombinant PANX1 in N2A cells NA NA Inhibitor NA Kurtenbach et al., 2013  
Thrombin (30 nM) Native PANX1 in A549 cells NA CBX (10 µM); BAPTA-AM (20 µM); thapsigargin (1 µM) CBX (10 µM); BAPTA-AM (20 µM) Seminario-Vidal et al., 2009  
Thrombin (1 or 1,000 U/ml) Native PANX1 in HUVECs NA CBX (5 µM); PANX1 shRNA; BAPTA-AM (5 µM) NA Gödecke et al., 2012  
Caffeine (concentration NA) Recombinant Panx1 in rat atrial myocytes Single-channel recording; CBX (20 µM); probenecid (200 µM) NA NA Kienitz et al., 2011  
SFK-mediated phosphorylation      
NMDA (100 µM) Native Panx1 in rat hippocampal neurons Whole-cell current; CBX (50 µM); 10Panx1 (100 µM); Panx1 shRNA NA CBX (50 µM); 10Panx1 (100 µM) Thompson et al., 2008; Weilinger et al., 2016  
Anoxia Native Panx1 in rat CA1 neurons Whole-cell current; 10Panx1 (100 µM)±APV (50 µM); probenecid (500 µM); brain-specific Panx1−/−; TAT-Panx305-318 peptide (1 or 10 µM) NA NA Weilinger et al., 2012  
TNFα (10 ng/ml) Native PANX1 in HUVECs NA CBX (50 µM); 10Panx1 (200 µM); Panx1 siRNA; endothelial cell–specific Panx1−/− 10Panx1 (200 µM) Lohman et al., 2015  
TNFα (50 ng/ml) Native Panx1 in mouse venous endothelia NA Endothelial cell–specific Panx1−/− NA Lohman et al., 2015  
BzATP (50 or 300 µM) Native Panx1 in J774 cells Whole-cell current; CBX (50 µM); mefloquine (100 nM); Panx1 siRNA NA CBX (50 µM); mefloquine (10 nM); Panx1 siRNA Iglesias et al., 2008  
BzATP (300 µM) Recombinant Panx1 in Xenopus oocytes Whole-cell current; inhibitor NA NA Inhibitor NA Iglesias et al., 2008  
BzATP (300 µM) Native Panx1 in peritoneal macrophage from A/J mice NA NA CBX (10 µM); 10Panx1 (300 µM) Sorge et al., 2012  
BzATP (300 µM) Native Panx1 in mouse astrocytes Whole-cell current; CBX (50 µM); mefloquine (100 nM); Panx1−/− Panx1−/− Panx1−/− Suadicani et al., 2012  
C-tail cleavage      
Anti-Fas (5 µg/ml) Native PANX1 in Jurkat cells Whole-cell current; CBX (10∼500 µM); probenecid (10 µM∼2 mM); CBX (100 µM)+PANX1 siRNA CBX (500 µM)c; probenecid (2 mM); PANX1 siRNA PANX1 siRNA; CBX (500 µM) Chekeni et al., 2010  
Anti-Fas (5 µg/ml) Native Panx1 in mouse thymocytes NA NA CBX (500 µM) Chekeni et al., 2010  
Anti-Fas (5 µg/ml) Recombinant PANX1 in Jurkat cells Whole-cell current; caspase site-deficient PANX1; CBX (100 µM) Caspase site-deficient PANX1 Caspase site-deficient PANX1 Chekeni et al., 2010  
Anti-Fas (5 µg/ml) Native Panx1 in mouse thymocytes NA NA Panx1−/− Qu et al., 2011  
Dexamethasone (0.5 µM) Native Panx1 in mouse thymocytes NA Panx1−/− NA Qu et al., 2011  
C-tail truncationc Recombinant PANX1 in Jurkat cells Whole-cell current; CBX (100 µM) NA Inhibitor NA Chekeni et al., 2010  
Caspase 3 Native PANX1 in Jurkat cells; Recombinant PANX1 in HEK293T cells Inside-out macropatch; Single-channel recording; CBX (50 µM) NA NA Sandilos et al., 2012; Chiu et al., 2017  
TEV proteased Recombinant PANX1 in HEK293T cells Whole-cell current; Inside-out macropatch; CBX (50 µM) NA Inhibitor NA Sandilos et al., 2012  
LPS (50 ng/ml) Native Panx1 in bone marrow–derived macrophage NA CBX (50 µM); probenecid (100 µM); trovafloxacin (100 µM); Panx1−/− NA Yang et al., 2015  
LPS (50 ng/ml) Recombinant Panx1 in bone marrow–derived macrophage NA Panx1−/− with Panx1-D378A NA Yang et al., 2015  
Activation mechanism and stimulationModel systemElectrophysiologyATP releaseDye permeationReference
Pressure or stretch      
Negative pressure (∼40 mbar) Recombinant PANX1 in Xenopus oocytes Single-channel recording; inhibitor NA NA NA Bao et al., 2004  
Pressure Native PANX1 in human erythrocytes Single-channel recording; inhibitor NA NA NA Locovei et al., 2006a  
Stretch (15 or 30 cmH2O) Native Panx1 in rat bladders NA CBX (100 µM); BB FCF (100 µM) NA Beckel et al., 2015  
Hypotonicity Native PANX1 in human erythrocytes NA CBX (100 µM) Inhibitor NA Locovei et al., 2006a  
Hypotonicity Native PANX1 in human bronchial epithelial cells NA CBX (10 µM); 10Panx1 (30 µM) CBX (10 µM); 10Panx1 (30 µM) Seminario-Vidal et al., 2011  
Hypotonicity Native PANX1 in A549 cells NA PANX1 siRNA PANX1 siRNA Seminario-Vidal et al., 2011  
Hypotonicity Native Panx1 in mouse tracheas NA Panx1−/− Panx1−/− Seminario-Vidal et al., 2011  
Hypotonicity Native PANX1 in CN-LM1A and MDA-LM2 cellsa NA CBX (500 µM)b NA Furlow et al., 2015  
Hypotonicity and 75 mM extracellular K+ Native Panx1 in mouse erythrocytes NA Probenecid (1 mM); Panx1−/−±probenecid Panx1−/− Qiu et al., 2011  
Extracellular K+      
20∼150 mM K+ Recombinant Panx1 in Xenopus oocytes Whole-cell current; CBX (100 µM); probenecid (1 mM) CBX (100 µM); probenecid (100 or 500 µM) NA Silverman et al., 2009; Wang et al., 2014  
150 mM K+ Recombinant Panx1 in Xenopus oocytes Single-channel recording; inhibitor NA CBX (100 µM) NA Wang et al., 2014  
? mM K+ Recombinant Panx1 in Xenopus oocytes NA BB FCF (10 µM) NA Wang et al., 2013  
50 mM K+ Native PANX1 in 1321N1 cells NA NA Panx1 shRNA Silverman et al., 2009  
10 mM K+ Native Panx1 in mouse hippocampal slides NA Mefloquine (100 nM); Panx1−/− Mefloquine (100 nM); Panx1−/− Santiago et al., 2011  
10 mM K+ Native Panx1 in mouse astrocytes Whole-cell current; Panx1−/− Panx1−/− Panx1−/− Suadicani et al., 2012  
75 mM extracellular K+ and hypotonicity Native Panx1 in mouse erythrocytes NA Probenecid (1 mM); Panx1−/−±probenecid Panx1−/− Qiu et al., 2011  
Intracellular Ca2+      
Ca2+ (0.1 µM∼10 mM) Recombinant PANX1 in Xenopus oocytes Inside-out macropatch; single-channel recording; inhibitor NA NA NA Locovei et al., 2006b  
A23187 (200 µM) Recombinant Panx1 in Xenopus oocytes Whole-cell current; inhibitor NA NA NA Locovei et al., 2006b  
Ionomycin (10 µM) Recombinant PANX1 in N2A cells NA NA Inhibitor NA Kurtenbach et al., 2013  
Thrombin (30 nM) Native PANX1 in A549 cells NA CBX (10 µM); BAPTA-AM (20 µM); thapsigargin (1 µM) CBX (10 µM); BAPTA-AM (20 µM) Seminario-Vidal et al., 2009  
Thrombin (1 or 1,000 U/ml) Native PANX1 in HUVECs NA CBX (5 µM); PANX1 shRNA; BAPTA-AM (5 µM) NA Gödecke et al., 2012  
Caffeine (concentration NA) Recombinant Panx1 in rat atrial myocytes Single-channel recording; CBX (20 µM); probenecid (200 µM) NA NA Kienitz et al., 2011  
SFK-mediated phosphorylation      
NMDA (100 µM) Native Panx1 in rat hippocampal neurons Whole-cell current; CBX (50 µM); 10Panx1 (100 µM); Panx1 shRNA NA CBX (50 µM); 10Panx1 (100 µM) Thompson et al., 2008; Weilinger et al., 2016  
Anoxia Native Panx1 in rat CA1 neurons Whole-cell current; 10Panx1 (100 µM)±APV (50 µM); probenecid (500 µM); brain-specific Panx1−/−; TAT-Panx305-318 peptide (1 or 10 µM) NA NA Weilinger et al., 2012  
TNFα (10 ng/ml) Native PANX1 in HUVECs NA CBX (50 µM); 10Panx1 (200 µM); Panx1 siRNA; endothelial cell–specific Panx1−/− 10Panx1 (200 µM) Lohman et al., 2015  
TNFα (50 ng/ml) Native Panx1 in mouse venous endothelia NA Endothelial cell–specific Panx1−/− NA Lohman et al., 2015  
BzATP (50 or 300 µM) Native Panx1 in J774 cells Whole-cell current; CBX (50 µM); mefloquine (100 nM); Panx1 siRNA NA CBX (50 µM); mefloquine (10 nM); Panx1 siRNA Iglesias et al., 2008  
BzATP (300 µM) Recombinant Panx1 in Xenopus oocytes Whole-cell current; inhibitor NA NA Inhibitor NA Iglesias et al., 2008  
BzATP (300 µM) Native Panx1 in peritoneal macrophage from A/J mice NA NA CBX (10 µM); 10Panx1 (300 µM) Sorge et al., 2012  
BzATP (300 µM) Native Panx1 in mouse astrocytes Whole-cell current; CBX (50 µM); mefloquine (100 nM); Panx1−/− Panx1−/− Panx1−/− Suadicani et al., 2012  
C-tail cleavage      
Anti-Fas (5 µg/ml) Native PANX1 in Jurkat cells Whole-cell current; CBX (10∼500 µM); probenecid (10 µM∼2 mM); CBX (100 µM)+PANX1 siRNA CBX (500 µM)c; probenecid (2 mM); PANX1 siRNA PANX1 siRNA; CBX (500 µM) Chekeni et al., 2010  
Anti-Fas (5 µg/ml) Native Panx1 in mouse thymocytes NA NA CBX (500 µM) Chekeni et al., 2010  
Anti-Fas (5 µg/ml) Recombinant PANX1 in Jurkat cells Whole-cell current; caspase site-deficient PANX1; CBX (100 µM) Caspase site-deficient PANX1 Caspase site-deficient PANX1 Chekeni et al., 2010  
Anti-Fas (5 µg/ml) Native Panx1 in mouse thymocytes NA NA Panx1−/− Qu et al., 2011  
Dexamethasone (0.5 µM) Native Panx1 in mouse thymocytes NA Panx1−/− NA Qu et al., 2011  
C-tail truncationc Recombinant PANX1 in Jurkat cells Whole-cell current; CBX (100 µM) NA Inhibitor NA Chekeni et al., 2010  
Caspase 3 Native PANX1 in Jurkat cells; Recombinant PANX1 in HEK293T cells Inside-out macropatch; Single-channel recording; CBX (50 µM) NA NA Sandilos et al., 2012; Chiu et al., 2017  
TEV proteased Recombinant PANX1 in HEK293T cells Whole-cell current; Inside-out macropatch; CBX (50 µM) NA Inhibitor NA Sandilos et al., 2012  
LPS (50 ng/ml) Native Panx1 in bone marrow–derived macrophage NA CBX (50 µM); probenecid (100 µM); trovafloxacin (100 µM); Panx1−/− NA Yang et al., 2015  
LPS (50 ng/ml) Recombinant Panx1 in bone marrow–derived macrophage NA Panx1−/− with Panx1-D378A NA Yang et al., 2015  

NA, data not available or unknown.

a

The cells endogenously express both wild-type and a truncated form of PANX1, which only expresses amino acid 1-89 of PANX1.

b

High concentration of CBX is required for inhibition of ATP release if albumin is present in the assay system (Chekeni et al., 2010).

c

A C-terminal truncated PANX1 (amino acid 1-371) was used in the study.

d

This study used a mutant human PANX1, with its caspase cleavage site replaced by a TEV protease cleavage site.

or Create an Account

Close Modal
Close Modal