TABLE 1.
Effects of inhibitors on swelling-induced ATP release from TM5 cells.
| Target Pathway | Drug (Concentration in μM) | Inhibition % ± SE % (wells) |
|---|---|---|
| PX1 | PRO (100) | 36.5 ± 1.6 (378)* |
| MFQ (0.03) | 24.3 ± 2.4 (100)* | |
| CBX (3) | 36.0 ± 3.8 (21)* | |
| CBX (30) | 53.6 ± 1.9 (192)* | |
| DTT (10,000) | 26.4 ± 1.2 (102)* | |
| DTT (10,000) + PRO (100) | 39.9 ± 2.0 (96)* | |
| DTT (10,000) + CBX (30) | 53.0 ± 1.4 (120)* | |
| CBX (30) + MFQ (0.03) | 51.6 ± 3.3 (54)* | |
| Cx | HEP (1,000) | 44.4 ± 2.9 (53)* |
| NFA (30) | 29.3 ± 3.1 (54)* | |
| External Ca2+ (2,500) | 36.1 ± 6.9 (72)* | |
| PX1+Cx | CBX (30) + HEP (1,000) | 80.4 ± 5.3 (54)* |
| DTT (10,000) + HEP (1,000) | 69.4 ± 0.9 (94)* | |
| P2RX7 | KN-62 (1) | 32.7 ± 2.6 (124)* |
| BBG (0.5) | 31.6 ± 3.1 (54)* | |
| A438079 (3) | 29.2 ± 4.0 (50)* | |
| PX1+Cx+P2RX7 | CBX (30) + HEP (1,000) + KN62 (1) | 96.2 ± 0.6 (56)* |
| CFTR | GLY (100) | 2.9 ± 3.8 (54) |
| VSOR and VSAC | DIDS (200) | 4.1 ± 5.5 (144) |
| DCPIB (10) | 9.0 ± 3.1 (96) | |
| Ca/CaMKII | LAC (1) | 5.8 ± 5.4 (54) |
| Vesicular Release | MON (100) | −9.1 ± 3.1 (54) |
| BAF (2) | 3.9 ± 3.8 (36) | |
| Maxi-anion channels | Gd3+ (50) | 3.1 ± 3.5 (54) |
| SITS (100) | 2.4 ± 3.1 (72) | |
| P-glycoprotein | VER (100) | 0.9 ± 3.0 (88) |
Note: Numbers in parentheses indicate numbers of wells measured. The inhibitors are grouped according to their putative major targets: pannexin-1 (PX1) hemichannels, connexin (Cx) hemichannels, P2X7 ionotropic ATP receptors (P2RX7), cystic fibrosis transmembrane conductance regulator (CFTR), volume-sensitive outwardly-rectifying chloride channel (VSOR), volume-sensitive anion channel (VSAC), and calcium/calmodulin-dependent protein kinase II (Ca/CaMKII). Positive and negative values indicate inhibition and stimulation, respectively. PRO, probenecid; MFQ, mefloquine; CBX, carbenoxolone; DTT, dithiothreitol; HEP, heptanol; NFA, niflumic acid; BBG, brilliant blue G; BAF: bafilomycin A1; Gd3+, gadolinium; GLY, glybenclamide; VER, verapamil; LAC, lavendustin C; MON, monensin.
P<0.001 vs hypotonicity controls.