Table 4.
Ligand-gated ionotropic receptors modulated by zinc.
| Receptor Type | Subtype or Subunit | Ligand | [Zn2+] (EC50 or IC50) |
|---|---|---|---|
| GABAergic | GABAρ1 (NM) | GABA 1 µM [98], GABA 3 µM [99] | 21.9 µM (1 min PI) [98], 20.4 µM [99] |
| GABAα1β2γ2 (NM) | GABA 3 µM [99] | 441.3 µM [99] | |
| GABAA (NM) | GABA (WC) [96], GABA 50 µM [97] | N.D. [96], 7.3 µM [97] | |
| Glycinergic | GlyRα1 (PM/NM) | Glycine 50 µM [22] | 80 nM (PM); 546 µM (NM) [22] |
| Cholinergic | α7 (NM) | Acetylcholine 3 µM [101] | 27 µM [101] |
| α2β2 (PM/NM) | Acetylcholine 3 µM [100] | 13 µM (PM); 52 µM (NM) [100] | |
| α2β4 (PM/NM) | Acetylcholine 3 µM [100] | 45 µM (PM); 590 µM (NM) [100] | |
| α3β2 (NM) | Acetylcholine 3 µM [100] | 97 µM [100] | |
| α3β4 (PM/NM) | Acetylcholine 3 µM [100] | 47 µM (PM); 3200 µM (NM) [100] | |
| α4β2 (PM/NM) | Acetylcholine 3 µM [100] | 16 µM (PM); 440 µM (NM) [100] | |
| α4β4 (PM/NM) | Acetylcholine 3 µM [100] | 22 µM (PM); 510 µM (NM) [100] | |
| Glutamatergic | NR1/NR2A (NM) | Glutamate 100 µM [104] | 5 nM (HAS); 79 µM (LAS) [104] |
| NR1/NR2B (NM) | Glutamate 100 µM [104] | 9.5 µM [104] | |
| GluR6R (NM) | AMPA 30–300 µM [105] | 67 µM (5 min PI) [105] | |
| GluR6R/KA1 (NM) | AMPA 30–300 µM [105] | 1.5 µM (5 min PI) [105] | |
| GluR6R/KA2 (NM) | AMPA 30–300 µM [105] | 2.1 µM (5 min PI) [105] | |
| GluK3 (PM/NM) | Glutamate 10 mM [20] | 46 µM (PM); 100 µM (NM) [20] | |
| Serotoninergic | 5-HT3A (PM) | 5-HT 1 µM [103] | N.D. [103] |
| H+ergic | ASIC2a (PM) | pH 5 [23] | 120 µM [23] |
| ASIC1a (NM) | pH 6.5 [32] | 7.0 nM [32] | |
| ASIC1a-ASIC2a (NM) | pH 6.0 [32] | 10.04 nM pH 6.5 [32] | |
| Na+ergic | ENaC αβγ (PM/NM) | Na+ 110 mM [24,106] | 1.74 µM [106], 2.1 µM [24] (PM); N.D. [107], 2.1 mM [24] (NM) |
| Purinergic | P2X1 (NM) | ATP 0.3 µM [108] | 9.34 µM, 0.82 µM (20 min PI), 1.1 µM (40 min PI) [108] |
| P2X2 (PM/NM) | ATP (WC) [109], 3 µM [110], 5 µM [25], 2 µM [26], 50 µM [111] |
N.D. [25,109], 9.3 µM, 6.1 µM (5 min PI) [110], 7.9 µM [26], 19.6 µM [111] (PM); N.D. (>30 µM, 5 min PI) [110] (NM) |
|
| P2X3 (PM/NM) | ATP 0.3 µM [108] | 10.9 µM (20 min PI), N.D. (<20 µM, 40 min PI) (PM); N.D. (>20 µM, 20 and 40 min PI) (NM) [108] |
|
| P2X4 (PM/NM) | ATP 5 µM [111,112], 3 µM [113], 1 µM 25 µM [68] |
N.D. (<10 µM) [112], 2.4 µM [111], 1.9 µM (0 and 15 min PI) [113], 2.4 µM, 4.9 µM (20 s PI) [68] (PM); N.D. (>100 µM) [112], N.D. (>30 µM, 0 and 15 min PI) [113] (NM) |
|
| P2X5 (PM/NM) | ATP 300 nM [114] | 42.6 µM ( 0 and 15 min PI) (PM); N.D. (0 and 15 min PI) (NM) [114] |
|
| P2X7 (NM) | BzATP 30 µM [33,115], ATP 600 µM [34] |
11.2 µM [115], 78 µM (10 s PI) [34], 4.6 µM [33] | |
| TRP | TRPM2 (NM) | ADPR [117] | N.D. [117] |
| TRPM5 (NM) | Intracellular Ca2+ 500 nM [118] | 4.3 µM [118] | |
| TRPA1 (A) | – | 2.3 µM [120] | |
| Hemichannels | Hemi-gap-junction channels (NM) | 0 Ca2+ [119] | 37 µM [119] |
PM, positive modulator; NM, negative modulator; A, activator; HAS, high affinity site; LAS, low affinity site; WC, without concentration; PI, preincubation; EC50 or IC50 refers to median excitatory or inhibitory concentration, respectively.