Table 1.
Neuronal voltage-gated sodium channels (VGSC) subtype selectivity and potency of μ-conotoxins.
| μ-Conotoxins | Conus species | Number of residues | VGSC subtypes (IC50) | References |
|---|---|---|---|---|
| KIIIA | C. kinoshitai | 16 | Nav1.3 (8 μM), | [100,101] |
| Nav1.7 (100–290 nM) | ||||
| SIIIA*/B | C. striatus | 20/20 | Nav1.3 (11 μM (SIIIA)), | [103,104,105] |
| Nav1.7 (65 μM (SIIIA)), | ||||
| Nav1.8 (insensitive to 10 μM) | ||||
| PIIIA | C. purpurascens | 22 | Nav1.3 (3.2 μM), | [96,106,107] |
| Nav1.7 (3.1–6.2 μM) | ||||
| GIIIA/B/C | C. geographus | 22/22/22 | N.D. | |
| CnIIIA/B/C | C. consors | 22/25/22 | Nav1.3 (11 μM (CnIIIA)), | [98,107,108] |
| Nav1.7 (489 nM (CnIIIC)) | ||||
| Nav1.8 (insensitive to 1 μM (CnIIIC)) | ||||
| CIIIA | C. catus | 22 | N.D. | |
| SmIIIA | C. stercusmuscarum | 22 | Nav1.3 (40 nM), | [97] |
| Nav1.7 (1.3 μM) | ||||
| MIIIA | C. magus | 22 | Nav1.3 (7.7 nM), | [107] |
| Nav1.7 (97 μM) | ||||
| SxIIIA/B | C. striolatus | 22/23 | N.D. | |
| BuIIIA/B/C | C. bullatus | 23/24/26 | Nav1.3 (350 nM (BuIIIA); 200 nM (BuIIIB)) | [107] |
| TIIIA | C. tulipa | 22 | Nav1.3 (50 nM), | [107] |
| Nav1.7 (insensitive to 3 μM) | ||||
| Nav1.8 (insensitive to 3 μM) |
N.D., not determined. *commercial name PEG-SIIIA; entered pre-clinical trial for inflammatory pain (i.v.) [109].