Table 1. Functional properties of α-Ctx VnIB at various nAChR subtypes.
The antagonist properties of VnIB were determined at nAChRs expressed in Xenopus laevis oocytes by two-electrode voltage clamp (TEVC) electrophysiology as described in Materials and methods, section 2.3. Data is given as IC50 values and Hill slopes (nH) (with 95% confidence intervals in parentheses) and were obtained from recordings on at least three individual oocytes. r, rat; h, human; ND, not determined.
| nAChR | IC50 (nM) | nH |
|---|---|---|
| rα6β4 | 12 (9.9–15) | 1.2 (0.95–1.5) |
| rα6/α3β4 | 18 (16–20) | 1.1 (0.97–1.2) |
| rα3β4 | 320 (250–390) | 1.2 (0.96–1.5) |
| rα6/α3β2β3 | 4000 (2500–6900) | 0.53 (0.42–0.66) |
| hα1β1δε | >10,000 | ND |
| rα2β2 | >10,000 | ND |
| rα2β4 | >10,000 | ND |
| rα3β2 | >10,000 | ND |
| rα4β2 | >10,000 | ND |
| rα4β4 | >10,000 | ND |
| rα7 | >10,000 | ND |
| rα9α10 | >10,000 | ND |
| hα6/α3β4 | 5.3 (4.1–6.9) | 1.1 (0.84–1.5) |
| hα3β4 | >10,000 | ND |
| hα6/α3β2β3 | >10,000 | ND |
| hα4β2 | >10,000 | ND |