Target selectivity and efficacy of analgesic α-conotoxins administered systemically
| α-Conotoxins | Efficacy | nAChR selectivity | Nanomolar GABAB-Cav Activity | References |
|---|---|---|---|---|
| Vc1.1 | Partially reverses mechanical allodynia in several neuropathic models after intramuscular dosing. Escalating actions and recovery of nerve function. | α9α10 ≫ α6α3β2β3 > α6α3β4 > α3β4 ∼ α3β2 | Yes | Sandall et al., 2003; Satkunanathan et al., 2005; Vincler et al., 2006; Klimis et al., 2011 |
| CyclizedVc1.1 | Partially reverses mechanical allodynia in several neuropathic models after oral dosing. | Very weak α9α10 | Yes | Clark et al., 2010 |
| Vc1a | No reversal of allodynia in a neuropathic pain model. Recovery of nerve function retained | α9α10 ≫ α3β4 ∼ α3β2 | No | Nevin et al., 2007 |
| Rg1A | Partially reverses mechanical allodynia in several neuropathic models after intramuscular dosing. | α9α10 ≫ α7 ≫ α3β4 ∼ α3β2 | Yes | Vincler et al., 2006 |
| AuIB | Partially reverses mechanical allodynia in several neuropathic models after intramuscular dosing. | α3β4 > α3β2 ≫ α9α10 | Yes | Klimis et al., 2011 |
| MII | Partially reverses mechanical allodynia in several neuropathic models after intramuscular dosing. | α3β2 > α3β4 ≫ α9α10 | No | Klimis et al., 2011 |
| Lt14a | Acute thermal antinociception (hotplate test) after intraperitoneal administration. | Unkown but inhibits PC12 cell nAChR (α3- α5-, α7-, β2-, β3-, and β4-subunits) | Unknown | Sun et al., 2011 |