Table 2.
α‐Conotoxin Conus species |
Framework | aIC50 (nM) at recombinant nAChRs | bReference | |
---|---|---|---|---|
α3β2 | α3β4 | |||
ImI Conus imperialis |
4/3 |
40.8 (h) (Ellison et al., 2004) |
3390 (h) (Ellison et al., 2004) |
McIntosh et al., 1994 |
BuIA Conus bullatus |
4/4 | 5.72 | 27.7 | Azam et al., 2005 |
TP‐2212‐59 (synthetic) | 4/4 | >10 000 | 2.3 | Chang et al., 2014 |
AuIB Conus aulicus |
4/6 |
>10 000 (Luo et al., 1998) >30 000 (h) (Cuny et al., 2016) |
750 (Luo et al., 1998) >30 000 (h) (Cuny et al., 2016) |
Luo et al., 1998 |
TxID Conus textile |
4/6 | >10 000 | 12.5 | Luo et al., 2013 |
MII Conus magus |
4/7 |
1.7 (Dowell et al., 2003) |
>200 | Cartier et al., 1996 |
PIA Conus purpurascens |
4/7 | 74.2 | 518 | Dowell et al., 2003 |
RegIIA Conus regius |
4/7 |
33 (Franco et al., 2012) 132.4 (h) (Cuny et al., 2016) |
97 (Franco et al., 2012) 45.6 (h) (Cuny et al., 2016) |
Franco et al., 2012 |
GIC Conus geographus |
4/7 | 1.1 (h) | 755 (h) | McIntosh et al., 2002 |
GID C. geographus |
4/7 | 3.1 | >10 000 | Nicke et al., 2003 |
PnIA (synthetic)c |
4/7 |
9.56 (Luo et al., 1999) |
>1000 (Everhart et al., 2003) |
Fainzilber et al., 1994 |
LsIA Conus limpusi |
4/7 | 10 | >1000 | Inserra et al., 2013 |
LvIA Conus lividus |
4/7 |
8.67 17.5 (h) |
148 | Luo et al., 2014 |
Most α‐conotoxins listed were tested on a range of nAChR subtypes; however, only IC50 values for subtypes covered in this review are shown. For full details see the cited references.
If not indicated otherwise, IC50 values were obtained at rat nAChRs. References to individual values indicate the publication in which the data were reported. h, human.
Reference in which the α‐conotoxin was first described.
IC50 values were obtained with the synthetic analogue PnIA[sTy15Y], which is commonly referred to as PnIA, albeit amino acid 15 differs from native PnIA of Conus pennaceus.