TABLE 1

IC50 and maximum inhibition of nicotine-stimulated [3H]DA release for toxins used in this study

All subunits used to form receptors in oocytes were from rat clones. α6/α3β2β3 subtype is composed of an α6/α3 chimera, which contains the extracellular region of α6 and the remaining portion of the α3 subunit. α-MII is the only toxin that does not distinguish between α3* and α6* nAChRs. For each toxin, the IC50 for [3H]DA release closely resembles that for inhibition of heterlogously expressed α6* nAChRs. The substituted residues in the α-MII analogs are underlined.


Toxin

Sequence

IC50 Oocytes

Ki α-MII Sites

IC50 [3H]DA Release (95% CI)

% Maximum Inhibition


α3β2
α6/a3β2β3



nM
α-MII GCCSNPVCHLEHSNLC 2.18a (1.2-3.8) 0.39a (0.28-0.55) 0.22a (0.20-0.25) 1.04 (0.47-2.3) 25 ± 1.8
α-MII[L15A] GCCSNPVCHLEHSNAC 34.1a (19-60) 0.92a(0.65-1.3) 0.30a (0.21-0.45) 0.84 (0.26-2.8) 22 ± 2.4
α-MII[H9A] GCCSNPVCALEHSNLC 59a (44-79) 0.79a (0.56-1.1) 1.1a (0.84-1.6) 1.25 (0.32-4.9) 21 ± 1.8
α-MII[E11A] GCCSNPVCHLAHSNLC 8.7a (6.8-11.1) 0.16a (0.13-0.19) 0.27a (0.19-0.37) 0.025 (0.010-0.061) 32 ± 3.5
α-PIA
RDPCCSNPVCTVHNPQIC
74.2b (49-110)
0.95b (0.71-1.3)
Not tested
1.48 (0.25-8.7)
26 ± 3.3
  • CI, confidence interval.

  • a Taken from McIntosh et al. (2004).

  • b Taken from Dowell et al. (2003).