Table 1 α-Conotoxins that inhibit α3β4 nAChR.

From: Structural mechanisms for α-conotoxin activity at the human α3β4 nicotinic acetylcholine receptor

α-conotoxin

Sequence

nAChR selectivity (nM)

Ref.

LsIA

SGCCSNPACRVNNPNIC *

α7(10.1) ≥ α3β2 (10.3), α3β4 (inactive)

23

RegIIA

-GCCSHPACNVNNPHIC *

α3β2(33) > α3β4(97) > α7(103) > α4β2(>1,000) > α9α10(1,000)

24

Mr 1.1

-GCCSHPACSVNNPDIC *

α3β2 (61%) > α7 (~55%) > α3β4 (40%)#

32

PeIA

-GCCSHPACAGNNQHIC *

α9α10 (6.9) > α3β2 (23) > α3β4 (480) > α7 (1,800) > α4β2 (11,600)

27

GIC

-GCCSHPACAGNNQHIC *

α3β2 (1.1) > α4β2 (309) > α3β4 (775)

28

BuIA

-GCCSTPPCAVLY—C *

α6/α3β2 (0.26) > α6/α3β4 (1.54) > α3β2 (5.72) > > α3β4 (27.7) > α4β4 (69.9) > α2β4 (121) > α7 (272) > α2β2 (800) > α4β2 (10,400).

26

AuIB

-GCCSYPPCFATNPD-C *

α3β4 (750) > α7, α4β4, α3β2, α4β2, α2β2, α2β4 (>1,000)

29

TxID

-GCCSHPVCSAMSP-IC *

α3β4 (12.5) > α6α3β4 (94.1) > α2β4 (4,550) > α4β4, α4β2, α6/α3β32β3, α3β2, α2β2,α9α10, α7 (>10,000)

30

TP-2212–59

-GCCSHPBCFBZY—C *

α3β4 (2.3) > α7 (>1,000), α3β2 (1,000)

31

  1. B is 2-aminobutyric acid (Abu), Z is norvaline (Nva), and (*) indicates C-terminal amidation. #Authors do not report an IC50 instead report % inhibition of Ach-evoked currents.
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