TABLE 1

Effects of mutations within the two pyrethroid receptor sites on the action of DMT and PMT

Symbols ↓, ↑, and ≈ indicate decrease, increase, or insignificant change of the ligand potency, respectively.

PyR1PyR2
MutantRef.aDMTPMTMutantRef.aDMTPMT
L2k7F/I1↓/↓≈ /↑I1k7A3
M2k11T1V1k11A3
S1o2A5
L2o6I1L1o6I/A3,5↑/≈≈/↑
T2o10I1I1o10C3
L2o13F1T1o13W3
C2o14A1
V2i18G3L1i18G3
F2i22Sb5I1i22A5
L2i25A5I1i25A5
L2i26A5
S1i29A5
I3i12A2V2i12A/L5≈/↑↑/↑
F3i13C3I2i13M3
S3i15A2N2i15S5
F3i16A2L2i16F/S3↓/↓↓/↓
F3i17I4
N3i20A2N2i20A5
  • a References: 1 (Usherwood et al., 2007); 2 (Du et al., 2009); 3 (Du et al., 2013) and references therein; 4 (Tan et al., 2005); and 5, this study (Figs. 3B and 4).

  • b F2i22 contributes to both PyR1 and PyR2.