Investigations of the antifeedant mode of action of azadirachtin and f
our synthetic analogues, 22,23-dihydroazadirachtin, 3-tigloylazadirach
tol, 11-methoxydihydroazadirachtin and 22,23-bromoethoxydihydroazadira
chtin have revealed that both polyphagous and oligophagous insects are
behaviourally responsive to azadirachtin, with the most responsive sp
ecies being able to differentiate extremely small changes in the paren
t molecule. In Lepidoptera the antifeedant response is correlated also
with increased neural activity of the chemoreceptors. When locusts ar
e treated on crop plants, the antifeedant and physiological actions of
azadirachtin and analogues work in concert and result in feeding dete
rrence, growth and moulting aberrations and mortality with the same or
der of potency as for antifeedancy. Specific binding studies using [H-
3]dihydroazadirachtin carried out on locust testes and Spodoptera Sf9
cells have shown that the competitive binding of the different analogu
es of azadirachtin to these binding sites occurs in a similar order of
potency to that found with antifeedant and IGR bioassays. This sugges
ts a causal link between specific binding to membrane proteins and the
ability of the molecule to exert biological effect. (C) 1998 Society
of Chemical Industry.