A. Hirashima et al., Identification of novel inhibitors of calling and in vitro [C-14]acetate incorporation by pheromone glands of Plodia interpunctella, PEST MAN SC, 57(8), 2001, pp. 713-720
Some octopamine agonists were found to suppress in vitro biosynthesis of th
e calling pheromone of the Indian meal moth, Plodia interpunctella. Isolate
d pheromone-gland preparations incorporated Sodium [C-14]acetate at a linea
r rate for 3h when incubated with the pheromone biosynthesis activating neu
ropeptide (PBAN). This incorporation was dependent on the dose of PBAN (up
to 0.5 muM). Thin-layer chromatography of a pheromone-gland extract reveale
d quantitative incorporation of radioactivity into a product exhibiting the
same mobility as (Z,E)-9,12-tetradecadienyl acetate, the main component of
the calling pheromone of P interpunctella. Twenty-seven octopamine agonist
s were initially screened using a calling behaviour bioassay of female P in
terpunctella. Four derivatives with activity in the nanomolar range were id
entified which were, in order of decreasing pheromonostatic activity: 2-(2,
6-diethylphenylimino)thiazolidine > 2-(2,6-diethylphenylimino)oxazolidine >
2-(2,6-dimethylphenylimino)thiazolidine > 2-(2-ethylphenylimino)oxazolidin
e. These compounds also showed in vitro inhibitory activity in intracellula
r de novo pheromone biosynthesis. The results of the present study indicate
that these derivatives could provide useful information in the characteriz
ation and differentiation of octopaminergic receptor types and subtypes. (C
) 2001 Society of Chemical Industry.