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Identification of novel synthetic octopamine receptor agonists which inhibit moth sex pheromone production
Year:
1999
Authors :
Gileadi, Carina
;
.
Rafaeli, Ada
;
.
Volume :
65
Co-Authors:
Rafaeli, A., Department of Stored Products, Pheromone Research Lab., Volcani Centre, P.O. Box 6, Bet Dagan 50250, Israel
Gileadi, C., Department of Stored Products, Pheromone Research Lab., Volcani Centre, P.O. Box 6, Bet Dagan 50250, Israel
Hirashima, A., Div. Biorsrc. Bioenvironmental Sci., Graduate School, Kyushu University, Fukuoka 812-8581, Japan
Facilitators :
From page:
194
To page:
204
(
Total pages:
11
)
Abstract:
The present study was designed to identify specific and sensitive compounds which may act as specific inhibitors of pheromone biosynthesis in the moth Helicoverpa armigera using physiological bioassays and three-dimentional quantitative structure-activity relationship studies. Twenty-eight octopamine agonists were initially screened using an in vivo bioassay for pheromone production by female moths. Fourteen compounds were found to inhibit pheromone production in the moths to a level of 50% or more and were subsequently used in dose-response studies to determine ID50s. The dose-response studies were performed in vitro, analyzing the effect of these compounds on intracellular cAMP production as well as on the de novo pheromone biosynthesis. Six active derivatives, with activity in the nanomolar range, were identified with the following order of decreasing pheromonostatic activity: 2-(2, 6-dimethylanilino)imidazolide > 2-(2-methyl-4-chloroanilino)oxazolidine > clonidine > 2-(2,6-diethylanilino) thiazolidine > 2-(3,5-dichlorobenzylamino)-2-oxazoline > tolazoline. Six other compounds were less active, with ID50s in the micromolar range. The active compounds were utilized for the development of a predictive model using physicochemical parameters. The results of the present study indicate that these derivatives could provide useful information in the characterization and differentiation of octopaminergic receptor types and subtypes.
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More details
DOI :
10.1006/pest.1999.2446
Article number:
Affiliations:
Database:
Scopus
Publication Type:
article
;
.
Language:
English
Editors' remarks:
ID:
22973
Last updated date:
02/03/2022 17:27
Creation date:
16/04/2018 23:55
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Scientific Publication
Identification of novel synthetic octopamine receptor agonists which inhibit moth sex pheromone production
65
Rafaeli, A., Department of Stored Products, Pheromone Research Lab., Volcani Centre, P.O. Box 6, Bet Dagan 50250, Israel
Gileadi, C., Department of Stored Products, Pheromone Research Lab., Volcani Centre, P.O. Box 6, Bet Dagan 50250, Israel
Hirashima, A., Div. Biorsrc. Bioenvironmental Sci., Graduate School, Kyushu University, Fukuoka 812-8581, Japan
Identification of novel synthetic octopamine receptor agonists which inhibit moth sex pheromone production
The present study was designed to identify specific and sensitive compounds which may act as specific inhibitors of pheromone biosynthesis in the moth Helicoverpa armigera using physiological bioassays and three-dimentional quantitative structure-activity relationship studies. Twenty-eight octopamine agonists were initially screened using an in vivo bioassay for pheromone production by female moths. Fourteen compounds were found to inhibit pheromone production in the moths to a level of 50% or more and were subsequently used in dose-response studies to determine ID50s. The dose-response studies were performed in vitro, analyzing the effect of these compounds on intracellular cAMP production as well as on the de novo pheromone biosynthesis. Six active derivatives, with activity in the nanomolar range, were identified with the following order of decreasing pheromonostatic activity: 2-(2, 6-dimethylanilino)imidazolide > 2-(2-methyl-4-chloroanilino)oxazolidine > clonidine > 2-(2,6-diethylanilino) thiazolidine > 2-(3,5-dichlorobenzylamino)-2-oxazoline > tolazoline. Six other compounds were less active, with ID50s in the micromolar range. The active compounds were utilized for the development of a predictive model using physicochemical parameters. The results of the present study indicate that these derivatives could provide useful information in the characterization and differentiation of octopaminergic receptor types and subtypes.
Scientific Publication
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