Journal of Pesticide Science
Online ISSN : 1349-0923
Print ISSN : 1348-589X
ISSN-L : 0385-1559
Brief Reports
Synthesis of N-alkylated octopamine derivatives and their interaction with octopamine receptor BmOAR1
Kenji OshimaRyunosuke YamamotoHaruna YamasakiMaki KatayamaKeita NodaTomohiro OishiHiroto Ohta
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2025 Volume 50 Issue 1 Pages 9-13

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Abstract

A series of N-alkylated octopamine derivatives was synthesized, and the structure–activity relationships of these derivatives with the silkworm Bombyx mori octopamine receptor BmOAR1 were evaluated using a secreted placental alkaline phosphatase reporter assay system. The N-alkyl moiety on the ligand affected the intensity of the agonist activity in the order: CH3>(H)>C2H5. Although linear alkyl chains of C3 or higher did not exhibit any activity, the fixed C3 alkyl group forming a pyrrolidine ring showed significant activity. These results suggest that BmOAR1 has a relatively small space around the amine-binding site, and the alkyl part constituting the cyclic amine could exert the same effect as the small alkyl group.

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© Pesticide Science Society of Japan 2025. This is an open access article distributed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International (CC BY-NC-ND 4.0) License (https://creativecommons.org/licenses/by-nc-nd/4.0/)

This article is licensed under a Creative Commons [Attribution-NonCommercial-NoDerivatives 4.0 International] license.
https://creativecommons.org/licenses/by-nc-nd/4.0/
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