Oshima Kenji, Yamamoto Ryunosuke, Yamasaki Haruna, Katayama Maki, Noda Keita, Oishi Tomohiro, Ohta Hiroto
Department of Biological and Chemical Systems Engineering, National Institute of Technology, Kumamoto College.
Graduate School of Science and Technology, Kumamoto University.
J Pestic Sci. 2025 Feb 20;50(1):9-13. doi: 10.1584/jpestics.D24-054.
A series of -alkylated octopamine derivatives was synthesized, and the structure-activity relationships of these derivatives with the silkworm octopamine receptor BmOAR1 were evaluated using a secreted placental alkaline phosphatase reporter assay system. The -alkyl moiety on the ligand affected the intensity of the agonist activity in the order: CH>(H)>CH. 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.
合成了一系列的 -烷基化章鱼胺衍生物，并使用分泌型胎盘碱性磷酸酶报告基因检测系统评估了这些衍生物与家蚕章鱼胺受体BmOAR1的构效关系。配体上的 -烷基部分对激动剂活性强度的影响顺序为：CH>(H)>CH。尽管C3或更长的直链烷基没有表现出任何活性，但形成吡咯烷环的固定C3烷基显示出显著活性。这些结果表明，BmOAR1在胺结合位点周围的空间相对较小，构成环胺的烷基部分可以发挥与小烷基相同的作用。
