Jia Huang, Tomohiro Hamasaki, Yoshihisa Ozoe
Institute of Insect Sciences, Zhejiang University, Hangzhou, China.
Archives of insect biochemistry and physiology 2010 FebSeries of agonists and antagonists were examined for their actions on a Bombyx morialpha-adrenergic-like octopamine receptor (OAR) stably expressed in HEK-293 cells. The rank order of potency of the agonists was clonidine>naphazoline>tolazoline in Ca(2+) mobilization assays, and that of the antagonists was chlorpromazine>yohimbine. These findings suggest that the B. mori OAR is more closely related to the class-1 OAR in the intact tissue than to the other classes. N'-(4-Chloro-o-tolyl)-N-methylformamidine (DMCDM) and 2-(2,6-diethylphenylimino)imidazolidine (NC-5) elevated the intracellular calcium concentration ([Ca(2+)](i)) with EC(50)s of 92.8 microM and 15.2 nM, respectively. DMCDM and NC-5 led to increases in intracellular cAMP concentration ([cAMP](i)) with EC(50)s of 234 nM and 125 nM, respectively. The difference in DMCDM potencies between the cAMP and Ca(2+) assays might be due to "functional selectivity." The Ca(2+) and cAMP assay results for DMCDM suggest that the elevation of [cAMP](i), but not that of [Ca(2+)](i), might account for the insecticidal effect of formamidine insecticides. 2009 Wiley Periodicals, Inc.
Jia Huang, Tomohiro Hamasaki, Yoshihisa Ozoe. Pharmacological characterization of a Bombyx mori alpha-adrenergic-like octopamine receptor stably expressed in a mammalian cell line. Archives of insect biochemistry and physiology. 2010 Feb;73(2):74-86
PMID: 19918790
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