RH 5849, a nonsteroidal ecdysone agonist: effects on a Drosophila cell line.
The steroid molting hormone 20-hydroxyecdysone is the physiological inducer of molting and metamorphosis in insects. In ecdysone-sensitive Drosophila Kc cells, the insecticide RH 5849 (1,2-dibenzoyl-1-tert-butylhydrazine) mimics the action of 20-hydroxyecdysone by causing the formation of processes, an inhibition of cell proliferation, and induction of acetylcholinesterase. RH 5849 also competes with [3H]ponasterone A for high-affinity ecdysone receptor sites from Kc cell extracts. Resistant cell populations selected by growth in the continued presence of either RH 5849 or 20-hydroxyecdysone are insensitive to both compounds and exhibit a decreased titer of measurable ecdysone receptors. Although it is less potent than 20-hydroxyecdysone in both whole-cell and cell-free receptor assays, RH 5849 is the first nonsteroidal ecdysone agonist.
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Research Labs, Rohm and Haas Co., Spring House, PA 19477.
D000110:Acetylcholinesterase / Q000096:biosynthesis; D000818:Animals; D001667:Binding, Competitive; D002454:Cell Differentiation / Q000187:drug effects; D002460:Cell Line; D004330:Drosophila / Q000166:cytology / Q000187:drug effects*; D004441:Ecdysterone / Q000031:analogs & derivatives / Q000378:metabolism; D006834:Hydrazines / Q000494:pharmacology*; D007306:Insecticides / Q000378:metabolism / Q000494:pharmacology*; D011987:Receptors, Steroid / Q000378:metabolism
D006834:Hydrazines; D007306:Insecticides; D011987:Receptors, Steroid; C056565:1,2-dibenzoyl-tert-butylhydrazine; D004441:Ecdysterone; C008999:ponasterone A; D000110:Acetylcholinesterase