Disease relevance of HSDB 7050

• There were no significant effects on drift or survival of the test species exposed to RH-5992 at the maximum test concentration of 3.5 mg/liter (100x the worst-case expected environmental concentration) in laboratory toxicity tests and stream channel treatments [1].
• Bacillus thuringiensis and tebufenozide showed no significant effects on parasitism [2].

Psychiatry related information on HSDB 7050

• The terminal feeding behavior ofobliquebanded leafroller larvae, low residues on terminal foliage before the end of the typical 2-wk spray interval, and the length of exposure necessary for high levels of mortality may decrease the effectiveness of tebufenozide for obliquebanded leafroller control [3].

High impact information on HSDB 7050

• Our studies of the Bombyx mori ecdysone receptor (BE) revealed that, unlike the Drosophila melanogaster ecdysone receptor (DE), treatment of BE with the ecdysone agonist tebufenozide stimulated high level transactivation in mammalian cells without adding an exogenous heterodimer partner [4].
• A ligand-mediated transactivation of Aa(Delta A/B)EcR-USP or Aa(Delta A/B)EcR-RXR heterodimers in response to an ecdysteroid agonist RH-5992 was observed only in the presence of GRIP1, a mouse co-activator [5].
• CHR75 mRNA was induced in ecdysone treated CF-203 cells and in the midgut, fat body and epidermis of larvae that were fed the non-steroidal ecdysteroid agonist, RH-5992 [6].
• The normal decline in JH biosynthesis by the corpora allata does not occur in starved or RH-5992-fed larvae [7].
• PDR5 (pleiotropic drug resistance 5) deletion mutants (Deltapdr5 and Deltapdr5Deltasnq2) retained significantly higher levels of 14C-radiolabeled RH-5992 within the cells when compared to wild-type strain or single deletion mutants of SNQ2 (Deltasnq2) and YCF1 (Deltaycf1) [8].

Chemical compound and disease context of HSDB 7050

• While two of the bisacylhydrazines (coded as RH-5992 and RH-2485) are predominantly toxic to lepidopteran pests, RH-5849, which has not been commercialized, has a broader spectrum of toxicity [9].
• A series of studies were conducted to examine the residual activity and toxicity of the ecdysone agonists tebufenozide and methoxyfenozide to codling moth, Cydia pomonella (L.), and oriental fruit moth, Grapholita molesta (Busck), in North Carolina apple systems [10].
• At a concentration of 20 ppm, PBO and DEM significantly synergized the toxicity of tebufenozide in resistant and susceptible colonies (three- to fourfold) [11].
• The effect of the metabolic synergists piperonyl butoxide (PBO) and diethyl maleate (DEM) on tebufenozide toxicity was examined to determine mechanisms for obliquebanded leafroller resistance to tebufenozide and potential mechanisms for other new insecticides [11].
• Toxicity tests using this system were conducted with two arthropod species that are found in saline habitats: mosquito Aedes taeniorhynchus (Wiedemann) and brine shrimp (Artemia sp.). Four insecticides-aldicarb, dimethoate, imidacloprid, and tebufenozide-were studied [12].

Biological context of HSDB 7050

• Basis for selective action of a synthetic molting hormone agonist, RH-5992 on lepidopteran insects [13].
• Injection of RH-5992 into pupae resulted in a dose dependent induction of mRNA for ecdysone-induced transcription factor, Choristoneura hormone receptor 3 (CHR3) [14].
• Using the IAL-PID2 cells derived from imaginal wing discs of last larval instar of Plodia interpunctella, we investigated the action of RH-5992 in the control of cell growth [15].
• Comparing the results here to those from a previous study with tebufenozide, which was selectively toxic to cladocerans and had little effect on food web stability, indicates that differential sensitivity among taxa can influence the ecological significance of pesticide effects on zooplankton communities [16].
• The clearance of RH-5992 from DM-2 cells was temperature dependent and was blocked by 10(-5) M ouabain, an inhibitor of Na+, K(+)-ATPase suggesting that the efflux was due to active transport [13].

Anatomical context of HSDB 7050

• The epithelial cell line from the dipteran Chironomus tentans responds to the insect steroid hormone 20-hydroxyecdysone and the non-steroidal analogue tebufenozide by undergoing a morphogenetic and biochemical differentiation program [17].
• Morphological and molecular effects of 20-hydroxyecdysone and its agonist tebufenozide on CF-203, a midgut-derived cell line from the spruce budworm, Choristoneura fumiferana [18].
• In vitro cultures of developing ovarioles reveal the requirement for the presence of an as yet unidentified growth factor(s) in the hemolymph, while the follicle developmental arrest that is observed after treatment with the ecdysone agonist tebufenozide indicates the requirement for a decline in the level of 20E [19].

Associations of HSDB 7050 with other chemical compounds

• Western blot analysis revealed that the expression of EcR and USP was significantly increased in tebufenozide- and methoxyfenozide-treated samples compared to the control, suggesting that ecdysone agonists regulated the Vg synthesis via the EcR and USP proteins complex [20].
• Sublethal concentrations of the bisacylhydrazine moulting hormone agonists, RH-5849, and tebufenozide (RH-5992) were fed to sixth (final) instar larvae of Spodoptera litura [21].
• The 20-hydroxyecdysone agonist, tebufenozide (RH5992), induced the expression of the CfChitinase gene in the early stage of the sixth-instar larvae and the enzyme was detected in the epidermis and molting fluid 24 h post treatment [22].
• Treatment of last-instar larvae of multi-resistant cotton leafworm Spodoptera littoralis with four dibenzoylhydrazines, methoxyfenozide (RH-2485), tebufenozide (RH-5992), halofenozide (RH-0345), and RH-5849, resulted in premature molting leading to death [23].
• The insecticidal activity of juvenile hormone agonists methoprene and pyriproxyfen, and the ecdysone agonists RH-5849 and tebufenozide was evaluated against susceptible and actellic-resistant strains of Tribolium castaneum and susceptible strains of Rhyzopertha dominica and Sitophilus oryzae [24].

Gene context of HSDB 7050

• RH-5992, a stable ecdysone agonist, caused a similar induction pattern of EcR-A and EcR-B mRNAs in the midgut, epidermis and fat body of sixth instar larvae [25].
• The hormonal activity of several tebufenozide analogs with varying alkyl groups such as CH(3), n-C(3)H(7), i-C(3)H(7), n-C(4)H(9) and n-C(5)H(11) at the para-position of the benzene ring furthest from the tert-butyl group was lower than that of tebufenozide (alkyl group is C(2)H(5)) [26].
• Safety testing of tebufenozide, a new molt-inducing insecticide, for effects on nontarget forest soil invertebrates [27].
• Similarly, population growth over 8-10 weeks in the four species of soil Collembola in LFH material contaminated with tebufenozide at 100x EEC was not affected [27].
• Concentrations of RH-5992 as low as 10(-10) M induced CHR3 mRNA in CF-203 cells, whereas concentrations as high as 10(-6) M induced only very low levels of DHR3 mRNA in DM-2 cells [13].

Analytical, diagnostic and therapeutic context of HSDB 7050

• Northern blot analysis showed that the mRNA transcript was expressed at times of increasing ecdysteroid titre in final instar S. littoralis larvae and was induced by the ecdysteroid receptor agonist, RH-5992, in midgut and fat body [28].
• The results of bioassays indicated that some of these title compounds exhibit higher larvicidal activities than RH5849 (N-tert-butyl-N,N '-dibenzoylhydrazine), but they are not good compared to the parent compound (tebufenozide) [29].
• Two-dimensional gel electrophoresis analysis of proteins following tebufenozide treatment of Chironomus riparius [30].

References