Effects of diazepam and chlordimeform analogs on the German and the American cockroaches |
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| Affiliation: | 1. Department of Ecology and Environmental Science, Umeå University, SE 90187 Umeå, Sweden;2. Department of Physics, Umeå University, SE 90187 Umeå, Sweden;3. Department of Chemistry, Umeå University, SE 90187 Umeå, Sweden;4. Department of Wildlife, Fish, and Environmental Studies, SLU, Umeå, Sweden;5. School of Marine Studies, The University of the South Pacific, Laucala Bay Road, Suva, Fiji;1. University of Lille, CNRS, UMR 8198—Evo-Eco-Paleo, F-59000 Lille, France;2. PHIM Plant Health Institute, Université de Montpellier, CIRAD, INRAE, Institut Agro, IRD, Montpellier, France;3. Agroécologie, AgroSup Dijon, INRAE, Univ. Bourgogne, Univ. Bourgogne-Franche-Comté, Dijon, France;4. Institut de Systématique, Evolution, Biodiversité (ISYEB), Muséum national d''Histoire naturelle, CNRS, SU, EPHE, UA, Paris, France;5. CEFE, CNRS, Montpellier, France;6. INRAE, Univ. Bordeaux, BIOGECO, Pessac, France;7. School of Natural Sciences, Bangor University, Bangor, Gwynedd, United Kingdom;8. UMR 1349 IGEPP—Institut de Génétique, Environnement et Protection des Plantes, INRAE—Agrocampus Ouest—Université Rennes 1, Rennes, France;9. UMR MIA-Paris, Université Paris-Saclay, AgroParisTech, INRAE, Paris, France;10. Department of Evolution, Ecology, and Organismal Biology, University of California, Riverside, Riverside, CA, United States;11. INRAE, UMR PVBMT, Saint Pierre, France;12. CBGP, INRAE, IRD, CIRAD, Institut Agro, Univ Montpellier, Montpellier, France;13. Cirad, UMR PVBMT, Saint Pierre, France;14. LPSM (UMR 8001)—Laboratoire de Probabilités, Statistiques et Modélisations, Paris, France;15. Univ. Lille, CNRS, Inserm, CHU Lille, Institut Pasteur de Lille, U1019—UMR 9017—CIIL—Center for Infection and Immunity of Lille, Lille, France;1. Sorbonne Université - Institut d''Écologie et des Sciences de l''Environnement de Paris (iEES Paris) - Département d''Écologie Sensorielle, Campus Pierre et Marie Curie (UPMC), 75252 Paris Cedex 05, France;2. UPRES-EA 4358 GlycoMev, Université de Rouen, Rouen, France;3. Sorbonne Université - Institut d''Écologie et des Sciences de l''Environnement de Paris (iEES Paris) - Département d''Écologie Sensorielle, Centre INRA, Bâtiment 1, Route de Saint Cyr, 78026 Versailles cedex, Versailles, France;4. École Pratique des Hautes Études (EPHE), PSL. UMR 7619 METIS, Université Pierre et Marie Curie (UPMC) – Sorbonne Universités, Paris, France |
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| Abstract: | ![]()
Twenty-one diazepam- and chlordimeform (CDM)-related compounds were synthesized by mimicking some parts of the 1,4-benzodiazepine tranquilizing drugs, and were tested for their insecticidal activity against the German cockroach. Some of these compounds showed knockdown effects and some were insecticidal. Against the German cockroach the most toxic CDM analog was N-propargyl CDM (compound 6), and that with a potent knockdown potency was compound 13 which has a structural resemblance to diazepam. Ligand-receptor binding assay was carried out, using [3H]diazepam as a ligand to examine the relation between CDM-related compounds and the 1,4-benzodiazepines. The [3H]diazepam binding to a specific site in the American cockroach brain was inhibited by the insecticidal compounds. Among these compounds a correlation exists between their inhibitory potency on specific [3H]diazepam binding and their insecticidal activity, suggesting a possible significance of such an interaction with the diazepam binding site for the toxicity of these compounds against cockroaches. |
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