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Norbormide : ウィキペディア英語版
Norbormide

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Norbormide (Raticate, Shoxin) is a toxic compound used as a rodenticide. It has several mechanisms of action, acting as a vasoconstrictor and calcium channel blocker,〔Rennison D, Bova S, Cavalli M, Ricchelli F, Zulian A, Hopkins B, Brimble MA. Synthesis and activity studies of analogues of the rat selective toxicant norbormide. ''Bioorganic and Medicinal Chemistry''. 2007 Apr 15;15(8):2963-74. PMID 17321141〕 but is selectively toxic to rats and has relatively low toxicity to other species, due to a species specific action of opening the permeability transition pores in rat mitochondria.〔Zulian A, Petronilli V, Bova S, Dabbeni-Sala F, Cargnelli G, Cavalli M, Rennison D, Stäb J, Laita O, Lee DJ, Brimble MA, Hopkins B, Bernardi P, Ricchelli F. Assessing the molecular basis for rat-selective induction of the mitochondrial permeability transition by norbormide. ''Biochimica et Biophysica Acta''. 2007 Jul;1767(7):980-8. PMID 17509521〕
== History ==
In the early 1960s norbormide was developed to serve as a non-anticoagulant rat poison. During the 1970s, however, the utilization of this rodenticide decreased, since anticoagulant toxins seemed to be more effective against a wider range of rodents.〔Telle, H.J., Some fields observations on the observations on the acceptability and effectiveness of norbormide to Rattus norvegicus. Who/VBC, 1967. 67.39: p. 10.〕 NRB only kills rodents of the genus Rattus (R. norvegicus, R. exulans and R. rattus) and happens to be moderately innocent to other rodents and mammals.〔Ravindran, S., et al., In vitro metabolism of norbormide in rat, mouse and guinea pig liver preparations Environmental Toxicology Pharmacology, 2009. 27(144-148).〕 Although many view its selective feature as a disadvantage, scientists of Land Research in New Zealand search for ways to improve this rodenticide and develop several analogues.〔Bova, S., et al., Signaling mechanisms for the selective vasoconstrictor effect of norbormide on the rat small arteries. The Journal of Pharmacology and Experimental Therapeutics, 2001. 296: p. 458-463.〕 〔Cavalli, M., et al., Distribution of the casoconstrictor and vasorelaxant effects of norbormide along the vascular tree of the rat. Life Sciences, 2004. 75: p. 2157.〕 〔Ricchelli, F., et al., Species-specific modulation of the mitochondrial permeability transition by norbormide. Biochemica et Biophysica Acta, 2005. 1708: p. 178-186.〕

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