Mice treated with idazoxan, which blocks theα2A-adrenergic receptor, behaved similarly to control animals despite still having amyloid-beta plaques in the brain, as a proof-of-concept experiment that dramatically reducedAlzheimer's disease pathology and symptoms in two mouse models, potentially offering an immediate treatment for this devastating disease.[5]
The reaction of catechol (1) with 2-Chloroacrylonitrile [920-37-6] (2) gives 2-cyano-1,4-benzodioxan [1008-92-0] (3).Pinner reaction with alcoholic hydrogen chloride leads to the iminoether,[11] (4). Treatment withethylenediamine [107-15-3] (5) gives the imidazoline ring affordingIdazoxin (6).
Idazoxan has been used to reversexylazine in cattle and sheep but it is rarely used in practice with other α2-adrenergic receptor antagonists such asyohimbine andatipamezole being used instead.[12]
^Bousquet P, Bruban V, Schann S, Greney H, Ehrhardt JD, Dontenwill M, Feldman J (June 1999). "Participation of imidazoline receptors and alpha(2-)-adrenoceptors in the central hypotensive effects of imidazoline-like drugs".Annals of the New York Academy of Sciences.881 (1):272–8.Bibcode:1999NYASA.881..272B.doi:10.1111/j.1749-6632.1999.tb09369.x.PMID10415925.S2CID38772290.
^Yakubu MA, Hamilton CA, Howie CA, Reid JL (1988). "Idazoxan and brain alpha2-adrenoceptor in the rabbit".Brain Research.436 (2):289–296.doi:10.1016/0006-8993(88)90402-7.PMID2848612.
^Hamilton CA, Yakubu MA, Jardine E, Reid JL (1991). "Imidazole binding sites in rabbit kidney and forebrain membranes".J Auton Pharmacol.11 (4):277–83.doi:10.1111/j.1474-8673.1991.tb00325.x.PMID1939285.
^Chapleo CB, Myers PL, Butler RC, Doxey JC, Roach AG, Smith CF (June 1983). "alpha-adrenoreceptor reagents. 1. Synthesis of some 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists and potential antidepressants".Journal of Medicinal Chemistry.26 (6):823–31.doi:10.1021/jm00360a008.PMID6133953.
^US 2979511, Krapcho J, Lott WA, "Certain 1, 4-benzodioxanyl imidazolines and corresponding pyrimidines and process", issued 11 April 1961, assigned to Olin Corp.
^US 7338970, Bougaret J, Avan JL, Segonds R, "Pharmaceutical composition based on idazoxan, salts, hydrates or polymorphs thereof", issued 3 March 2008, assigned to Pierre Fabre Medicament.
^Lamont LA, Creighton CM (11 September 2024). "Sedatives and Tranquilizers". In Lamont L, Grimm K, Robertson S, Love L, Schroeder C (eds.).Veterinary Anesthesia and Analgesia, The 6th Edition of Lumb and Jones. Wiley Blackwell. pp. 338–344.ISBN978-1-119-83027-6.
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