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Chemical Compound Review

oxymetazoline     3-(4,5-dihydro-1H-imidazol-2- ylmethyl)-2,4...

Synonyms: Nasivine, Ocuclear, Iliadin, Nafrine, Navasin, ...
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Disease relevance of oxymetazoline


Psychiatry related information on oxymetazoline


High impact information on oxymetazoline

  • Similar increments (above basal) in the concentration of InsP(6) induced by oxymetazoline prevented AP-2 binding to the NKA alpha-subunit in response to dopamine [9].
  • The effect of oxymetazoline on Na+,K(+)-ATPase activity was prevented by a specific peptide inhibitor of calcineurin, as well as by FK 506, an immunosuppressant agent known to inhibit calcineurin; these results indicate that the action of oxymetazoline is mediated via activation of calcineurin (a calcium/calmodulin-dependent protein phosphatase) [10].
  • The alpha 1a-selective agonist oxymetazoline induced the co-internalization of the alpha 1a- and alpha 1b-AR, whereas the alpha 1b-AR could not co-internalize with the NK1 tachykinin or CCR5 chemokine receptors [11].
  • In cerebral vessels, endothelial alpha2-adrenoceptor-dependent stimulation induced greater contractile responses in treated rats which were sensitive to bosentan, suggesting that oxymetazoline stimulates ET-1 release from the endothelium [12].
  • Pretreatments with NPY (20 nmol), oxymetazoline hydrochloride (20 nmol), or saline solution (NaCl 0.9%) were administered in one nostril 5 minutes before nasal challenge with grass pollen allergen (10,000 standardized quality units) [13].

Chemical compound and disease context of oxymetazoline


Biological context of oxymetazoline


Anatomical context of oxymetazoline


Associations of oxymetazoline with other chemical compounds


Gene context of oxymetazoline


Analytical, diagnostic and therapeutic context of oxymetazoline


  1. Bradycardia, hypotension, and near-syncope associated with Afrin (oxymetazoline) nasal spray. Glazener, F., Blake, K., Gradman, M. N. Engl. J. Med. (1983) [Pubmed]
  2. Nasal resistance in snorers with or without sleep apnea: effect of posture and nasal ventilation with continuous positive airway pressure. Desfonds, P., Planès, C., Fuhrman, C., Foucher, A., Raffestin, B. Sleep. (1998) [Pubmed]
  3. Oxymetazoline inhibits proinflammatory reactions: effect on arachidonic acid-derived metabolites. Beck-Speier, I., Dayal, N., Karg, E., Maier, K.L., Schumann, G., Semmler, M., Koelsch, S.M. J. Pharmacol. Exp. Ther. (2006) [Pubmed]
  4. Functional and biochemical evidence for the lack of cardiac presynaptic alpha-2 adrenoceptor stimulant properties of cirazoline (LD 3098), a potent alpha-1 adrenoceptor agonist in dogs and rats. Cavero, I., Lefèvre-Borg, F., Roach, A.G., Gomeni, R., Scatton, B. J. Pharmacol. Exp. Ther. (1982) [Pubmed]
  5. Thunderclap headache and reversible segmental cerebral vasoconstriction associated with use of oxymetazoline nasal spray. Loewen, A.H., Hudon, M.E., Hill, M.D. CMAJ : Canadian Medical Association journal = journal de l'Association medicale canadienne. (2004) [Pubmed]
  6. A case of panic disorder precipitated by oxymetazoline withdrawal. Saadah, H.A. The Journal of clinical psychiatry. (1987) [Pubmed]
  7. Effects of the nasal decongestant oxymetazoline on human olfactory and intranasal trigeminal function in acute rhinitis. Hummel, T., Rothbauer, C., Pauli, E., Kobal, G. Eur. J. Clin. Pharmacol. (1998) [Pubmed]
  8. Effect of oxymetazoline nose drops on acute sinusitis in the rabbit. Bende, M., Fukami, M., Arfors, K.E., Mark, J., Stierna, P., Intaglietta, M. The Annals of otology, rhinology, and laryngology. (1996) [Pubmed]
  9. G protein-coupled receptors regulate Na+,K+-ATPase activity and endocytosis by modulating the recruitment of adaptor protein 2 and clathrin. Ogimoto, G., Yudowski, G.A., Barker, C.J., Köhler, M., Katz, A.I., Féraille, E., Pedemonte, C.H., Berggren, P.O., Bertorello, A.M. Proc. Natl. Acad. Sci. U.S.A. (2000) [Pubmed]
  10. Calcineurin mediates alpha-adrenergic stimulation of Na+,K(+)-ATPase activity in renal tubule cells. Aperia, A., Ibarra, F., Svensson, L.B., Klee, C., Greengard, P. Proc. Natl. Acad. Sci. U.S.A. (1992) [Pubmed]
  11. Oligomerization of the alpha 1a- and alpha 1b-adrenergic receptor subtypes. Potential implications in receptor internalization. Stanasila, L., Perez, J.B., Vogel, H., Cotecchia, S. J. Biol. Chem. (2003) [Pubmed]
  12. Endothelin-1 regulates tone of isolated small arteries in the rat: effect of hyperendothelinemia. Thorin, E., Cernacek, P., Dupuis, J. Hypertension (1998) [Pubmed]
  13. Attenuation of allergen-evoked nasal responses by local pretreatment with exogenous neuropeptide Y in atopic patients. Lacroix, J.S., Mosimann, B.L. J. Allergy Clin. Immunol. (1996) [Pubmed]
  14. Benzalkonium chloride in a decongestant nasal spray aggravates rhinitis medicamentosa in healthy volunteers. Graf, P., Hallén, H., Juto, J.E. Clin. Exp. Allergy (1995) [Pubmed]
  15. Rhinitis medicamentosa: aspects of pathophysiology and treatment. Graf, P. Allergy (1997) [Pubmed]
  16. Centrally mediated ocular hypotension: potential role of imidazoline receptors. Campbell, W.R., Potter, D.E. Ann. N. Y. Acad. Sci. (1995) [Pubmed]
  17. A double-blind comparison between oral pseudoephedrine and topical oxymetazoline in the prevention of barotrauma during air travel. Jones, J.S., Sheffield, W., White, L.J., Bloom, M.A. The American journal of emergency medicine. (1998) [Pubmed]
  18. Effects of topical nasal decongestants on histology of nasal respiratory mucosa in rabbits. Suh, S.H., Chon, K.M., Min, Y.G., Jeong, C.H., Hong, S.H. Acta Otolaryngol. (1995) [Pubmed]
  19. Nasal administration of the nitric oxide synthase inhibitor L-NAME induces daytime somnolence. Sippel, J.M., Giraud, G.D., Holden, W.E. Sleep. (1999) [Pubmed]
  20. Identification of alpha 2-adrenergic receptors in chicken pineal gland using [3H]rauwolscine. Bylund, D.B., Rudeen, P.K., Petterborg, L.J., Ray-Prenger, C. J. Neurochem. (1988) [Pubmed]
  21. Evidence that catecholamines stimulate renal gluconeogenesis through an alpha 1-type of adrenoceptor. Kessar, P., Saggerson, E.D. Biochem. J. (1980) [Pubmed]
  22. Oxymetazoline inhibits adenylate cyclase by activation of serotonin-1 receptors in the OK cell, an established renal epithelial cell line. Murphy, T.J., Bylund, D.B. Mol. Pharmacol. (1988) [Pubmed]
  23. Regional distribution of alpha 2A- and alpha 2B-adrenoceptor subtypes in postmortem human brain. De Vos, H., Vauquelin, G., De Keyser, J., De Backer, J.P., Van Liefde, I. J. Neurochem. (1992) [Pubmed]
  24. Effect of noradrenergic lesions on subtypes of alpha 2-adrenoceptors in rat brain. Ordway, G.A. J. Neurochem. (1995) [Pubmed]
  25. Potent alpha(2A)-adrenoceptor-mediated vasoconstriction by brimonidine in porcine ciliary arteries. Wikberg-Matsson, A., Simonsen, U. Invest. Ophthalmol. Vis. Sci. (2001) [Pubmed]
  26. Benzalkonium chloride in nasal decongestive sprays has a long-lasting adverse effect on the nasal mucosa of healthy volunteers. Hallén, H., Graf, P. Clin. Exp. Allergy (1995) [Pubmed]
  27. Dissociation of the alpha-adrenergic inhibitory effects on glucagon- and secretin-stimulated bile volume and on cyclic adenosine monophosphate production in the isolated perfused rat liver. Yamatani, K., Sato, N., Takahashi, K., Hara, M., Sasaki, H. Endocrinology (1985) [Pubmed]
  28. Effect of compound D-600 (methoxyverapamil) on gluconeogenesis and on acceleration of the process by alpha-adrenergic stimuli in rat kidney tubules. Saggerson, E.D., Carpenter, C.A. Biochem. J. (1980) [Pubmed]
  29. Characterization of alpha-2 adrenergic receptors in the OK cell, an opossum kidney cell line. Murphy, T.J., Bylund, D.B. J. Pharmacol. Exp. Ther. (1988) [Pubmed]
  30. Involvement of alpha-2 adrenergic receptor subtypes in hyperglycemia. Angel, I., Niddam, R., Langer, S.Z. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  31. Differential capacities of the RGS1, RGS16 and RGS-GAIP regulators of G protein signaling to enhance alpha2A-adrenoreceptor agonist-stimulated GTPase activity of G(o1)alpha. Hoffmann, M., Ward, R.J., Cavalli, A., Carr, I.C., Milligan, G. J. Neurochem. (2001) [Pubmed]
  32. Hypothalamic alpha 2A-adrenoceptors stimulate growth hormone release in the rat. Makara, G.B., Kiem, D.T., Vizi, E.S. Eur. J. Pharmacol. (1995) [Pubmed]
  33. Somatostatin release from the median eminence of unanesthetized rats: lack of correlation with pharmacologically suppressed growth hormone secretion. Fukata, J., Kasting, N.W., Martin, J.B. Neuroendocrinology (1985) [Pubmed]
  34. In vivo effects of alpha-adrenoceptor agonists and antagonists on pial veins of cats. Ulrich, K., Kuschinsky, W. Stroke (1985) [Pubmed]
  35. A magnetic resonance imaging evaluation of histamine-mediated allergic response in the guinea pig nasopharynx. Sherwood, J.E., Hutt, D.A., Kreutner, W., Morton, J.B., Chapman, R.W. J. Allergy Clin. Immunol. (1993) [Pubmed]
  36. Early changes in insulin secretion and action induced by high-fat diet are related to a decreased sympathetic tone. Cruciani-Guglielmacci, C., Vincent-Lamon, M., Rouch, C., Orosco, M., Ktorza, A., Magnan, C. Am. J. Physiol. Endocrinol. Metab. (2005) [Pubmed]
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