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Chemical Compound Review

Bromoxidine     5-bromo-N-(4,5-dihydro-1H- imidazol-2...

Synonyms: brimonidina, brimonidine, brimonidinum, Lopac-U-104, CHEMBL844, ...
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Disease relevance of brimonidine

  • After overnight incubation with pertussis toxin, inhibition by UK-14,304 and Oxo-M was much reduced [1].
  • PURPOSE: To examine the neuroprotective effect of the alpha(2)-adrenergic agonist brimonidine in a chronic ocular hypertension model [2].
  • METHODS: According to a 4 x 4 Latin squares design for repeated measures, 27 untreated patients and patients with newly diagnosed primary open-angle glaucoma (POAG) were treated with timolol 0.5% at 8 AM and 8 PM; brimonidine 0.2% at 8 AM and 8 PM; dorzolamide 2% at 8 AM, 2 PM, and 8 PM; and latanoprost 0.005% at 8 PM [3].
  • When administered shortly after ischemia (up to 2 hours) AGN 190342 rescued substantial proportions of RGCs destined to die and diminished slow RGC death [4].
  • Brimonidine reduced the progressive loss of ganglion cells to 26% +/- 1% and 15% +/- 2% at doses of 0.5 and 1 mg/kg. d, respectively [2].

Psychiatry related information on brimonidine


High impact information on brimonidine

  • Second, the large contraction-induced attenuation in sympathetic vasoconstriction elicited by nerve stimulation or UK 14,304 was partially reversed when the physiologic activation of KATP channels produced by muscle contraction was prevented with glibenclamide [7].
  • The pharmacological properties of action potential-evoked NE release paralleled those of N-type Ca2+ channels: Release was completely blocked by Cd2+ or omega-conotoxin GVIA, reduced 50% by 10 microM NE or 62% by 2 microM UK-14,304, an alpha2-adrenergic agonist, and reduced 63% by 10 microM oxotremorine M (Oxo-M), a muscarinic agonist [1].
  • However, when extracellular Ca2+ was removed in the presence of UK 14304, [Ca2+]i and MLC phosphorylation fell to resting levels, but force remained significantly elevated above basal levels [8].
  • In the previously denuded arteries with regenerated endothelium, the endothelium-dependent relaxations to UK 14304 (a selective alpha 2-adrenergic agonist), serotonin, and aggregating platelets were impaired 4 weeks after endothelium removal and remained so throughout the study [9].
  • Systemic intravenous UK-14304, a highly selective alpha 2-adrenoceptor agonist, produced a precipitous, neurogenic vasodilation that lowered vascular resistance below the subsequently denervated resistance, thus indicating that an active vasodilation was involved [10].

Chemical compound and disease context of brimonidine


Biological context of brimonidine


Anatomical context of brimonidine


Associations of brimonidine with other chemical compounds

  • Activation of p70s6k by both UK 14304 and LPA was accompanied by increased phosphorylation of the protein [11].
  • Deprivation for glucose or glutamine also impeded the recovery process; by contrast, addition of UK-14,304 or clonidine did not interfere, indicating that the expression of the alpha 2-adrenoceptor is not subject to homologous regulation in the HT29 cell [21].
  • Preincubation of human platelet membranes with the full alpha 2-agonist UK 14,304 in the absence of GTP increases the potency of the agonist to inhibit adenylate cyclase in a pre-steady state (15-sec) assay [24].
  • The antinociceptive effects of both UK-14,304 and guanfacine were blocked by intraperitoneal injections of yohimbine, a result indicating that both drugs induced their actions by activating alpha 2-adrenoceptors [25].
  • The specific alpha 2-agonist UK-14,304 reduced cAMP accumulation (maximum 43% reduction) and inhibited melatonin release (EC50 = 19 nM) in the presence of 3 X 10(-8) M VIP [26].

Gene context of brimonidine

  • CONCLUSIONS: Brimonidine appears to maintain BCL-2 levels by supporting the activity of an intrinsic anti-apoptosis signalling system that involves phosphorylation of protein kinase B. Phosphorylated protein kinase B appears to counteract the apoptosis signalling mechanisms which operate in glaucomatous retina [27].
  • The preferential R alpha-2A/H alpha-2A AR antagonist, [2-(2H-(1-methyl-1, 3-dihydroisoindole)methyl)-4, 5-dihydro-imidazole (BRL 44408), enhanced hippocampal synthesis of NA and blocked the antinociceptive and motor effects of UK 14,304, xylazine, guanfacine and guanabenz [28].
  • The effects on alpha(i2)-mRNA were accompanied by a parallel, albeit weaker effect on the protein level (only GIP and UK 14,304 were investigated) [29].
  • The changes in alpha(i2)-mRNA levels by either compound were paralleled by inverse changes in insulin secretion: preincubation with UK 14,304 for 8 h led to an increased insulin secretion when challenged by either GLP-1, GIP or glucose (8.3 mM) [29].
  • DESIGN: Prospective longitudinal follow-up of serial visual fields in patients enrolled onto an open-label, nonrandomized pilot study of topical brimonidine purite as prophylactic treatment after first eye involvement in LHON [30].

Analytical, diagnostic and therapeutic context of brimonidine


  1. Modulation by neurotransmitters of catecholamine secretion from sympathetic ganglion neurons detected by amperometry. Koh, D.S., Hille, B. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  2. Neuroprotection of retinal ganglion cells by brimonidine in rats with laser-induced chronic ocular hypertension. WoldeMussie, E., Ruiz, G., Wijono, M., Wheeler, L.A. Invest. Ophthalmol. Vis. Sci. (2001) [Pubmed]
  3. Effects of topical hypotensive drugs on circadian IOP, blood pressure, and calculated diastolic ocular perfusion pressure in patients with glaucoma. Quaranta, L., Gandolfo, F., Turano, R., Rovida, F., Pizzolante, T., Musig, A., Gandolfo, E. Invest. Ophthalmol. Vis. Sci. (2006) [Pubmed]
  4. Neuroprotective effects of alpha(2)-selective adrenergic agonists against ischemia-induced retinal ganglion cell death. Lafuente, M.P., Villegas-Pérez, M.P., Sobrado-Calvo, P., García-Avilés, A., Miralles de Imperial, J., Vidal-Sanz, M. Invest. Ophthalmol. Vis. Sci. (2001) [Pubmed]
  5. Decreased density of presynaptic alpha 2-adrenoceptors in postmortem brains of patients with Alzheimer's disease. Meana, J.J., Barturen, F., Garro, M.A., García-Sevilla, J.A., Fontán, A., Zarranz, J.J. J. Neurochem. (1992) [Pubmed]
  6. Pharyngeal, esophageal, and proximal gastric responses associated with vomiting. Lang, I.M., Sarna, S.K., Dodds, W.J. Am. J. Physiol. (1993) [Pubmed]
  7. ATP-sensitive potassium channels mediate contraction-induced attenuation of sympathetic vasoconstriction in rat skeletal muscle. Thomas, G.D., Hansen, J., Victor, R.G. J. Clin. Invest. (1997) [Pubmed]
  8. Mechanisms of signal transduction during alpha 2-adrenergic receptor-mediated contraction of vascular smooth muscle. Aburto, T.K., Lajoie, C., Morgan, K.G. Circ. Res. (1993) [Pubmed]
  9. Natural course of the impairment of endothelium-dependent relaxations after balloon endothelium removal in porcine coronary arteries. Possible dysfunction of a pertussis toxin-sensitive G protein. Shimokawa, H., Flavahan, N.A., Vanhoutte, P.M. Circ. Res. (1989) [Pubmed]
  10. Neurogenic histaminergic vasodilation in canine skeletal muscle: mediation by alpha 2-adrenoceptor stimulation. Camazine, B., Shannon, R.P., Guerrero, J.L., Graham, R.M., Powell, W.J. Circ. Res. (1988) [Pubmed]
  11. Wortmannin-sensitive activation of p70s6k by endogenous and heterologously expressed Gi-coupled receptors. Wilson, M., Burt, A.R., Milligan, G., Anderson, N.G. J. Biol. Chem. (1996) [Pubmed]
  12. Regional and gender variations in adipose tissue lipolysis in response to weight loss. Mauriège, P., Imbeault, P., Langin, D., Lacaille, M., Alméras, N., Tremblay, A., Després, J.P. J. Lipid Res. (1999) [Pubmed]
  13. Presynaptic inhibition of transmitter release from rat sympathetic neurons by bradykinin. Edelbauer, H., Lechner, S.G., Mayer, M., Scholze, T., Boehm, S. J. Neurochem. (2005) [Pubmed]
  14. Three-month comparison of brimonidine and latanoprost as adjunctive therapy in glaucoma and ocular hypertension patients uncontrolled on beta-blockers: tolerance and peak intraocular pressure lowering. Simmons, S.T., Earl, M.L. Ophthalmology (2002) [Pubmed]
  15. Is the sympathoinhibitory effect of rilmenidine mediated by alpha-2 adrenoceptors or imidazoline receptors? Urban, R., Szabo, B., Starke, K. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  16. Direct effects of alpha 2-adrenergic receptor stimulation on intravascular systemic capacity in the dog. Supple, E.W., Graham, R.M., Powell, W.J. Hypertension (1988) [Pubmed]
  17. Inhibition by brimonidine of forskolin-induced nitrite production in isolated pig ciliary processes. Liu, R., Wu, R., Flammer, J., Haefliger, I.O. Invest. Ophthalmol. Vis. Sci. (2002) [Pubmed]
  18. Increased alpha 2-adrenergic binding sites and antilipolytic effect in adipocytes from genetically obese rats. Carpéné, C., Rebourcet, M.C., Guichard, C., Lafontan, M., Lavau, M. J. Lipid Res. (1990) [Pubmed]
  19. Reduced alpha(2)-adrenergic sensitivity of subcutaneous abdominal adipocytes as a modulator of fasting and postprandial triglyceride levels in men. Imbeault, P., Couillard, C., Tremblay, A., Després, J.P., Mauriège, P. J. Lipid Res. (2000) [Pubmed]
  20. Molecular interaction of the human alpha 2-C10-adrenergic receptor, when expressed in Rat-1 fibroblasts, with multiple pertussis toxin-sensitive guanine nucleotide-binding proteins: studies with site-directed antisera. McClue, S.J., Milligan, G. Mol. Pharmacol. (1991) [Pubmed]
  21. In vitro study of alpha 2-adrenoceptor turnover and metabolism using the adenocarcinoma cell line HT29. Paris, H., Taouis, M., Galitzky, J. Mol. Pharmacol. (1987) [Pubmed]
  22. Norepinephrine release and neuropeptide Y in medulla oblongata of spontaneously hypertensive rats. Tsuda, K., Tsuda, S., Masuyama, Y., Goldstein, M. Hypertension (1990) [Pubmed]
  23. Alpha2-adrenoreceptor agonists are neuroprotective in a rat model of optic nerve degeneration. Yoles, E., Wheeler, L.A., Schwartz, M. Invest. Ophthalmol. Vis. Sci. (1999) [Pubmed]
  24. Inhibition of adenylate cyclase is mediated by the high affinity conformation of the alpha 2-adrenergic receptor. Thomsen, W.J., Jacquez, J.A., Neubig, R.R. Mol. Pharmacol. (1988) [Pubmed]
  25. Antinociceptive actions of alpha 2-adrenoceptor agonists in the rat spinal cord: evidence for antinociceptive alpha 2-adrenoceptor subtypes and dissociation of antinociceptive alpha 2-adrenoceptors from cyclic AMP. Uhlén, S., Persson, M.L., Alari, L., Post, C., Axelsson, K.L., Wikberg, J.E. J. Neurochem. (1990) [Pubmed]
  26. Vasoactive intestinal polypeptide and alpha 2-adrenoceptor agonists regulate adenosine 3',5'-monophosphate accumulation and melatonin release in chick pineal cell cultures. Pratt, B.L., Takahashi, J.S. Endocrinology (1989) [Pubmed]
  27. Apoptosis and anti-apoptosis signalling in glaucomatous retinopathy. Tatton, W.G., Chalmers-Redman, R.M., Tatton, N.A. European journal of ophthalmology. (2001) [Pubmed]
  28. Multiple alpha-2 adrenergic receptor subtypes. II. Evidence for a role of rat R alpha-2A adrenergic receptors in the control of nociception, motor behavior and hippocampal synthesis of noradrenaline. Millan, M.J., Bervoets, K., Rivet, J.M., Widdowson, P., Renouard, A., Le Marouille-Girardon, S., Gobert, A. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  29. Galpha(i2)-mRNA and -protein regulation as a mechanism for heterologous sensitization and desensitization of insulin secretion. Kesper, S., Rucha, J., Neye, H., Mazenot, C., Verspohl, E.J. Cell. Signal. (1999) [Pubmed]
  30. Progression of visual field defects in leber hereditary optic neuropathy: experience of the LHON treatment trial. Newman, N.J., Biousse, V., Newman, S.A., Bhatti, M.T., Hamilton, S.R., Farris, B.K., Lesser, R.L., Turbin, R.E. Am. J. Ophthalmol. (2006) [Pubmed]
  31. Increased alpha2-adrenergic constriction of isolated arterioles in diffuse scleroderma. Flavahan, N.A., Flavahan, S., Liu, Q., Wu, S., Tidmore, W., Wiener, C.M., Spence, R.J., Wigley, F.M. Arthritis Rheum. (2000) [Pubmed]
  32. Heat, but not mechanical hyperalgesia, following adrenergic injections in normal human skin. Fuchs, P.N., Meyer, R.A., Raja, S.N. Pain (2001) [Pubmed]
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