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Chemical Compound Review

Brovana     N-[2-hydroxy-5-[(1S)-1- hydroxy-2-[[(2R)-1...

Synonyms: Foradil, formoterol, Arformoterol, CHEMBL1363, CS-1413, ...
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Disease relevance of formoterol


Psychiatry related information on formoterol


High impact information on formoterol


Chemical compound and disease context of formoterol


Biological context of formoterol

  • Inhaled formoterol in the prevention of exercise-induced bronchoconstriction in asthmatic children [18].
  • METHODS: A total of 24 patients with asthma (forced expiratory volume in 1 second, < or = 70% predicted) inhaled single doses (12 micrograms or 24 micrograms) of formoterol solution and suspension so that we could investigate the immediate tremor, airway, and cardiovascular responses in a randomized, double-blind, crossover trial [19].
  • Budesonide or formoterol at 10(-)(8) M inhibited upregulation of CD11b to 26 [15 to 40]% and 38 [23 to 46]%, respectively, and inhibited L-selectin shedding to 14 [-3 to 50]% and 27 [2 to 62]%, respectively, of control values [20].
  • CONCLUSIONS: Formoterol and salmeterol cause dose related changes in heart rate, diastolic blood pressure, and plasma glucose and potassium concentrations [21].
  • The relative dose potency for formoterol compared with salmeterol at four and eight hours for the different end points excluding systolic blood pressure ranged from 1.6 to 7.0 after adjusting for baseline values [21].

Anatomical context of formoterol

  • After formoterol treatment there was a significant decrease in eosinophils and the epithelial expression of activated NF-kappaB, but these changes were not accompanied by reduced immunoreactivity for adhesion molecules or cytokines [22].
  • Anti-edema action of formoterol in rat trachea does not depend on capsaicin-sensitive sensory nerves [23].
  • In the indirect method, both budesonide and formoterol inhibited lung fibroblast activation, resulting in diminished eosinophil activation after 4 h [20].
  • In a double-blind parallel-group study, we evaluated the effect of adding formoterol to a low dose of budesonide, compared with a higher dose of budesonide, on the composition of induced sputum [24].
  • Studies performed on airway smooth muscle in vitro have indicated that salmeterol is a partial agonist on the beta2-receptor in comparison to formoterol [25].

Associations of formoterol with other chemical compounds


Gene context of formoterol

  • RESULTS: Formoterol exerted an additive effect on the inhibition of IL-1beta stimulated ICAM-1 and VCAM-1 upregulation and GM-CSF production by budesonide in concentrations of 10(-9) M and above (p<0.05) [30].
  • The glucocorticoid budesonide and the long-acting beta2-adrenoceptor agonist formoterol are used in asthma therapy for their anti-inflammatory and bronchodilating effects, respectively [31].
  • Serum marker measurements in the formoterol group showed decreased concentrations of eosinophil blood count, ECP, and IL-4, but there was no difference in before and after measurements of sIL-2R, sICAM-1, and IgE [32].
  • Budesonide and formoterol inhibit ICAM-1 and VCAM-1 expression of human lung fibroblasts [31].
  • The beta adrenergic agonist, formoterol hemifumarate, led to increases in K+ flux into MDA-MB-453 cells, and this increase was inhibited by the GIRK channel inhibitor clozapine [33].

Analytical, diagnostic and therapeutic context of formoterol


  1. Inhaled formoterol dry powder versus ipratropium bromide in chronic obstructive pulmonary disease. Dahl, R., Greefhorst, L.A., Nowak, D., Nonikov, V., Byrne, A.M., Thomson, M.H., Till, D., Della Cioppa, G. Am. J. Respir. Crit. Care Med. (2001) [Pubmed]
  2. Protective effect and duration of action of inhaled formoterol and salbutamol on exercise-induced asthma in children. Henriksen, J.M., Agertoft, L., Pedersen, S. J. Allergy Clin. Immunol. (1992) [Pubmed]
  3. Long-acting beta2 agonists in the management of stable chronic obstructive pulmonary disease. Cazzola, M., Donner, C.F. Drugs (2000) [Pubmed]
  4. Inhaled budesonide/formoterol combination. McGavin, J.K., Goa, K.L., Jarvis, B. Drugs (2001) [Pubmed]
  5. Budesonide/formoterol maintenance and reliever therapy: an effective asthma treatment option? Vogelmeier, C., D'Urzo, A., Pauwels, R., Merino, J.M., Jaspal, M., Boutet, S., Naya, I., Price, D. Eur. Respir. J. (2005) [Pubmed]
  6. Choices of therapy for exercise-induced asthma in children. Price, J.F. Allergy (2001) [Pubmed]
  7. Formoterol--where does it fit in the current guidelines? Pauwels, R. Respiratory medicine. (2001) [Pubmed]
  8. Interaction between glucocorticoids and beta2 agonists on bronchial airway smooth muscle cells through synchronised cellular signalling. Roth, M., Johnson, P.R., Rüdiger, J.J., King, G.G., Ge, Q., Burgess, J.K., Anderson, G., Tamm, M., Black, J.L. Lancet (2002) [Pubmed]
  9. Exosites: their current status, and their relevance to the duration of action of long-acting beta 2-adrenoceptor agonists. Coleman, R.A., Johnson, M., Nials, A.T., Vardey, C.J. Trends Pharmacol. Sci. (1996) [Pubmed]
  10. Effects of treatment with formoterol on bronchoprotection against methacholine. Lipworth, B., Tan, S., Devlin, M., Aiken, T., Baker, R., Hendrick, D. Am. J. Med. (1998) [Pubmed]
  11. Opposing actions of (R,R)-isomers and (S,S)-isomers of formoterol on T-cell function. Steinke, J.W., Baramki, D., Borish, L. J. Allergy Clin. Immunol. (2006) [Pubmed]
  12. Effects of beta2-agonists on resident and infiltrating inflammatory cells. Johnson, M. J. Allergy Clin. Immunol. (2002) [Pubmed]
  13. Biphasic effect-time courses in man after formoterol inhalation: eosinopenic and hypokalemic effects and inhibition of allergic skin reactions. Derks, M.G., van den Berg, B.T., van der Zee, J.S., Braat, M.C., van Boxtel, C.J. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
  14. Low dose formoterol administration improves muscle function in dystrophic mdx mice without increasing fatigue. Harcourt, L.J., Schertzer, J.D., Ryall, J.G., Lynch, G.S. Neuromuscul. Disord. (2007) [Pubmed]
  15. IGF-1 is downregulated in experimental cancer cachexia. Costelli, P., Muscaritoli, M., Bossola, M., Penna, F., Reffo, P., Bonetto, A., Busquets, S., Bonelli, G., Lopez-Soriano, F.J., Doglietto, G.B., Argilés, J.M., Baccino, F.M., Fanelli, F.R. Am. J. Physiol. Regul. Integr. Comp. Physiol. (2006) [Pubmed]
  16. Anti-allergic activities of the beta-adrenoceptor stimulant formoterol (BD 40A). Tomioka, K., Yamada, T., Ida, H. Archives internationales de pharmacodynamie et de thérapie. (1981) [Pubmed]
  17. Prolonged bronchodilating effect of formoterol versus procaterol in bronchial asthma. Chetta, A., Del Donno, M., Maiocchi, G., Pisi, G., Moretti, D., Olivieri, D. Annals of allergy. (1993) [Pubmed]
  18. Inhaled formoterol in the prevention of exercise-induced bronchoconstriction in asthmatic children. Boner, A.L., Spezia, E., Piovesan, P., Chiocca, E., Maiocchi, G. Am. J. Respir. Crit. Care Med. (1994) [Pubmed]
  19. Effect of solution and suspension type aerosol of formoterol on tremor response and airways in patients with asthma. Bauer, K., Sertl, K., Kaik, B., Kaik, G. J. Allergy Clin. Immunol. (1995) [Pubmed]
  20. Effects of budesonide and formoterol on eosinophil activation induced by human lung fibroblasts. Spoelstra, F.M., Kauffman, H.F., Hovenga, H., Noordhoek, J.A., de Monchy, J.G., Postma, D.S. Am. J. Respir. Crit. Care Med. (2000) [Pubmed]
  21. Systemic effects of formoterol and salmeterol: a dose-response comparison in healthy subjects. Guhan, A.R., Cooper, S., Oborne, J., Lewis, S., Bennett, J., Tattersfield, A.E. Thorax (2000) [Pubmed]
  22. Effects of budesonide and formoterol on NF-kappaB, adhesion molecules, and cytokines in asthma. Wilson, S.J., Wallin, A., Della-Cioppa, G., Sandström, T., Holgate, S.T. Am. J. Respir. Crit. Care Med. (2001) [Pubmed]
  23. Anti-edema action of formoterol in rat trachea does not depend on capsaicin-sensitive sensory nerves. Sulakvelidze, I., McDonald, D.M. Am. J. Respir. Crit. Care Med. (1994) [Pubmed]
  24. A long-term study of the antiinflammatory effect of low-dose budesonide plus formoterol versus high-dose budesonide in asthma. Kips, J.C., O'Connor, B.J., Inman, M.D., Svensson, K., Pauwels, R.A., O'Byrne, P.M. Am. J. Respir. Crit. Care Med. (2000) [Pubmed]
  25. Comparison of the relative efficacy of formoterol and salmeterol in asthmatic patients. Palmqvist, M., Ibsen, T., Mellén, A., Lötvall, J. Am. J. Respir. Crit. Care Med. (1999) [Pubmed]
  26. Bronchodilation and bronchoprotection in asthmatic preschool children from formoterol administered by mechanically actuated dry-powder inhaler and spacer. Nielsen, K.G., Bisgaard, H. Am. J. Respir. Crit. Care Med. (2001) [Pubmed]
  27. Effect of beta 2-agonists on histamine-induced airway microvascular leakage in ozone-exposed guinea pigs. Inoue, H., Aizawa, H., Matsumoto, K., Shigyo, M., Takata, S., Hara, M., Hara, N. Am. J. Respir. Crit. Care Med. (1997) [Pubmed]
  28. Binding pockets of the beta(1)- and beta(2)-adrenergic receptors for subtype-selective agonists. Isogaya, M., Sugimoto, Y., Tanimura, R., Tanaka, R., Kikkawa, H., Nagao, T., Kurose, H. Mol. Pharmacol. (1999) [Pubmed]
  29. Formoterol. An update of its pharmacological properties and therapeutic efficacy in the management of asthma. Bartow, R.A., Brogden, R.N. Drugs (1998) [Pubmed]
  30. Additive anti-inflammatory effect of formoterol and budesonide on human lung fibroblasts. Spoelstra, F.M., Postma, D.S., Hovenga, H., Noordhoek, J.A., Kauffman, H.F. Thorax (2002) [Pubmed]
  31. Budesonide and formoterol inhibit ICAM-1 and VCAM-1 expression of human lung fibroblasts. Spoelstra, F.M., Postma, D.S., Hovenga, H., Noordhoek, J.A., Kauffman, H.F. Eur. Respir. J. (2000) [Pubmed]
  32. A randomized, double-blind trial of the effect of treatment with formoterol on clinical and inflammatory parameters of asthma in children. Stelmach, I., Gorski, P., Jerzynska, J., Stelmach, W., Majak, P., Kuna, P. Ann. Allergy Asthma Immunol. (2002) [Pubmed]
  33. Expression of inwardly rectifying potassium channels (GIRKs) and beta-adrenergic regulation of breast cancer cell lines. Plummer, H.K., Yu, Q., Cakir, Y., Schuller, H.M. BMC Cancer (2004) [Pubmed]
  34. Effect of inhaled formoterol and budesonide on exacerbations of asthma. Formoterol and Corticosteroids Establishing Therapy (FACET) International Study Group. Pauwels, R.A., Löfdahl, C.G., Postma, D.S., Tattersfield, A.E., O'Byrne, P., Barnes, P.J., Ullman, A. N. Engl. J. Med. (1997) [Pubmed]
  35. Association between beta 2-adrenoceptor polymorphism and susceptibility to bronchodilator desensitisation in moderately severe stable asthmatics. Tan, S., Hall, I.P., Dewar, J., Dow, E., Lipworth, B. Lancet (1997) [Pubmed]
  36. Regular formoterol treatment in mild asthma. Effect on bronchial responsiveness during and after treatment. Yates, D.H., Sussman, H.S., Shaw, M.J., Barnes, P.J., Chung, K.F. Am. J. Respir. Crit. Care Med. (1995) [Pubmed]
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