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Chemical Compound Review

Veliflapon     (2R)-2-cyclopentyl-2-[4- (quinolin-2...

Synonyms: BAY-X-005, Bay-x-1005, Bay-X1005, Bayx-1005, CHEMBL88712, ...
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Disease relevance of Bay X1005


High impact information on Bay X1005


Biological context of Bay X1005

  • For BAY x 1005, the ratios of treatment C versus treatment A were 94% for Cmax and 101% for AUC tau [6].
  • An open, randomized, three-period crossover study was conducted to compare the steady-state pharmacokinetics, pharmacodynamics, and tolerability of concomitant administration of BAY x 1005 and theophylline in 12 healthy volunteers [6].
  • The antiproliferative properties of AA861 and BAY-X-1005 were associated with the occurrence of condensed nuclei, fragmented DNA, and changes in DNA content and cell cycle frequency distribution consistent with an apoptotic process [7].

Anatomical context of Bay X1005

  • Using mainly human polymorphonuclear leukocytes (PMNL) this study elucidates the mechanism of inhibition of 5-lipoxygenase (5-LOX, EC arachidonic acid metabolites by BAY X 1005 [5].
  • Compared to the inhibition of leukotriene synthesis in intact human PMNL about 800-fold higher concentrations of BAY X 1005 were required to inhibit leukotriene formation in a cell-free system suggesting that the inhibitory effect of BAY X 1005 cannot be explained by a direct effect on 5-LOX [5].
  • In all three assays, BAY Y 1015 was more potent than BAY X 1005, and for both compounds much higher concentrations were required to inhibit LT synthesis by whole blood compared to isolated neutrophils and eosinophils [8].
  • BAY X 1005 inhibits 5-LOX translocation from the cytosol to membranes and reverses 5-LOX translocation [9].

Associations of Bay X1005 with other chemical compounds

  • Pharmacokinetic parameters were derived from concentrations of BAY x 1005 and theophylline as measured by high-performance liquid chromatography in plasma collected before the morning dose on days 5 and 6 and at various times on day 7 of each period until 24 hours after drug administration [6].
  • Basal and LIT induced IL-1beta and TNF-alpha production were inhibited by Bay-x-1005 in a dose dependent manner, while the addition of NS-398 caused a potent stimulatory effect [10].
  • AIM: This study was performed to investigate the effects of indomethacin (cyclooxygenase inhibitor) and Bay x 1005 (5-lipoxygenase inhibitor) on MUC5AC release from human airways in vitro [11].
  • Furthermore, experiments were carried out in which the animals were conditioned with a combination of the H1/5-HT receptor antagonists pyrilamine and methysergide in addition to treatment with BAY X 1005 [2].
  • To further characterize the antiinflammatory properties of BAY X 1005 in the conditioned and unconditioned AA-MEIT, BAY X 1005 was tested in combination with the nitric oxide (NO) synthase inhibitor L-NAME, with the cyclooxygenase inhibitor indomethacin, and in combination with both compounds [2].

Gene context of Bay X1005

  • The effect of endogenous eicosanoids on basal and induced levels of IL-1beta, TNF-alpha, and MMP-1 synthesis was examined by incubating explants in the presence of NS-398 and Bay-x-1005 [10].
  • Potential anti-inflammatory effects of 5-lipoxygenase inhibition--exemplified by the leukotriene synthesis inhibitor BAY X 1005 [12].

Analytical, diagnostic and therapeutic context of Bay X1005


  1. Inhibition of 5-lipoxygenase-activating protein abrogates experimental liver injury: role of Kupffer cells. Titos, E., Clària, J., Planagumà, A., López-Parra, M., González-Périz, A., Gaya, J., Miquel, R., Arroyo, V., Rodés, J. J. Leukoc. Biol. (2005) [Pubmed]
  2. Antiedematous effects of combination therapies with the leukotriene synthesis inhibitor BAY X 1005 in the archidonic acid-induced mouse ear inflammation test. Burchardt, E.R., Müller-Peddinghaus, R. Prostaglandins Leukot. Essent. Fatty Acids (1997) [Pubmed]
  3. Clinical activity of leukotriene inhibitors. Harris, R.R., Carter, G.W., Bell, R.L., Moore, J.L., Brooks, D.W. Int. J. Immunopharmacol. (1995) [Pubmed]
  4. The effect of leukotriene synthesis inhibitors in models of acute and chronic inflammation. Nickerson-Nutter, C.L., Medvedeff, E.D. Arthritis Rheum. (1996) [Pubmed]
  5. Mode of action of the new selective leukotriene synthesis inhibitor BAY X 1005 ((R)-2-[4-(quinolin-2-yl-methoxy)phenyl]-2-cyclopentyl acetic acid) and structurally related compounds. Hatzelmann, A., Fruchtmann, R., Mohrs, K.H., Raddatz, S., Müller-Peddinghaus, R. Biochem. Pharmacol. (1993) [Pubmed]
  6. No pharmacokinetic or pharmacodynamic interaction between theophylline and the leukotriene biosynthesis inhibitor BAY x 1005. Groen, H., Moesker, H.L., Leeuwenkamp, O.R., Sollie, F.A., Jonkman, J.H. Journal of clinical pharmacology. (1996) [Pubmed]
  7. Inhibition of 5-lipoxygenase induces cell growth arrest and apoptosis in rat Kupffer cells: implications for liver fibrosis. Titos, E., Clària, J., Planagumà, A., López-Parra, M., Villamor, N., Párrizas, M., Carrió, A., Miquel, R., Jiménez, W., Arroyo, V., Rivera, F., Rodés, J. FASEB J. (2003) [Pubmed]
  8. Pharmacology of the 5-lipoxygenase inhibitors BAY Y 1015 and BAY X 1005 in the horse. Cunningham, F.M., Andrews, M., Landoni, M.F., Lees, P. J. Vet. Pharmacol. Ther. (1997) [Pubmed]
  9. Mode of action of the leukotriene synthesis (FLAP) inhibitor BAY X 1005: implications for biological regulation of 5-lipoxygenase. Hatzelmann, A., Fruchtmann, R., Mohrs, K.H., Raddatz, S., Matzke, M., Pleiss, U., Keldenich, J., Müller-Peddinghaus, R. Agents Actions (1994) [Pubmed]
  10. Synthesis of interleukin 1beta, tumor necrosis factor-alpha, and interstitial collagenase (MMP-1) is eicosanoid dependent in human osteoarthritis synovial membrane explants: interactions with antiinflammatory cytokines. He, W., Pelletier, J.P., Martel-Pelletier, J., Laufer, S., Di Battista, J.A. J. Rheumatol. (2002) [Pubmed]
  11. MUC5AC mucin release from human airways in vitro: effects of indomethacin and Bay X1005. Roger, P., Gascard, J.P., Bara, J., de Montpreville, V.T., Brink, C. Mediators of inflammation. (2001) [Pubmed]
  12. Potential anti-inflammatory effects of 5-lipoxygenase inhibition--exemplified by the leukotriene synthesis inhibitor BAY X 1005. Müller-Peddinghaus, R. J. Physiol. Pharmacol. (1997) [Pubmed]
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