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Chemical Compound Review

CHEMBL8747     1-[3-(quinolin-2- ylmethoxy)phenyl]hexan-1-ol

Synonyms: REV-901, SureCN678489, REV-5901, AG-K-25644, BSPBio_001522, ...
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Disease relevance of Rev 5901


High impact information on Rev 5901

  • In addition, the 5-lipoxygenase inhibitor RG 5901 (1 or 10 mg/kg i.v.) produced a two-thirds attenuation in PAF priming [4].
  • Described in this first report are the structure-activity relationships that led to a more than a 20-fold improvement of the potency and selectivity of the initial chemical lead (RG 5901) [5].
  • On the other hand, the leukotriene (LT) B(4) receptor antagonist U-75302, the LTD(4) receptor antagonists LY-171883 and MK-571, and the cysteinyl-LT receptor antagonist REV-5901 also inhibit cell proliferation and [(3)H]-thymidine incorporation in a concentration-dependent manner, and delay the RAW 264.7 cell cycle [6].
  • However, the pulmonary infiltration of neutrophils and eosinophils induced by antigen was unaltered by prior treatment with PF 5901 (10 mg) [7].
  • 2. While PF 5901 (10 mg) had no significant effect on the acute bronchoconstriction induced by antigen, this dose was sufficient to inhibit significantly the increase in airway responsiveness to inhaled histamine 24 h following antigen challenge (P < 0.05) [7].

Biological context of Rev 5901

  • REV-5901 also inhibited the calcium ionophore-induced release of immunoreactive leukotrienes from human lung in vitro with IC50 values of 11.7 +/- 2.2 MicroM versus peptide leukotrienes and 10.0 +/- 1.1 microM versus iLTB4 [8].
  • The physicochemical basis of improvement of the bioavailability of a poorly water-soluble drug [REV 5901; alpha-pentyl-3-(2-quinolinylmethoxy)benzenemethanol; 1] after oral administration as organic solutions was investigated [9].
  • The indices of hypoxic vasoconstriction were not affected by RG 5901 [3].

Anatomical context of Rev 5901


Associations of Rev 5901 with other chemical compounds


Gene context of Rev 5901


Analytical, diagnostic and therapeutic context of Rev 5901

  • 3. Total leucocyte infiltration into the airways induced by antigen, as assessed by bronchoalveolar lavage, was significantly inhibited by pretreatment with PF 5901 (10 mg) [7].


  1. Exacerbation of experimental colitis by nonsteroidal anti-inflammatory drugs is not related to elevated leukotriene B4 synthesis. Wallace, J.L., Keenan, C.M., Gale, D., Shoupe, T.S. Gastroenterology (1992) [Pubmed]
  2. PF-5901 inhibits gastrointestinal platelet-activating factor synthesis in vivo. Hogaboam, C.M., Donigi-Gale, D., Shoupe, T.S., Wallace, J.L. Eur. J. Pharmacol. (1992) [Pubmed]
  3. Antagonism of leukotriene receptors and administration of a 5-lipoxygenase inhibitor do not affect hypoxic vasoconstriction. Thomas, H.M., Sourour, M.S., Lopez, D., Foster, S.H. Lung (1989) [Pubmed]
  4. Priming interactions between platelet activating factor and histamine in the in vivo microcirculation. Tomeo, A.C., Egan, R.W., Durán, W.N. FASEB J. (1991) [Pubmed]
  5. Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 1. Initial structure-activity relationships. Youssefyeh, R.D., Magnien, E., Lee, T.D., Chan, W.K., Lin, C.J., Galemmo, R.A., Johnson, W.H., Tan, J., Campbell, H.F., Huang, F.C. J. Med. Chem. (1990) [Pubmed]
  6. Role of 5-lipoxygenase pathway in the regulation of RAW 264.7 macrophage proliferation. Nieves, D., Moreno, J.J. Biochem. Pharmacol. (2006) [Pubmed]
  7. Effect of a 5-lipoxygenase inhibitor and leukotriene antagonist (PF 5901) on antigen-induced airway responses in neonatally immunized rabbits. Herd, C.M., Donigi-Gale, D., Shoupe, T.S., Burroughs, D.A., Yeadon, M., Page, C.P. Br. J. Pharmacol. (1994) [Pubmed]
  8. Inhibition by REV-5901 of leukotriene release from guinea-pig and human lung tissue in vitro. Kusner, E.J., Marks, R.L., Aharony, D., Krell, R.D. Biochem. Pharmacol. (1989) [Pubmed]
  9. Physicochemical basis of increased bioavailability of a poorly water-soluble drug following oral administration as organic solutions. Serajuddin, A.T., Sheen, P.C., Mufson, D., Bernstein, D.F., Augustine, M.A. Journal of pharmaceutical sciences. (1988) [Pubmed]
  10. Comparison of antioxidant and nonantioxidant lipoxygenase inhibitors on neutrophil function. Implications for pathogenesis of myocardial reperfusion injury. Shappell, S.B., Taylor, A.A., Hughes, H., Mitchell, J.R., Anderson, D.C., Smith, C.W. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  11. Platelet-activating factor synthesis by peritoneal mast cells and its inhibition by two quinoline-based compounds. Hogaboam, C.M., Donigi-Gale, D., Shoupe, T.S., Bissonnette, E.Y., Befus, A.D., Wallace, J.L. Br. J. Pharmacol. (1992) [Pubmed]
  12. An examination of the influence of the epithelium on contractile responses to peptidoleukotrienes and blockade by ICI 204,219 in isolated guinea pig trachea and human intralobar airways. Buckner, C.K., Fedyna, J.S., Robertson, J.L., Will, J.A., England, D.M., Krell, R.D., Saban, R. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  13. Neutrophil infiltration into the ischaemic/reperfused rabbit isolated myocardium: effect of PF-5901 and cycloheximide. Lad, N., Williams, T.J., Booth, R.F. Eur. J. Pharmacol. (1992) [Pubmed]
  14. Myocardial salvage induced by REV-5901: an inhibitor and antagonist of the leukotrienes. Mullane, K., Hatala, M.A., Kraemer, R., Sessa, W., Westlin, W. J. Cardiovasc. Pharmacol. (1987) [Pubmed]
  15. In vitro synthesis of 12-hydroxy-eicosatetraenoic acid is increased in uninvolved psoriatic epidermis. Kragballe, K., Desjarlais, L., Duell, E.A., Voorhees, J.J. J. Invest. Dermatol. (1986) [Pubmed]
  16. Effects of 5-lipoxygenase inhibitors on interleukin production by human synovial tissues in organ culture: comparison with interleukin-1-synthesis inhibitors. Rainsford, K.D., Ying, C., Smith, F. J. Pharm. Pharmacol. (1996) [Pubmed]
  17. Leukotrienes mediate 5-hydroxytryptamine-induced plasma extravasation in the rat knee joint via CysLT-type receptors. Wang, Y., Mitchell, J., Sharma, M., Gabriel, A., Moriyama, K., Palmer, P.P. Inflamm. Res. (2004) [Pubmed]
  18. REV 5901 and Ly 171,883 protect rat gastric mucosa against ethanol-induced damage. Nielsen, S.T., Beninati, L., Chang, J. Agents Actions (1987) [Pubmed]
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