Correlation Engine 2.0
Clear Search sequence regions

  • bn 50739 (1)
  • cell (2)
  • cmi 392 (1)
  • edema (3)
  • erythema (2)
  • factor receptor (1)
  • female (1)
  • furans (2)
  • G Protein (2)
  • glycoproteins (2)
  • guinea pigs (2)
  • human (2)
  • leukotrienes (1)
  • membrane (2)
  • mice (4)
  • mk 287 (2)
  • PAF (5)
  • paf receptor (5)
  • platelet (3)
  • rats (2)
  • receptors (4)
  • urea (2)
  • zileuton (2)
  • Sizes of these terms reflect their relevance to your search.

    Leukotrienes (LTs) and platelet-activating factor (PAF) are important mediators of inflammation and allergy. LDP-392, a novel dual PAF receptor antagonist and 5-lipoxygenase (5-LO) inhibitor, has been identified. LDP-392 is 17.9-fold more potent than zileuton (5-LO inhibitor) in the RBL cytosolic 5-LO assay, and equally potent as MK 287 (PAF receptor antagonist) in the human platelet PAF receptor binding assay. The in vivo dual activities of LDP-392 were confirmed by measuring the inhibition of ex vivo LTB(4)production in rats and PAF-induced hemoconcentration in mice. Intravenous administration of LDP-392 demonstrated greater inhibition than zileuton, BN 50739 or MK 287 on arachidonic acid-induced ear edema and protected mice from LPS-induced lethality. Topical administration of LDP-392, in a dose-dependent manner, inhibited TPA-induced ear edema in mice and UVB-induced erythema in guinea-pigs. These data suggest that LDP-392, as a dual PAF receptor antagonist and 5-LO inhibitor, may be of greater clinical effectiveness. Copyright 2001 Academic Press.


    C Qian, S B Hwang, L Libertine-Garahan, J B Eckman, X Cai, R T Scannell, C G Yeh. Anti-inflammatory activities of LDP-392, a dual PAF receptor antagonist and 5-lipoxygenase inhibitor. Pharmacological research. 2001 Sep;44(3):213-20

    Expand section icon Mesh Tags

    Expand section icon Substances

    PMID: 11529688

    View Full Text