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Chemical Compound Review

SureCN7018004     (2S,5S)-2,5-bis(3,4,5- trimethoxyphenyl)oxo...

Synonyms: CHEBI:169517, KST-1A0233, AC1L3GQQ, CTK8E0293, AR-1A3586, ...
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Disease relevance of L 652731

  • When L-652,731 was added to the antibody employed in the reversed passive Arthus reaction, the injury resulting from immune complex-induced vasculitis was significantly attenuated [1].
  • The same L-652,731-dosing regimen inhibited immune complex-stimulated hypotension (87%), extravasation (77%), and vascular lysosomal hydrolase release (31%) [2].
  • L-652,731 when orally administered to rats (20 mg/kg, 1.5 hr before PAF infusion) inhibited PAF-induced hypotension (69%), extravasation (76%), vascular lysosomal hydrolase release (79%), and neutropenia (73%) [2].
  • To evaluate if PAF has a major role in promoting glomerular inflammatory reaction and fibrin deposition, we studied the effect of a molecule, L-652,731, which blocks the PAF receptor, on the evolution of an experimental model of anti-glomerular basement membrane (anti-GBM) glomerulonephritis (GN) [3].
  • PAF-induced proteinuria was prevented by L-652,731, a specific PAF receptor antagonist, suggesting that PAF's effect on glomerular permeability to proteins is likely to be related to its biologic activity [4].

High impact information on L 652731

  • With this model, we demonstrated that the effects of neutrophil reconstitution are substantially diminished if the cells are pretreated with L-652,731 and then washed [1].
  • The antagonists WEB 2086 and L-652,731 had no effect on neutrophil migration across resting EC induced by formylmethionyl-leucyl-phenylalanine (FMLP) [5].
  • The PAF induction of the acetyltransferase was less sensitive to inhibition by the specific PAF receptor antagonist L-652,731 than was PAF-induced degranulation [6].
  • Intratracheal instillation of anti-IL-1 beta plus L-652,731 resulted in reduction in lung vascular permeability and retarded net pulmonary neutrophil recruitment [7].
  • In contrast, L-652,731 had little effect on MDP-induced IL-1 synthesis in the absence of exogenous paf [8].

Chemical compound and disease context of L 652731


Biological context of L 652731

  • L-652,731 is orally active; it inhibits PAF-induced rat cutaneous vascular permeability with an ED50 of 30 mg/kg orally [11].
  • The most potent PAF antagonist in this group of compounds is trans-2,5-bis(3,4,5-trimethoxyphenyl)tetrahydrofuran (L-652,731, 14) with an IC50 of 0.02 microM [12].
  • Platelet aggregation induced by the thrombin-like enzymes could not be inhibited by PAF antagonists-BN 52021, kadsurenone or L-652,731 [13].
  • Scatchard analysis of the binding data indicated that no significant change in the dissociation constant (Kd) and maximum number of binding sites (Bmax) occurred after preincubation of platelet membrane with L 652731, whereas a reduction of Bmax was observed when PAF and BN 52021 were measured [14].
  • In addition, L-652,731 completely restored macrophage phagocytosis, partially improved macrophage killing and significantly inhibited leukopenia [15].

Anatomical context of L 652731

  • When the paf receptor antagonist, L-652,731 was added to monocytes, it prevented the enhancement of IL-1 activity induced by exogenous paf [8].
  • 5. The potencies of L-652,731 and BN 52021 were also markedly less (2 log units) for the macrophage receptors than for platelet or PMNL receptors and BN 52021 was more potent than L-652,731 in the macrophages [16].
  • 1. The effects of the platelet activating factor (Paf) antagonists alprazolam, BN 52021, kadsurenone, L 652,731 and SRI 63119 have been studied on Paf-induced chemiluminescence (CL) of guinea-pig, C. parvum-activated peritoneal macrophages in vitro [17].
  • When membranes were extensively washed, full recovery of specific [3H]PAF binding was attained with L 652731 and partial recoveries (60%, 55% and 30%) were reached with BN 52021, WEB 2086 and PAF, respectively; no recovery was seen with the dioxolanes BN 52111 and BN 52115 [14].
  • The addition of L-652,731 and L-653,150, two synthetic PAF-specific receptor antagonists, to 72 hour cultures of phytohemagglutinin (PHA)-stimulated human peripheral blood mononuclear leukocytes (PBML) caused a dose-dependent inhibition of (3H)-thymidine incorporation into T-cells (IC50: 25 microM and 3.2 microM, respectively) [18].

Associations of L 652731 with other chemical compounds


Gene context of L 652731

  • Subplantar co-injection of PAF antagonist, BN 52021 or L 652731, with cardiotoxin had no effect on paw oedema, whereas superoxide dismutase/catalase reduced this oedematous response [21].
  • Inhibition of neutrophil and eosinophil chemotactic responses to PAF by the PAF-antagonists WEB-2086, L-652,731, and SRI-63441 [22].
  • Under the same conditions L-652,731 at the concentration of 5 x 10(-6) mol/litre inhibited (P less than .01) the eosinophil chemotactic response to 10(-8) and 10(-9) mol PAF per litre [22].
  • We investigated the effects of PAF infusions in unanesthetized sheep and the effects of the PAF receptor antagonist L-652,731 [trans-2,5-bis(3,4,5-trimethoxyphenyl)tetrahydrofuran] on the hematologic, hemodynamic and biochemical alterations produced by infusions of both ZAP and PAF [9].
  • PAF receptor antagonists (L-652,731, WEB2086, and FR900452) at up to 10 nmol per tube had no affect on the SPRIA [23].

Analytical, diagnostic and therapeutic context of L 652731


  1. Evidence for the role of platelet-activating factor in immune complex vasculitis in the rat. Warren, J.S., Mandel, D.M., Johnson, K.J., Ward, P.A. J. Clin. Invest. (1989) [Pubmed]
  2. Platelet-activating factor (PAF) mediation of rat anaphylactic responses to soluble immune complexes. Studies with PAF receptor antagonist L-652,731. Doebber, T.W., Wu, M.S., Biftu, T. J. Immunol. (1986) [Pubmed]
  3. Platelet activating factor (PAF) as a mediator of injury in nephrotoxic nephritis. Bertani, T., Livio, M., Macconi, D., Morigi, M., Bisogno, G., Patrono, C., Remuzzi, G. Kidney Int. (1987) [Pubmed]
  4. Effect of platelet-activating factor and its specific receptor antagonist on glomerular permeability to proteins in isolated perfused rat kidney. Perico, N., Delaini, F., Tagliaferri, M., Abbate, M., Cucchi, M., Bertani, T., Remuzzi, G. Lab. Invest. (1988) [Pubmed]
  5. Neutrophil migration across monolayers of cytokine-prestimulated endothelial cells: a role for platelet-activating factor and IL-8. Kuijpers, T.W., Hakkert, B.C., Hart, M.H., Roos, D. J. Cell Biol. (1992) [Pubmed]
  6. Platelet-activating factor (PAF) stimulates the PAF-synthesizing enzyme acetyl-CoA:1-alkyl-sn-glycero-3-phosphocholine O2-acetyltransferase and PAF synthesis in neutrophils. Doebber, T.W., Wu, M.S. Proc. Natl. Acad. Sci. U.S.A. (1987) [Pubmed]
  7. Relationship between interleukin-1 beta and platelet-activating factor in the pathogenesis of acute immune complex alveolitis in the rat. Warren, J.S. Am. J. Pathol. (1992) [Pubmed]
  8. Immunoregulatory functions of paf-acether. IV. Enhancement of IL-1 production by muramyl dipeptide-stimulated monocytes. Salem, P., Deryckx, S., Dulioust, A., Vivier, E., Denizot, Y., Damais, C., Dinarello, C.A., Thomas, Y. J. Immunol. (1990) [Pubmed]
  9. Effects of L-652,731, a platelet-activating factor (PAF) receptor antagonist, on PAF- and complement-induced pulmonary hypertension in sheep. Smallbone, B.W., Taylor, N.E., McDonald, J.W. J. Pharmacol. Exp. Ther. (1987) [Pubmed]
  10. Effect of the PAF antagonists, CV-3988 and L-652,731 on the pulmonary and hematological responses to guinea pig anaphylaxis. Danko, G., Sherwood, J.E., Grissom, B., Kreutner, W., Chapman, R.W. Pharmacological research communications. (1988) [Pubmed]
  11. trans-2,5-Bis-(3,4,5-trimethoxyphenyl)tetrahydrofuran. An orally active specific and competitive receptor antagonist of platelet activating factor. Hwang, S.B., Lam, M.H., Biftu, T., Beattie, T.R., Shen, T.Y. J. Biol. Chem. (1985) [Pubmed]
  12. Conformation and activity of tetrahydrofuran lignans and analogues as specific platelet activating factor antagonists. Biftu, T., Gamble, N.F., Doebber, T., Hwang, S.B., Shen, T.Y., Snyder, J., Springer, J.P., Stevenson, R. J. Med. Chem. (1986) [Pubmed]
  13. Comparison of the platelet aggregation induced by three thrombin-like enzymes of snake venoms and thrombin. Teng, C.M., Ko, F.N. Thromb. Haemost. (1988) [Pubmed]
  14. Reversible or irreversible modification of [3H]PAF binding on rabbit platelet membranes differentiates various PAF receptor antagonists. Domingo, M.T., Piro, F., Broquet, C., Auclair, E., Chabrier, P.E., Braquet, P. Lipids (1992) [Pubmed]
  15. Platelet activating factor involvement in splanchnic artery occlusion shock in rats. Squadrito, F., Sturniolo, R., Altavilla, D., Santoro, G., Campo, G.M., Arena, A., Caputi, A.P. Eur. J. Pharmacol. (1991) [Pubmed]
  16. Characterization of receptors for platelet-activating factor on platelets, polymorphonuclear leukocytes and macrophages. Stewart, A.G., Dusting, G.J. Br. J. Pharmacol. (1988) [Pubmed]
  17. Antagonism of platelet activating factor-induced chemiluminescence in guinea-pig peritoneal macrophages in differing states of activation. Parnham, M.J., Bittner, C., Lambrecht, G. Br. J. Pharmacol. (1989) [Pubmed]
  18. Platelet-activating factor (PAF) receptor antagonists inhibit mitogen-induced human peripheral blood T-cell proliferation. Patrignani, P., Valitutti, S., Aiello, F., Musiani, P. Biochem. Biophys. Res. Commun. (1987) [Pubmed]
  19. Stimulation of neutrophil adherence to vascular endothelial cells by histamine and thrombin and its inhibition by PAF antagonists and dexamethasone. Watanabe, M., Yagi, M., Omata, M., Hirasawa, N., Mue, S., Tsurufuji, S., Ohuchi, K. Br. J. Pharmacol. (1991) [Pubmed]
  20. Granulocyte chemotaxis in the canine trachea: inhibition by lipid mediator antagonists and systemic inhibitors. Johnson, H.G., McNee, M.L. Agents Actions (1991) [Pubmed]
  21. Effect of anti-inflammatory drugs on the cardiotoxin-induced hind-paw oedema in rats. Wang, J.P., Teng, C.M. J. Pharm. Pharmacol. (1990) [Pubmed]
  22. Inhibition of neutrophil and eosinophil chemotactic responses to PAF by the PAF-antagonists WEB-2086, L-652,731, and SRI-63441. Håkansson, L., Venge, P. J. Leukoc. Biol. (1990) [Pubmed]
  23. Development of a novel scintillation proximity radioimmunoassay for platelet-activating factor measurement: comparison with bioassay and GC/MS techniques. Sugatani, J., Lee, D.Y., Hughes, K.T., Saito, K. Life Sci. (1990) [Pubmed]
  24. A specific antagonist of platelet-activating factor suppresses oedema formation in an Arthus reaction but not oedema induced by leukocyte chemoattractants in rabbit skin. Hellewell, P.G., Williams, T.J. J. Immunol. (1986) [Pubmed]
  25. A study of PAF-induced ocular inflammation in the rat and its inhibition by the PAF antagonist, L-652,731. Gautheron, P.D., Coulbault, L., Sugrue, M.F. J. Pharm. Pharmacol. (1987) [Pubmed]
  26. Platelet-activating factor mediates endotoxin-induced acute renal insufficiency in rats. Wang, J., Dunn, M.J. Am. J. Physiol. (1987) [Pubmed]
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