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Chemical Compound Review

FAROPAFANT     N',N'-dimethyl-N-(pyridin-3- ylmethyl)-N-[4...

Synonyms: Foropafant, CHEMBL1628662, SureCN7156608, ANW-71420, AC1L3OON, ...
 
 
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Disease relevance of SR27417

  • Stasis-induced thrombosis performed in the rabbit jugular vein was enhanced in a dose-dependent manner by the prior i.v. administration of LPS (0.05 to 100 micrograms/ kg, i.v.). SR 27417 administered simultaneously with LPS prevented thrombus formation with an ED50 value of 0.1 +/- 0.04 mg/kg [1].
  • These results confirm that PAF plays a major role in the development of cutaneous anaphylaxis and that SR 27417 may be an effective prophylactic drug [2].
  • SR 27417, a potent PAF receptor antagonist injected iv, reduced venous thrombosis in a dose-dependent manner (14, 29 and 63% inhibition after 1, 3 and 6 mg/kg respectively) [3].
  • Effect of SR 27417, a novel PAF antagonist on antigen-induced hypotension in the rat [4].
  • These results therefore confirm that PAF plays a major role in septic shock and that SR 27417 may be an effective prophylactic as well as a potent curative drug [5].
 

High impact information on SR27417

 

Chemical compound and disease context of SR27417

 

Biological context of SR27417

 

Anatomical context of SR27417

  • In conclusion, these data suggest that tracheal epithelial cells contain PAF-specific receptors and indicate that SR 27417 is an extremely potent PAF-receptor antagonist, as well as being a suitable radioligand for labelling PAF receptors on intact cells [10].
  • In conclusion, these data indicate that SR 27417 appears to be one of the most potent PAF receptor antagonists yet described, as well as a suitable radioligand for labelling PAF receptors on intact blood cells [14].
  • Effect of SR 27417 on the binding of [3H]PAF to rabbit and human platelets and human polymorphonuclear leukocytes [15].
  • In addition, a dose of apafant (1.5 mg/kg) that showed almost maximal effect when given 30 min before PAF, had lost most of its protective action by 3 h, while SR 27417 at a comparably effective dose (0.5 mg/kg) retained substantial ability to prevent gut lesions in all the GI tract segments investigated, 18 h after administration [16].
  • The platelet-specific agonist collagen (1 microg/mL) increased leukocyte CD11b expression from 2.94+/-0.52 to 3.81+/-0.58 (P:<0. 05); this was not inhibited by the thromboxane A(2) receptor antagonist ICI 192.605 or the PAF antagonist SR27417 [17].
 

Associations of SR27417 with other chemical compounds

 

Gene context of SR27417

  • Biochemical and pharmacological activities of SR 27417, a highly potent, long-acting platelet-activating factor receptor antagonist [12].
 

Analytical, diagnostic and therapeutic context of SR27417

References

  1. Hypoxia primes endotoxin-induced tissue factor expression in human monocytes and endothelial cells by a PAF-dependent mechanism. Herbert, J.M., Corseaux, D., Lale, A., Bernat, A. J. Cell. Physiol. (1996) [Pubmed]
  2. Effect of SR 27417 on oedema formation induced in rabbit skin by platelet-activating factor or antigen. Herbert, J.M., Laplace, M.C., Bernat, A., Salel, V., Maffrand, J.P. Eur. J. Pharmacol. (1992) [Pubmed]
  3. Effect of various drugs on adriamycin-enhanced venous thrombosis in the rat: importance of PAF. Bernat, A., Herbert, J.M. Thromb. Res. (1994) [Pubmed]
  4. Effect of SR 27417, a novel PAF antagonist on antigen-induced hypotension in the rat. Herbert, J.M., Bernat, A., Tibiriça, E. Journal of lipid mediators and cell signalling. (1997) [Pubmed]
  5. Protective effect of SR 27417, a novel PAF antagonist, on PAF- or endotoxin-induced hypotension in the rat and the guinea-pig. Bernat, A., Herbert, J.M., Salel, V., Lespy, L., Maffrand, J.P. Journal of lipid mediators. (1992) [Pubmed]
  6. Role of platelet-activating factor in Chinese hamster ovary cell responses to cholera toxin. Thielman, N.M., Marcinkiewicz, M., Sarosiek, J., Fang, G.D., Guerrant, R.L. J. Clin. Invest. (1997) [Pubmed]
  7. Role of platelet activating factor in the intestinal epithelial secretory and Chinese hamster ovary cell cytoskeletal responses to cholera toxin. Guerrant, R.L., Fang, G.D., Thielman, N.M., Fonteles, M.C. Proc. Natl. Acad. Sci. U.S.A. (1994) [Pubmed]
  8. Inhibition by platelet-activating factor of Src- and hepatocyte growth factor-dependent invasiveness of intestinal and kidney epithelial cells. Phosphatidylinositol 3'-kinase is a critical mediator of tumor invasion. Kotelevets, L., Noë, V., Bruyneel, E., Myssiakine, E., Chastre, E., Mareel, M., Gespach, C. J. Biol. Chem. (1998) [Pubmed]
  9. Platelet-activating factor induces NF-kappa B activation through a G protein-coupled pathway. Kravchenko, V.V., Pan, Z., Han, J., Herbert, J.M., Ulevitch, R.J., Ye, R.D. J. Biol. Chem. (1995) [Pubmed]
  10. Characterization of specific binding sites of 3H-labelled platelet-activating factor ([3H]PAF) and a new antagonist, [3H]SR 27417, on guinea-pig tracheal epithelial cells. Herbert, J.M. Biochem. J. (1992) [Pubmed]
  11. Pharmacological evidence for the putative existence of two different subtypes of PAF receptors on platelets and leukocytes; studies with yangambin. Herbert, J.M., Castro-Faria-Neto, H.C., Barbosa-Filho, J.M., Cordeiro, R.S., Tibiriça, E. Journal of lipid mediators and cell signalling. (1997) [Pubmed]
  12. Biochemical and pharmacological activities of SR 27417, a highly potent, long-acting platelet-activating factor receptor antagonist. Herbert, J.M., Bernat, A., Valette, G., Gigo, V., Lale, A., LaPlace, M.C., Lespy, L., Savi, P., Maffrand, J.P., Le Fur, G. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  13. In vitro inhibitory effect of SR 27417, a potent platelet-activating factor (PAF) receptor antagonist, on the PAF-induced bovine platelet aggregation. Bastos da Silva, M., Delaunois, A., Gustin, P., Godeau, J.M., Lekeux, P. Vet. Res. (2000) [Pubmed]
  14. Binding of [3H]SR 27417, a novel platelet-activating factor (PAF) receptor antagonist, to rabbit and human platelets and polymorphonuclear leukocytes. Herbert, J.M., Laplace, M.C., Maffrand, J.P. Biochem. Pharmacol. (1993) [Pubmed]
  15. Effect of SR 27417 on the binding of [3H]PAF to rabbit and human platelets and human polymorphonuclear leukocytes. Herbert, J.M., Laplace, M.C., Cailleau, C., Maffrand, J.P. Journal of lipid mediators. (1993) [Pubmed]
  16. Prevention of platelet-activating factor-induced gastrointestinal lesions in rats by the new specific antagonist N-(2-dimethylaminoethyl)-N-(3-pyridinylmethyl)[4-(2,4,6-triisopropylphe nyl) thiazol-2yl]amine. Giudice, A., Herbert, J.M., Maffrand, J.P., Manara, L., Manzoni, L., Le Fur, G. Arzneimittel-Forschung. (1996) [Pubmed]
  17. Platelet-leukocyte cross talk in whole blood. Li, N., Hu, H., Lindqvist, M., Wikström-Jonsson, E., Goodall, A.H., Hjemdahl, P. Arterioscler. Thromb. Vasc. Biol. (2000) [Pubmed]
  18. Ex vivo effects of SR 27417, a novel PAF antagonist, on rabbit platelet aggregation and [3H]-PAF binding. Herbert, J.M., Laplace, M.C., Maffrand, J.P. Journal of lipid mediators. (1992) [Pubmed]
 
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