The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
Chemical Compound Review

CHEMBL99869     4-[(E)-2-[[[2,4-dichloro-3- [[2-methyl-4...

Synonyms: SureCN5936739, CHEBI:258876, AC1NSK0Q, FR190997, L024093
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of FR190997


High impact information on FR190997


Chemical compound and disease context of FR190997


Biological context of FR190997

  • FR190997 induced concentration-dependent PI hydrolysis in IMR-90 cells with a pD2 of 8.4+/-0.1, and this effect was inhibited by Hoe 140 [5].
  • The lack of capability of FR190997 to activate or to bind the double mutant W256A/Y295F suggests that these residues are part of the same binding site, which is also important for receptor activation by the nonpeptide ligand [6].
  • 2. Intradermal injection of FR190997 (0.03 - 3 nmol site(-1)) into dorsal skin of rats increased vascular permeability in a dose-dependent manner [7].

Anatomical context of FR190997


Associations of FR190997 with other chemical compounds

  • Indomethacin (10 mg/kg, i.p. 30 min before) inhibited the response to FR190997, suggesting that release of prostaglandins induced by the B2 agonistic action might be involved in this inflammatory process induced by FR190997 [2].

Gene context of FR190997

  • These data indicate FR190997 and relaxin 3 as selective agonists for hB(2)R and hGPR100, respectively, and support the concept that different agonists may specifically bias the conformational states of a receptor to result in a final common G protein coupling, which is differentially recognized by antagonists [11].
  • A different molecular interaction of bradykinin and the synthetic agonist FR190997 with the human B2 receptor: evidence from mutational analysis [6].
  • 6. In mice sponge implants, topical application of FR190997 increased angiogenesis and granulation with enhanced expressions of basic fibroblast growth factor (bFGF) and vascular endothelial growth factor (VEGF) mRNAs [7].
  • 5 FR190997, a nonpeptide B(2) agonist, which was infused (10 microg kg(-1) h(-1)) into the vena cava of BN-Ka rats for 24 h with an osmotic mini-pump, caused significant reduction in the size of MI (38+/-3%), in comparison with the size in vehicle solution-treated rats (51+/-3%) [12].
  • However FR190997 produces a long lasting desensitisation both to itself and to LBK and it did not prove possible to protect against this using the high affinity antagonist at B2 receptors, Hoe 140 [9].

Analytical, diagnostic and therapeutic context of FR190997


  1. A nonpeptide mimic of bradykinin blunts the development of hypertension in young spontaneously hypertensive rats. Majima, M., Hayashi, I., Inamura, N., Fujita, T., Ogino, M. Hypertension (2000) [Pubmed]
  2. FR190997, a novel bradykinin B2 agonist, expresses longer action than bradykinin in paw edema formation and hypotensive response. Ueno, A., Naraba, H., Kojima, F., Morita, E., Oh-ishi, S. Immunopharmacology (1999) [Pubmed]
  3. Potentiation of the vascular response to kinins by inhibition of myocardial kininases. Dendorfer, A., Wolfrum, S., Schäfer, U., Stewart, J.M., Inamura, N., Dominiak, P. Hypertension (2000) [Pubmed]
  4. Nonpeptide mimic of bradykinin with long-acting properties at the bradykinin B2 receptor. Aramori, I., Zenkoh, J., Morikawa, N., Asano, M., Hatori, C., Sawai, H., Kayakiri, H., Satoh, S., Inoue, T., Abe, Y., Sawada, Y., Mizutani, T., Inamura, N., Nakahara, K., Kojo, H., Oku, T., Notsu, Y. Mol. Pharmacol. (1997) [Pubmed]
  5. Pharmacological characterization of a nonpeptide bradykinin B2 receptor antagonist, FR165649, and agonist, FR190997. Asano, M., Hatori, C., Sawai, H., Johki, S., Inamura, N., Kayakiri, H., Satoh, S., Abe, Y., Inoue, T., Sawada, Y., Mizutani, T., Oku, T., Nakahara, K. Br. J. Pharmacol. (1998) [Pubmed]
  6. A different molecular interaction of bradykinin and the synthetic agonist FR190997 with the human B2 receptor: evidence from mutational analysis. Bellucci, F., Meini, S., Cucchi, P., Catalani, C., Reichert, W., Zappitelli, S., Rotondaro, L., Quartara, L., Giolitti, A., Maggi, C.A. Br. J. Pharmacol. (2003) [Pubmed]
  7. Proinflammatory characteristics of a nonpeptide bradykinin mimic, FR190997, in vivo. Hayashi, I., Ishihara, K., Kumagai, Y., Majima, M. Br. J. Pharmacol. (2001) [Pubmed]
  8. Nonpeptide mimic of bradykinin with long-acting properties. Aramori, I., Zenkoh, J., Morikawa, N., Asano, M., Hatori, C., Sawai, H., Kayakiri, H., Satoh, S., Inoue, T., Abe, Y., Sawada, Y., Mizutani, T., Inamura, N., Iwami, M., Nakahara, K., Kojo, H., Oku, T., Notsu, Y. Immunopharmacology (1999) [Pubmed]
  9. Anion secretory effects of a non-peptide mimic of bradykinin (FR190997) on mouse colon epithelium. Cuthbert, A.W. Immunopharmacology (1999) [Pubmed]
  10. Migratory responses of polymorphonuclear leukocytes to kinin peptides. Paegelow, I., Trzeczak, S., Böckmann, S., Vietinghoff, G. Pharmacology (2002) [Pubmed]
  11. Bradykinin B2 and GPR100 receptors: a paradigm for receptor signal transduction pharmacology. Meini, S., Bellucci, F., Cucchi, P., Giuliani, S., Quartara, L., Giolitti, A., Zappitelli, S., Rotondaro, L., Boels, K., Maggi, C.A. Br. J. Pharmacol. (2004) [Pubmed]
  12. Bradykinin inhibits development of myocardial infarction through B2 receptor signalling by increment of regional blood flow around the ischaemic lesions in rats. Ito, H., Hayashi, I., Izumi, T., Majima, M. Br. J. Pharmacol. (2003) [Pubmed]
WikiGenes - Universities