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Chemical Compound Review

CHEMBL130517     (E)-3-(6-acetamidopyridin-3- yl)-N-[[[2,4...

Synonyms: SureCN3718364, FK-3657, CHEBI:317036, AC1NSK08, DNC009756, ...
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Disease relevance of FR173657


High impact information on FR173657

  • FR167344 and FR173657 inhibited the B2 receptor-mediated phosphatidylinositol (PI) hydrolysis and produced a concentration-dependent rightward shift in the dose-response curve to bradykinin [5].
  • Estimated pA2 values for the antagonism of bradykinin-induced PI hydrolysis by FR167344 and FR173657 were 8.0 and 9.0, respectively [5].
  • MEN16132, and the other reference antagonists, inhibited only one portion of BK specific binding, and the rank order of potency was (pIC(50)): Icatibant (lung 10.7; ileum 10.2)=MEN11270 (lung 10.4; ileum 9.9)=MEN16132 (lung 10.5; ileum 9.9). > LF16-0687 (lung 8.9; ileum 8.8) > FR173657 (lung 8.6; ileum 8.2) [6].
  • 2. To this end we have tested the effects of the B2 receptor antagonists Hoe 140, FR173657 or FR172357 on the pleural inflammatory response triggered by intrapleural ( injection of allergen (ovalbumin, 12 microg cavity(-1)) in 14 day-actively sensitized Wistar rats [7].
  • FR173657 had no effect on B1 receptor-mediated relaxations in response to des-Arg9-BK [8].

Chemical compound and disease context of FR173657


Biological context of FR173657


Anatomical context of FR173657

  • 2. Contractions of the isolated ileum of the guinea-pig in response to BK were inhibited by FR173657 (10-300 nM) in a concentration-dependent manner [8].
  • FR173657 was a competitive antagonist in the rat uterus but showed a deviation from competitive inhibition in the other preparations studied similar to other second generation peptide antagonists [8].
  • The oral administration of FR173657 to rats (30 mg kg-1, 1 h before carrageenin) significantly (by 50-77%) blunted the plasma exudation 1, 3, 5, and 7 h after carrageenin, causing a significant parallel reduction (by 42-57%) in the volume of exudates [12].
  • 3. The concentration-response curves for B2 receptor-mediated relaxations of the rat isolated duodenum induced by BK were shifted to the right together with a concomitant reduction of the maximum BK effect in the presence of FR173657 (10-300 nM) [8].
  • In sensitized guinea pigs pretreated with phosphoramidon, FR173657 (20 mg/kg, p.o.) inhibited plasma extravasation evoked by ovalbumin aerosol (5%, 2 min) by 77+/-14.2% in the trachea and 65+/-11.2% in the main bronchi [13].

Associations of FR173657 with other chemical compounds

  • 4. In guinea-pig isolated preparations, FR173657 antagonized BK-induced contractions with an IC50 of 7.9 x 10(-9) M, but did not antagonize acetylcholine or histamine-induced contractions even at a concentration of 10(-6) M [9].
  • 1. Effects of an orally active non-peptide (BK) B2 receptor antagonist, FR173657 ((E)-3-(6-acetamido-3-pyridyl)-N-[N-[2,4-dichloro-3-[(2-methyl-8-quinoli nyl) oxymethyl]phenyl]-N-methylaminocarbonylmethyl] acrylamide) on the plasma exudation in rat carrageenin-induced pleurisy were investigated [12].
  • The latency in B/N-Kitasato rat was prolonged by administration of a bradykinin (BK) B2 receptor antagonist, FR173657 (30 mg/kg, p.o.), whereas it was shortened by pretreatment with a kininase II inhibitor, captopril (10 mg/kg, i.p.). Both agents did not affect the latency in B/N-Katholiek rats [14].

Gene context of FR173657


Analytical, diagnostic and therapeutic context of FR173657


  1. The nonpeptide B2 receptor antagonist FR173657: inhibition of effects of bradykinin related to its role in nociception. Griesbacher, T., Amann, R., Sametz, W., Diethart, S., Juan, H. Br. J. Pharmacol. (1998) [Pubmed]
  2. Effects of FR173657, a non-peptide B2 antagonist, on kinin-induced hypotension, visceral and peripheral oedema formation and bronchoconstriction. Griesbacher, T., Legat, F.J. Br. J. Pharmacol. (1997) [Pubmed]
  3. Inhibition of guinea pig skin allergic reactions by nonpeptide bradykinin B2 receptor antagonist FR173657. Mori, T., Imamura, T. Int. Arch. Allergy Immunol. (1998) [Pubmed]
  4. Bradykinin B2 receptor antagonist FR173657 ameliorates small bowel ischemia-reperfusion injury in dogs. Arakawa, K., Takeyoshi, I., Akao, Y., Totsuka, O., Matsumoto, K., Morishita, Y. Dig. Dis. Sci. (2005) [Pubmed]
  5. Novel subtype-selective nonpeptide bradykinin receptor antagonists FR167344 and FR173657. Aramori, I., Zenkoh, J., Morikawa, N., O'Donnell, N., Asano, M., Nakamura, K., Iwami, M., Kojo, H., Notsu, Y. Mol. Pharmacol. (1997) [Pubmed]
  6. Comparative antagonist pharmacology at the native mouse bradykinin B(2) receptor: radioligand binding and smooth muscle contractility studies. Meini, S., Cucchi, P., Bellucci, F., Catalani, C., Giuliani, S., Santicioli, P., Maggi, C.A. Br. J. Pharmacol. (2007) [Pubmed]
  7. Suppressive effect of distinct bradykinin B2 receptor antagonist on allergen-evoked exudation and leukocyte infiltration in sensitized rats. Bandeira-Melo, C., Calheiros, A.S., Silva, P.M., Cordeiro, R.S., Teixeira, M.M., Martins, M.A. Br. J. Pharmacol. (1999) [Pubmed]
  8. Effects of the non-peptide B2 antagonist FR173657 on kinin-induced smooth muscle contraction and relaxation, vasoconstriction and prostaglandin release. Griesbacher, T., Sametz, W., Legat, F.J., Diethart, S., Hammer, S., Juan, H. Br. J. Pharmacol. (1997) [Pubmed]
  9. The identification of an orally active, nonpeptide bradykinin B2 receptor antagonist, FR173657. Asano, M., Inamura, N., Hatori, C., Sawai, H., Fujiwara, T., Katayama, A., Kayakiri, H., Satoh, S., Abe, Y., Inoue, T., Sawada, Y., Nakahara, K., Oku, T., Okuhara, M. Br. J. Pharmacol. (1997) [Pubmed]
  10. Role of bradykinin B2 receptors in the modulation of the peristaltic reflex of the guinea pig isolated ileum. Chan, S.K., Rudd, J.A. Eur. J. Pharmacol. (2006) [Pubmed]
  11. Suppression of dextran sulfate sodium-induced colitis in kininogen-deficient rats and non-peptide B2 receptor antagonist-treated rats. Kamat, K., Hayashi, I., Mizuguchi, Y., Arai, K., Saeki, T., Ohno, T., Saigenji, K., Majima, M. Jpn. J. Pharmacol. (2002) [Pubmed]
  12. Effects of an orally active non-peptide bradykinin B2 receptor antagonist, FR173657, on plasma exudation in rat carrageenin-induced pleurisy. Majima, M., Kawashima, N., Hiroshi, I., Katori, M. Br. J. Pharmacol. (1997) [Pubmed]
  13. Effects of the orally active non-peptide bradykinin B2 receptor antagonist, FR173657, on plasma extravasation in guinea pig airways. Watanabe, M., Yoshihara, S., Abe, T., Oyama, M., Arisaka, O. Eur. J. Pharmacol. (1999) [Pubmed]
  14. Role of kinin and prostaglandin in cutaneous thermal nociception. Matsuzaki, S., Hayashi, I., Nara, Y., Kamata, K., Yamanaka, M., Okamoto, H., Hoka, S., Majima, M. Int. Immunopharmacol. (2002) [Pubmed]
  15. Roles of bradykinin in vascular permeability and angiogenesis in solid tumor. Ishihara, K., Kamata, M., Hayashi, I., Yamashina, S., Majima, M. Int. Immunopharmacol. (2002) [Pubmed]
  16. Effects of a bradykinin B(2) receptor antagonist on ischemia-reperfusion injury in a canine lung transplantation model. Hashimoto, N., Takeyoshi, I., Tsutsumi, H., Sunose, Y., Tokumine, M., Totsuka, O., Ohwada, S., Matsumoto, K., Morishita, Y. J. Heart Lung Transplant. (2004) [Pubmed]
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