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Chemical Compound Review

FK-888     (2S,4R)-N-[(1S)-1-(benzyl- methyl...

Synonyms: SureCN8079679, FK888, LS-193299, FK 888, PDSP2_000648, ...
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Disease relevance of FK-888


High impact information on FK-888

  • The purpose of this study was to investigate the importance of tachykinins in exercise-induced airway narrowing in patients with asthma using a selective neurokinin 1-receptor (NK1-receptor) antagonist, FK-888 [2].
  • Inhalation of FK-888 had no significant effect on baseline SGaw [2].
  • However, FK 888 at concentrations of 10(-7) and 10(-6) M decreased the number of coughs without effect on bronchoconstriction [3].
  • Full NK-1-like susceptibility to SR 140,333, FK 888, and CP 96,345 could be transferred to the NK-3 receptor by exchange of transmembrane segments V and VI and adjacent parts with corresponding segments from the NK-1 receptor [4].
  • Surprisingly, exchange of the four divergent residues located around the previously located apparent binding site for CP 96,345 and FK 888 at the top of transmembrane segment (TM) V and VI, either alone or as a group, did not affect the binding of these nonpeptide compounds [5].

Biological context of FK-888


Anatomical context of FK-888

  • 4. FK 888 (1-30 microM) did not induce histamine release from rat peritoneal mast cells [6].
  • 1. 3. FK 888 (1 nM-100 microM) was without effect on the electrically-evoked, cholinergic response of the rabbit iris sphincter and the electrically-evoked, sympathetic response of the guinea-pig vas deferens [6].
  • Phosphoramidon significantly potentiated plasma extravasation in the trachea and main bronchi, whereas FK-888 significantly inhibited that extravasation in a dose-related manner [9].
  • Plasma and ileal SP concentrations, ileal muscle SP receptor binding and SP-induced contractions in isolated ileum were investigated 3 and 14 days post-irradiation and FK 888 treatment [10].

Associations of FK-888 with other chemical compounds

  • The co-injection of the selective neurokinin (NK) NK(2) (SR 48968, 0.05-0.5 nmol/paw), and to a lesser extent the selective NK(1) (FK 888, 0.25-1.0 nmol/paw) receptor antagonists, resulted in a significant inhibition of glutamate-induced nociception [11].
  • The effect of SP was antagonised by two selective antagonists of NK1 receptors, namely (+/-) CP 96,345 (10(-10)-10(-8) M) and FK 888 (10(-9)-10(-7) M), while the NK2 receptor antagonist MEN 10627 (10(-8)-10(-7) M) was not effective [12].
  • The selective NK1 tachykinin antagonist (FK 888), but not NK2 (SR 48968) antagonized substance P-induced contraction, but both drugs failed to effect Phyllanthus urinaria-induced contraction [13].
  • The intradermal (i.d.) injection of NK1 receptor antagonists GR 82334 and FK 888 (1-50 pmol/paw), in association with formalin, produced graded inhibition of the early but not the late phase of the formalin test [14].
  • The increase in IP1 was greatly reduced, at approximately the same extent by the 10 min pretreatment with a concentration of (+/-)CP 96,345 (100 nM) 10 times smaller than that of FK 888 and GR 82,334 (1 microM) [15].

Gene context of FK-888

  • In contrast, FK 888 (1.0 mg/kg, i.v. and 500 pmol/site) was ineffective in the response to SP [16].
  • We examined the effect of SR 140333, a nonpeptide NK1 receptor antagonist, FK 888, a peptide NK1 antagonist, and SR 142801, a non-peptide NK3 antagonist, on ear oedema induced by topical application of capsaicin (250 micrograms/ear) in mice [16].
  • The NK1 receptor selective antagonists, SR 140,333 (0.1 microM), FK 888 (10 microM) RP 67,580 (1 microM) and GR 82,334 (10 microM) were also without effect (n = 4-5) [17].
  • The aim of this study was to investigate the effect of a SP receptor blockade by FK 888 on gut SP levels and contractile properties after rat irradiation [10].


  1. Inhibition of emesis by tachykinin NK1 receptor antagonists in Suncus murinus (house musk shrew). Rudd, J.A., Ngan, M.P., Wai, M.K. Eur. J. Pharmacol. (1999) [Pubmed]
  2. A neurokinin 1-receptor antagonist improves exercise-induced airway narrowing in asthmatic patients. Ichinose, M., Miura, M., Yamauchi, H., Kageyama, N., Tomaki, M., Oyake, T., Ohuchi, Y., Hida, W., Miki, H., Tamura, G., Shirato, K. Am. J. Respir. Crit. Care Med. (1996) [Pubmed]
  3. Role of substance P in cough during bronchoconstriction in awake guinea pigs. Sekizawa, K., Ebihara, T., Sasaki, H. Am. J. Respir. Crit. Care Med. (1995) [Pubmed]
  4. Evidence for a common molecular mode of action for chemically distinct nonpeptide antagonists at the neurokinin-1 (substance P) receptor. Gether, U., Emonds-Alt, X., Brelière, J.C., Fujii, T., Hagiwara, D., Pradier, L., Garret, C., Johansen, T.E., Schwartz, T.W. Mol. Pharmacol. (1994) [Pubmed]
  5. The species selectivity of chemically distinct tachykinin nonpeptide antagonists is dependent on common divergent residues of the rat and human neurokinin-1 receptors. Jensen, C.J., Gerard, N.P., Schwartz, T.W., Gether, U. Mol. Pharmacol. (1994) [Pubmed]
  6. Investigation of the specificity of FK 888 as a tachykinin NK1 receptor antagonist. Wang, Z.Y., Tung, S.R., Strichartz, G.R., Håkanson, R. Br. J. Pharmacol. (1994) [Pubmed]
  7. Comparative, general pharmacology of SDZ NKT 343, a novel, selective NK1 receptor antagonist. Walpole, C.S., Brown, M.C., James, I.F., Campbell, E.A., McIntyre, P., Docherty, R., Ko, S., Hedley, L., Ewan, S., Buchheit, K.H., Urban, L.A. Br. J. Pharmacol. (1998) [Pubmed]
  8. Role of substance P in experimental allergic conjunctivitis in guinea pigs. Yamaji, M., Takada, M., Fujiwara, R., Ohishi, H., Izushi, K., Sugimoto, Y., Kamei, C. Methods and findings in experimental and clinical pharmacology. (1997) [Pubmed]
  9. Esophageal stimulation by hydrochloric acid causes neurogenic inflammation in the airways in guinea pigs. Hamamoto, J., Kohrogi, H., Kawano, O., Iwagoe, H., Fujii, K., Hirata, N., Ando, M. J. Appl. Physiol. (1997) [Pubmed]
  10. A substance P receptor antagonist (FK 888) modifies gut alterations induced by ionizing radiation. Esposito, V., Linard, C., Wysocki, J., Griffiths, N.M., Mathe, D. Int. J. Radiat. Biol. (1998) [Pubmed]
  11. The role of neuropeptides and capsaicin-sensitive fibres in glutamate-induced nociception and paw oedema in mice. Beirith, A., Santos, A.R., Calixto, J.B. Brain Res. (2003) [Pubmed]
  12. The tachykinin NK1 receptor mediates the migration-promoting effect of substance P on human skin fibroblasts in culture. Parenti, A., Amerini, S., Ledda, F., Maggi, C.A., Ziche, M. Naunyn Schmiedebergs Arch. Pharmacol. (1996) [Pubmed]
  13. Analysis of the mechanisms underlying the contractile response induced by the hydroalcoholic extract of Phyllanthus urinaria in the guinea-pig urinary bladder in-vitro. Dias, M.A., Campos, A.H., Cechinel Filho, V., Yunes, R.A., Calixto, J.B. J. Pharm. Pharmacol. (1995) [Pubmed]
  14. Further evidence for the involvement of tachykinin receptor subtypes in formalin and capsaicin models of pain in mice. Santos, A.R., Calixto, J.B. Neuropeptides (1997) [Pubmed]
  15. Effect of the non-peptide blocker (+/-) CP 96,345 on the cellular mechanism involved in the response to NK1 receptor stimulation in human skin fibroblasts. Ziche, M., Parenti, A., Amerini, S., Zawieja, D., Maggi, C.A., Ledda, F. Neuropeptides (1996) [Pubmed]
  16. Effect of the tachykinin receptor antagonists, SR 140333, FK 888, and SR 142801, on capsaicin-induced mouse ear oedema. Inoue, H., Nagata, N., Koshihara, Y. Inflamm. Res. (1996) [Pubmed]
  17. Evidence that tachykinin NK2 receptors modulate resting tone in the rat isolated small intestine. Maggi, C.A., Giuliani, S. Br. J. Pharmacol. (1996) [Pubmed]
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