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Chemical Compound Review

AC1L4UEP     3-[(2S,8S,14S,17S)-8-benzyl- 5-(1H-indol-3...

Synonyms: L-659877, L-659,877, L 659877, L 659,877, Cyclo(gln-trp-phe-gly-leu-met)
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Disease relevance of L-659877

  • Epinastine could not block bronchospasm in the presence of 1 mg/kg NK2 receptor antagonist L 659877 or 20 microg/kg potassium channel blocker iberiotoxin, suggesting the epinastine was acting on a neurokinin- and potassium channel-mediated mechanism [1].

High impact information on L-659877


Biological context of L-659877


Anatomical context of L-659877


Associations of L-659877 with other chemical compounds

  • However, pretreatment with a peripheral NK-2-selective antagonists, L-659,877, attenuated the SP-induced responses but not the NKA-induced responses [11].
  • This response was blocked by concurrent intranigral administration of the NK-1 tachykinin receptor antagonist RP 67580 (2 nmol), but not by NK-2 (L-659,877) or NK-3 ([Trp7, beta-Ala8]NKA4-10) antagonists [12].
  • The NK2-selective antagonist L-659,877, at a dose of 10(-6) M, abolished the effect of SP (10(-8) M) without affecting basal phosphoinositide breakdown [13].
  • Evidence for activation of tachykinin NK1 and NK2 receptors by scyliorhinin I was obtained by using the selective tachykinin antagonists FK 888, MEN 10,376 and L 659,877 [14].
  • 3. The inhibitory effect on drinking observed after central injection of the NK-2 agonist, GR64349, was attenuated by co-administration of the NK-2 antagonist, L-659,877, but not by the NK-1 antagonist, GR82334 [15].

Gene context of L-659877

  • On the contrary, the NK-2 receptor antagonist L 659,877 (0.1-1 mumol/kg i.v.) abolished the effect of [beta Ala8] NK-A(4-10) (1 nmol/kg i.v.), but failed to affect the response to [Sar9]SP sulfone [16].
  • The NK2 receptor selective antagonist L-659,877 (cyclo[Leu-Met-Gln-Trp-Phe-Gly]) inhibited the stimulation of PI turnover and bladder contractions induced by all three tachykinins [17].
  • 4. Spantide (3 microM) selectively antagonized the SP-induced contraction while L-659,877 (3-10 microM) or MEN 10,376 (10-30 microM) which are NK2 receptor selective antagonists selectively blocked the response to NKA [18].
  • The non-selective NK receptor antagonist spantide I only slightly reduced the contractile response to NP gamma, as did the selective NK1 antagonist GR 82,334, and the selective NK2 antagonist L-659,877 and MEN 10,376 [19].

Analytical, diagnostic and therapeutic context of L-659877

  • The antagonists MEN 10,207 and L 659,877 inhibited the noncholinergic contraction to electrical stimulation in a concentration-dependent manner; L 668,169 and R 396 were poorly effective [20].


  1. The mechanism by which epinastine stops an adenosine analog from contracting BDE rat airways. Meade, C.J. Am. J. Respir. Crit. Care Med. (1998) [Pubmed]
  2. Nitric oxide enhances substance P-induced itch-associated responses in mice. Andoh, T., Kuraishi, Y. Br. J. Pharmacol. (2003) [Pubmed]
  3. Substance P induction of itch-associated response mediated by cutaneous NK1 tachykinin receptors in mice. Andoh, T., Nagasawa, T., Satoh, M., Kuraishi, Y. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  4. Effect of newly developed tachykinin agonist and antagonists on the guinea pig isolated gallbladder. Patacchini, R., Maggi, C.A. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  5. Tachykininergic transmission to the circular muscle of the guinea-pig ileum: evidence for the involvement of NK2 receptors. Bartho, L., Santicioli, P., Patacchini, R., Maggi, C.A. Br. J. Pharmacol. (1992) [Pubmed]
  6. Receptors mediating tachykinin-induced contractile responses in guinea-pig trachea. Ireland, S.J., Bailey, F., Cook, A., Hagan, R.M., Jordan, C.C., Stephens-Smith, M.L. Br. J. Pharmacol. (1991) [Pubmed]
  7. Effects of neuropeptides on the sumatriptan-disturbed circulation in the optic nerve head of rabbits. Gaspar, M.N., Ribeiro, C.A., Cunha-Vaz, J.G., Macedo, T.R. Pharmacology (2004) [Pubmed]
  8. In vivo role of the adenosine A3 receptor: N6-2-(4-aminophenyl)ethyladenosine induces bronchospasm in BDE rats by a neurally mediated mechanism involving cells resembling mast cells. Meade, C.J., Mierau, J., Leon, I., Ensinger, H.A. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  9. In vivo and in vitro pharmacology of SR 48,968, a non-peptide tachykinin NK2 receptor antagonist. Maggi, C.A., Patacchini, R., Giuliani, S., Giachetti, A. Eur. J. Pharmacol. (1993) [Pubmed]
  10. [125I]neurokinin A labels pharmacologically distinct populations of NK2 binding sites in hamster and rabbit urinary bladder. Guard, S., Pain, D., Franks, R., Watling, K.J. Eur. J. Pharmacol. (1993) [Pubmed]
  11. Identification of the central tachykinin receptor subclass involved in substance P-induced cardiovascular and behavioral responses in conscious rats. Itoi, K., Tschöpe, C., Jost, N., Culman, J., Lebrun, C., Stauss, B., Unger, T. Eur. J. Pharmacol. (1992) [Pubmed]
  12. Pharmacological characterization of grooming induced by a selective NK-1 tachykinin receptor agonist. Stoessl, A.J., Brackstone, M., Rajakumar, N., Gibson, C.J. Brain Res. (1995) [Pubmed]
  13. Effects of tachykinins on phosphoinositide metabolism in the hypothalamus: is the NK1 receptor involved? Lebrun, C.J., Wende, P., Steckelings, U., Itoi, K., Unger, T. Brain Res. (1993) [Pubmed]
  14. Effect of scyliorhinin I and synthetic scyliorhinin I derivatives at mammalian tachykinin NK1, NK2 and NK3 receptors. Patacchini, R., Quartara, L., Rolka, K., Zboinska, J., Kupryszewski, G., Maggi, C.A. Eur. J. Pharmacol. (1993) [Pubmed]
  15. Role of NK-2 receptors in the antidipsogenic activity of neurokinins in the mouse. Walsh, D.M., Elliott, P.J., Hagan, R.M. Gen. Pharmacol. (1992) [Pubmed]
  16. Evidence against a peripheral role of tachykinins in the initiation of micturition reflex in rats. Lecci, A., Giuliani, S., Patacchini, R., Maggi, C.A. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  17. Comparison of the effects of neuropeptide K and neuropeptide gamma with neurokinin A at NK2 receptors in the hamster urinary bladder. van Giersbergen, P.L., Shatzer, S.A., Burcher, E., Buck, S.H. Naunyn Schmiedebergs Arch. Pharmacol. (1992) [Pubmed]
  18. Tachykinin antagonists and capsaicin-induced contraction of the rat isolated urinary bladder: evidence for tachykinin-mediated cotransmission. Maggi, C.A., Patacchini, R., Santicioli, P., Giuliani, S. Br. J. Pharmacol. (1991) [Pubmed]
  19. Intestinal motility responses to neuropeptide gamma in vitro and in vivo in the rat: comparison with neurokinin 1 and neurokinin 2 receptor agonists. Rahman, M., Lördal, M., al-Saffar, A., Hellström, P.M. Acta Physiol. Scand. (1994) [Pubmed]
  20. Tachykinin antagonists inhibit nerve-mediated contractions in the circular muscle of the human ileum. Involvement of neurokinin-2 receptors. Maggi, C.A., Giuliani, S., Patacchini, R., Santicioli, P., Theodorsson, E., Barbanti, G., Turini, D., Giachetti, A. Gastroenterology (1992) [Pubmed]
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