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Chemical Compound Review

AC1MIXH9     3-amino-3-[[(1S)-1-[[(1S)-1- [[(1S)-1...

Synonyms: Mdl 28564, Mdl 28,564, 127370-75-6, Asp-ser-phe-val-gly-leu-CH2NH-leu-NH2
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High impact information on Mdl 28564

  • The pseudopeptide derivative of NKA(4-10), MDL 28,564 behaved as a full or near-to-full agonist in both preparations, its EC50s being 474 nM and 55 nM in the ileum and colon, respectively [1].
  • On the other hand, MDL 28,564 had an agonist effect in the isolated gallbladder, its maximal effect approaching 58% of that to NKA [2].
  • Contractile responses to neurokinin A (NKA), neuropeptide gamma(NP gamma), and the NK2 receptor-selective analogs [Lys5,MeLeu9,Nle10]NKA(4-10) and MDL 28,564 were determined in the endothelium-denuded rabbit pulmonary artery [3].
  • MDL 28,564 also produced full contraction in rabbit pulmonary artery (NK2 tissue) but was inactive in rat vas deferens (NK2 tissue) [4].
  • [Leu9 psi(CH2NH)Leu10]-neurokinin A (4-10) (MDL 28,564) distinguishes tissue tachykinin peptide NK2 receptors [4].

Anatomical context of Mdl 28564


Gene context of Mdl 28564

  • The pseudopeptide, MDL 28,564, which is one of the most selective NK2 ligands available, behaved as a full agonist [6].


  1. Comparison of tachykinin NK1 and NK2 receptors in the circular muscle of the guinea-pig ileum and proximal colon. Maggi, C.A., Patacchini, R., Meini, S., Quartara, L., Sisto, A., Potier, E., Giuliani, S., Giachetti, A. Br. J. Pharmacol. (1994) [Pubmed]
  2. 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]
  3. Characterization of the tachykinin NK2 receptor subtype in the rabbit pulmonary artery. Xiao, X.H., Mussap, C.J., Burcher, E. Peptides (1992) [Pubmed]
  4. [Leu9 psi(CH2NH)Leu10]-neurokinin A (4-10) (MDL 28,564) distinguishes tissue tachykinin peptide NK2 receptors. Buck, S.H., Harbeson, S.L., Hassmann, C.F., Shatzer, S.A., Rouissi, N., Nantel, F., van Giersbergen, P.L. Life Sci. (1990) [Pubmed]
  5. Tachykinin receptors in the guinea-pig isolated bronchi. Maggi, C.A., Patacchini, R., Quartara, L., Rovero, P., Santicioli, P. Eur. J. Pharmacol. (1991) [Pubmed]
  6. NK2 tachykinin receptors and contraction of circular muscle of the human colon: characterization of the NK2 receptor subtype. Giuliani, S., Barbanti, G., Turini, D., Quartara, L., Rovero, P., Giachetti, A., Maggi, C.A. Eur. J. Pharmacol. (1991) [Pubmed]
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