Tachykinin Antagonists with Cyclic Structures

  • E. Escher
  • P. D’Orléans-Juste
  • S. Dion
  • D. Regoli
Conference paper


During the last years, huge efforts have been made to upgrade the available tachykinin antagonists. We and several groups have done design studies with purely synthetic permutation series [1,2], others have attempted mathematical predictions based on various physicochemical considerations [3] but in no case antagonists with pA2-values above 8 were obtained or which satisfied all pharmacological criteria of selectivity and specificity.


Aromatic Amino Acid Adipic Acid Linear Precursor Bridgehead Position Kinin Antagonist 
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  1. 1.
    Regoli D, Escher E, and Mizrahi J (1984) Substance P - Structure-Activity studies and the development of antagonists. Pharmacology 28:301–320PubMedCrossRefGoogle Scholar
  2. 2.
    Folkers K, Hörig J, Rampold E, Lane P, Rosell S, Björkroth U (1982) Design and synthesis of effective antagonists of substance P. Acta Chern Scand B36:389–395CrossRefGoogle Scholar
  3. 3.
    Momany F, Personal communicationGoogle Scholar
  4. 4.
    Regoli D, Escher E, Drapeau G, D’OrleansJuste P, Mizrahi J (1984) Receptors for substance P III. Classification by competitive antagonists. Eur J Pharmacol 97:179–189PubMedCrossRefGoogle Scholar
  5. 5.
    Escher E, D’Orléans-Juste P, Dion S, Drapeau G, Mizrahi J, Regoli D (1984) A substance P antagonist not containing D-tryptophan. Eur J Pharmacol 105:375–377PubMedCrossRefGoogle Scholar
  6. 6.
    Schiller PW, Eggimann B, DiMaio J, Lemieux C, Nguyen TMD (1981) Cyclic enkephalin analogs containing a cysteine bridge. Biochem Biophys Res Comm 101:337–343PubMedCrossRefGoogle Scholar
  7. 7.
    Schiller PW, Nguyen TMD, Miller J (1985) Synthesis of sidechain to sidechain cyclized peptide analogs on solid supports. Int J Peptide Protein Res 25:171–177CrossRefGoogle Scholar
  8. 8.
    Siemion IZ, Szeweczuk Z (1981) To the problem of biologically active conformation of enkephalin. Mol Cell Biochem 34:23–29PubMedCrossRefGoogle Scholar
  9. 9.
    Escher E, Bernier M, Parent P (1983) Angiotensin II analogues. Part II. Synthesis and incorporation of the sulfur-containing aromatic amino acids: L-(4’-SH)Phe,L-(4’-SO2NH2)Phe, L-(4’-SO3-)Phe and L-(4’-SCH3)Phe. Helv Chim Acta 66:1355–1365CrossRefGoogle Scholar
  10. 10.
    Laczko E, Escher E (1981) Synthesis of photoaffinity labelling analogues of the peptide hormone bradykinin. Helv Chim Acta 64:621–627CrossRefGoogle Scholar
  11. 11.
    Regoli D, Drapeau G, Dion Sand D’OrléansJuste P. Receptors for neurokinins in peripheral organs. This issue pp.Google Scholar

Copyright information

© Springer-Verlag New York Inc. 1987

Authors and Affiliations

  • E. Escher
    • 1
  • P. D’Orléans-Juste
    • 1
  • S. Dion
    • 1
  • D. Regoli
    • 1
  1. 1.Department of Pharmacology, Faculty of MedicineUniversity of SherbrookeSherbrookeCanada

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