Parallel bioassay of 39 tachykinins on 11 smooth muscle preparations. Structure and receptor selectivity/affinity relationship

  • Severini C
  • Salvadori S
  • Guerrini R
 et al. 
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Abstract

Parallel bioassay on smooth muscle preparations demonstrated that: all TKs having a neutral or basic residue at position 7 from the C-terminus show a clear-cut preference for the NK1 TK receptor, reinforced by the presence of the aromatic doublet Phe-Phe or Phe-Tyr (aromatic TKs); all aliphatic TKs (Phe-Ile/Val) having an acidic residue at position 7 show a clear-cut preference for NK2/NK3 receptors, generally without selectivity for a single receptor. However, in aromatic TKs having the same acidic residue, the preference for NK2/NK3 receptors is weakened, with a more or less pronounced co-preference for the NK1 receptor. Amino acid substitutions in the C-terminal tripeptide may influence receptor affinity. (C) 2000 Elsevier Science Inc.

Author-supplied keywords

  • Parallel bioassay
  • Smooth muscle preparations
  • Structure/Receptor selectivity relationship
  • Tachykinins

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Authors

  • Cinzia Severini

  • Severo Salvadori

  • Remo Guerrini

  • Giuliana Falconieri-Erspamer

  • Giuseppina Mignogna

  • Vittorio Erspamer

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