An enzymatically stable kyotorphin analog induces pain in subattomol doses

Hiroshi Ueda, Makoto Inoue, Grazyna Weltrowska, Peter W. Schiller

Research output: Contribution to journalArticlepeer-review

Abstract

Intraplantar injection of the enzymatically stable, N-methylated kyotorphin analog Tyr(NMe)-Arg-OH produced marked and sharp nociceptive flexor responses in a dose-dependent manner. A significant response was observed with this compound at a dose of 0.01 amol (6000 molecules). Tyr(NMe)-Arg-OH-nociception was completely blocked by the kyotorphin antagonist leucyl-arginine and its enzymatically stable, N-methylated analog, as well as by CP-99994, a specific neurokinin 1 antagonist. These findings suggest that the nociceptive effect produced by Tyr(NMe)-Arg-OH in subattomol doses occurs via specific interaction with the kyotorphin receptor and that the extraordinary potency observed may result from amplification through local substance P release. Copyright (C) 2000 Elsevier Science Inc.

Original languageEnglish (US)
Pages (from-to)717-722
Number of pages6
JournalPeptides
Volume21
Issue number5
DOIs
StatePublished - May 2000
Externally publishedYes

Keywords

  • Kyotorphin
  • Kyotorphin analogs
  • Kyotorphin antagonists
  • Nociception
  • Peripheral nociception assay
  • Subattomol potency
  • Substance P

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Endocrinology
  • Cellular and Molecular Neuroscience

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