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 language | English (US) |
---|---|
Pages (from-to) | 717-722 |
Number of pages | 6 |
Journal | Peptides |
Volume | 21 |
Issue number | 5 |
DOIs | |
State | Published - May 2000 |
Externally published | Yes |
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