An enzymatically stable kyotorphin analog induces pain in subattomol doses.
作者： Hiroshi Ueda , Makoto Inoue , Grazyna Weltrowska , Peter W Schiller
DOI: 10.1016/S0196-9781(00)00190-X
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摘要: 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 dose 0.01 amol (6000 molecules). Tyr(NMe)-Arg-OH-nociception completely blocked by antagonist leucyl-arginine its analog, as well CP-99994, specific neurokinin 1 antagonist. These findings suggest that effect subattomol doses occurs via interaction receptor extraordinary potency may result from amplification through local substance P release.
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