Minami T, Okuda-Ashitaka E, Nishiuchi Y, Kimura T, Tachibana S, Mori H, Ito S
Department of Anesthesiology, Osaka Medical College, Takatsuki, Japan.
Br J Pharmacol. 1998 Jul;124(6):1016-8. doi: 10.1038/sj.bjp.0701995.
b-nocistatin is a heptadecapeptide produced from bovine prepronociceptin and blocks the induction of hyperalgesia and touch-evoked pain (allodynia) by intrathecal administration of nociceptin or prostaglandin E2 (PGE2). Human prepronociceptin may generate a 30-amino acid peptide different in length from b-nocistatin. Here, we examine whether the human putative counterpart of nocistatin (h-nocistatin) possessed the same biological activities as b-nocistatin. Simultaneous intrathecal injection of h-nocistatin in mice blocked the induction of allodynia by nociceptin and PGE2 in a dose-dependent manner with ID50 values of 329 pg kg(-1) and 16.6 ng kg(-1), respectively. h-nocistatin was about 10 times less potent than b-nocistatin. h-nocistatin also attenuated the nociceptin- and PGE2-induced hyperalgesia. These results demonstrate that h-nocistatin is biologically active and may be involved in the processing of pain at the spinal level in humans.
β-诺西汀是一种由牛前阿片黑素皮质素原产生的十七肽,通过鞘内注射诺西汀或前列腺素E2(PGE2)可阻断痛觉过敏和触觉诱发疼痛(异常性疼痛)的诱导。人前阿片黑素皮质素原可能产生一种长度与β-诺西汀不同的30个氨基酸的肽。在此,我们研究了诺西汀的人假定对应物(h-诺西汀)是否具有与β-诺西汀相同的生物学活性。在小鼠中同时鞘内注射h-诺西汀可剂量依赖性地阻断诺西汀和PGE2诱导的异常性疼痛,ID50值分别为329 pg kg(-1)和16.6 ng kg(-1)。h-诺西汀的效力比β-诺西汀低约10倍。h-诺西汀还可减轻诺西汀和PGE2诱导的痛觉过敏。这些结果表明,h-诺西汀具有生物学活性,可能参与人类脊髓水平的疼痛处理。