Rossi G C, Leventhal L, Pasternak G W
Cotzias Laboratory of Neuro-Oncology Memorial Sloan-Kettering Cancer Center, New York, NY 10021, USA.
Eur J Pharmacol. 1996 Sep 12;311(2-3):R7-8. doi: 10.1016/0014-2999(96)00578-x.
Orphanin FQ, also known as nociceptin, is a heptadecapeptide with very high affinity for a novel member of the cloned opioid receptor family which produces hyperalgesia in mice. In addition to hyperalgesia, which is observed soon after administration of orphanin FQ, we now describe a delayed analgesic response. Unlike orphanin FQ-induced hyperalgesia, orphanin FQ-induced analgesia is readily reversed by the opioid antagonist naloxone, implying an opioid mechanism of action. In view of the very poor affinity of orphanin FQ for all the known traditional opioid receptors and the low affinity of opioids for the 125I[Tyr14]orphanin FQ binding site, orphanin FQ-induced analgesia is probably mediated through a novel orphanin FQ receptor subtype.
孤啡肽FQ,也称为痛敏肽,是一种十七肽,对克隆的阿片受体家族的一个新成员具有非常高的亲和力,该受体在小鼠中会产生痛觉过敏。除了在给予孤啡肽FQ后很快就会出现的痛觉过敏外,我们现在还描述了一种延迟的镇痛反应。与孤啡肽FQ诱导的痛觉过敏不同,孤啡肽FQ诱导的镇痛作用很容易被阿片拮抗剂纳洛酮逆转,这意味着其作用机制为阿片类机制。鉴于孤啡肽FQ对所有已知传统阿片受体的亲和力非常低,以及阿片类药物对125I[酪氨酸14]孤啡肽FQ结合位点的亲和力也很低,孤啡肽FQ诱导的镇痛作用可能是通过一种新的孤啡肽FQ受体亚型介导的。