Peripheral orphanin FQ/nociceptin analgesia in the mouse.
Peripheral orphanin FQ/nociceptin analgesia in the mouse.
复制标题
小鼠外周孤啡肽 FQ/伤害感受肽镇痛。
DOI：
10.1016/s0024-3205(99)00149-6
复制
发表时间：
1999
期刊：
影响因子：
6.1
通讯作者：
Pasternak,GW
中科院分区：
文献类型：
--
作者：
Kolesnikov,YA;Pasternak,GW
孤啡肽/孤啡肽（OFQ/N）外周给药对小鼠甩尾有镇痛作用（ED_（50）16.3 μg），作用高峰在5 min，持续30 min，而纳洛酮苯甲酰腙外周给药也有镇痛作用（ED_（50）3.8 μg）。两种药物的镇痛作用均被纳洛酮阻断。OFQ/N（1-11）和OFQ/N（1-7）均无明显外周活性。针对鼠孤儿阿片受体（KOR-3）的反义映射两种化合物证实了该克隆在其作用中的重要性。针对第二和第三编码外显子的反义探针显著降低了两种化合物的镇痛作用。而靶向第一外显子的反义寡核苷酸仅阻断OFQ/N的镇痛作用，而不阻断κ 3镇痛作用。
Orphanin FQ/Nociceptin (OFQ/N) administered peripherally was an effective analgesic in the tailflick test in mice (ED5016.3 μg) It had a peak effect at 5 min and lasted up to 30 min. The kappa3analgesic naloxone benzoylhydrazone was also active peripherally (ED503.8 μg). The analgesic actions of both agents were blocked by naloxone. Neither OFQ/N(1–11) nor OFQ/N(1–7) had appreciable peripheral activity. Antisense mapping both compounds against the murine orphan opioid receptor (KOR-3) confirmed the importance of this clone in their actions. Antisense probes targeting the second and third coding exons significantly lowered the analgesic effects of both compounds. However, the antisense targeting the first coding exon blocked only the actions of OFQ/N and not kappa3analgesia.