李富春, 孙秀君, 胡文辉, 任民峰. 大鼠蛛网膜下腔联合注射kappa受体激动剂和NMDA受体拮抗剂协同镇痛J. 药学学报, 1994, 29(12): 881-886.
引用本文: 李富春, 孙秀君, 胡文辉, 任民峰. 大鼠蛛网膜下腔联合注射kappa受体激动剂和NMDA受体拮抗剂协同镇痛J. 药学学报, 1994, 29(12): 881-886.
FC Li, XJ Sun, WH Hu , MF Jen, . INTRATHECAL CO-ADMINISTRATION OF KAPPA OPIOID RECEPTOR AGONISTS AND NMDA RECEPTOR ANTAGONISTS INDUCES SYNERGISTIC ANALGESIA IN RATSJ. Acta Pharmaceutica Sinica, 1994, 29(12): 881-886.
Citation: FC Li, XJ Sun, WH Hu , MF Jen, . INTRATHECAL CO-ADMINISTRATION OF KAPPA OPIOID RECEPTOR AGONISTS AND NMDA RECEPTOR ANTAGONISTS INDUCES SYNERGISTIC ANALGESIA IN RATSJ. Acta Pharmaceutica Sinica, 1994, 29(12): 881-886.

大鼠蛛网膜下腔联合注射kappa受体激动剂和NMDA受体拮抗剂协同镇痛

INTRATHECAL CO-ADMINISTRATION OF KAPPA OPIOID RECEPTOR AGONISTS AND NMDA RECEPTOR ANTAGONISTS INDUCES SYNERGISTIC ANALGESIA IN RATS

  • 摘要: 以大鼠热辐射甩尾潜伏期为测痛指标,蛛网膜下腔(it)联合注射非镇痛剂量的kappa阿片受体激动剂强啡肽(dynorphin,Dyn)A-(1-13)5nmol或U50488H(trans-(±)-3,4-dichloro-N-methyl-2-(1-pyrrolidinyl)-cyclohexyl-benzeneacetamide)100nmol和N-methyl-D-aspartate(NMDA)受体拮抗剂DL-2-amino-5-phosphonovalericacid(APv)10 nmol 或 kynurenicacid (KYN) 50 nmol 有显著的协同镇痛效应,其效应与NMDA受体拮抗剂呈一定量效关系。Kappa阿片受体特异性拮抗剂nor-binaltorphi-mine(nor-BNI)15nmolit可完全翻转Dyn A-(1-13)5nmol和APv10nmol及U50488H100nmol和KYN50nmol的协同镇痛。说明协同作用是通过kappa受体和谷氨酸能神经元之间的相互作用实现的。

     

    Abstract: It is reported that intrathecal(it)injection of low dose of dynorphin(Dyn)induces no analgesia while high dose of Dyn induces analgesia and might lead to hindlimb paralysis andloss of reflex via NMDA receptor.We hypothesized that NMDA receptor antagonists may reveal kappa analgesic-potential of subliminal dose of Dyn. Twenty-four hours after intrathecal cannulation,tailflick latency was measured before and after it of drugs. Combination of Dyn A-(1-13)5 nmol orU50488H 100 nmol,a kappa receptor agonist with either DL-2-amino-5-phosphonovaleric acid(5 and10 nmol)or kynurenic acid(25 and 50 nmol)it induced synergistic analgesia,which was reversed bynor-binaltorphimine 15 nmol,a kappa receptor antagonist.It is concluded that kappa opioid receptoragonists and NMDA receptor antagonists synergistically induce analgesia via interaction with theirreceptors.

     

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