Peripheral kappa 1-opioid receptor-mediated analgesia in mice.
Peripheral kappa 1-opioid receptor-mediated analgesia in mice.
复制标题
小鼠外周 kappa 1-阿片受体介导的镇痛作用。
DOI：
10.1016/0014-2999(96)00520-1
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发表时间：
1996
影响因子：
5
通讯作者：
Pasternak,GW
中科院分区：
文献类型：
--
作者：
Kolesnikov,Y;Jain,S;Wilson,R;Pasternak,GW
在甩尾实验中，U50,488H直接注射到尾，显示出强效镇痛作用（ED503.1 μg）。如果辐射热聚焦在距注射部位1厘米的地方，镇痛活性就会丧失。全身给药的κ1-阿片受体拮抗剂不-binaltorphimine逆转了U50,488H的局部镇痛反应，但直接注射到尾部的拮抗剂的效力是U50,488H的100倍。以编码κ1-阿片受体mRNA为靶点的鞘内反义处理可阻断尾部U50,488H的局部镇痛作用，提示U50,488H作用于背神经节神经元。
When injected directly into the tail, U50,488H is a potent analgesic in the tailflick assay (ED503.1 μg). The analgesic activity is lost if the radiant heat is focused 1 cm away from the site of injection. The κ1-opioid receptor antagonist nor-binaltorphimine given systemically reverses the local analgesic response of U50,488H, but the antagonist is 100-fold more potent when injected directly into the tail. Intrathecal antisense treatment with a probe targeting the mRNA encoding the κ1-opioid receptor blocks the local analgesic actions of U50,488H in the tail, suggesting that U50,488H is acting on dorsal ganglia neurons.