Antinociceptive effects of intrathecally administered human beta-endorphin in the rat and cat.
Antinociceptive effects of intrathecally administered human beta-endorphin in the rat and cat.
复制标题
鞘内注射人β-内啡肽对大鼠和猫的镇痛作用。
DOI：
10.1139/y78-120
复制
发表时间：
1978
影响因子：
2.1
通讯作者：
J. Henry
中科院分区：
文献类型：
--
作者：
T. Yaksh;J. Henry
长期植入鞘内导管的大鼠在通过留置导管向腰椎蛛网膜下腔注射人β -内啡肽后，热板反应和甩尾反应潜伏期呈剂量依赖性增加。-内啡肽的药效大约是吗啡的25倍。吗啡和内啡肽的剂量相匹配，产生了近似相等的亚极大次效应，观察到-内啡肽产生的抗痛觉作用持续时间大约是吗啡产生的三倍。鞘内注射-内啡肽到装有鞘内导管的猫的脊髓蛛网膜下腔也显示出有效的抗伤害感受作用，这种作用被纳洛酮完全拮抗。在大鼠中，纳洛酮系统给药剂量为10- 100微克/千克，在两种伤害性措施的剂量-反应曲线中产生平行位移，表明竞争性拮抗作用。通过剂量比分析，纳洛酮的体内pA2为7.1。这些数据和先前基于pA2的研究结果表明，吗啡、某些五肽和-内啡肽的相互作用在脊髓阿片受体群体介导行为定义的镇痛方面是相同的。
Rats chronically implanted with intrathecal catheters displayed a dose-dependent increase in the hot-plate and tail-flick response latencies following the injection of human beta-endorphin into the lumbar spinal subarachnoid space through the indwelling catheter. beta-Endorphin was approximately 25 times more potent than morphine on a molar basis. Matching morphine and beta-endorphin doses such that approximately equal submaximal submaximal effects occurred, it was observed that the antinociception produced by beta-endorphin lasted approximately three times longer than that produced by morphine. Experiments with intrathecal injection of beta-endorphin into the spinal subarachnoid space of cats fitted with intrathecal catheters also revealed a potent antinociceptive effect which was completely antagonized by naloxone. In the rats, naloxone administered systemically in doses of 10--100 microgram/kg produced a parallel shift in the dose-response curves of both nociceptive measures suggesting a competitive antagonism. Using a dose ratio analysis, an in vivo pA2 of 7.1 for naloxone was obtained. These data and those derived from previous work based on the pA2 suggest that the interaction of morphine, certain pentapeptides, and beta-endorphin is the same with regard to the spinal opiate receptor population mediating behaviorally defined analgesia.