Ontogeny of opioid pharmacology and receptors: high and low affinity site differences.
Ontogeny of opioid pharmacology and receptors: high and low affinity site differences.
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DOI：
10.1016/0014-2999(81)90142-4
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发表时间：
1981-07
影响因子：
5
通讯作者：
A. Zhang;G. Pasternak
中科院分区：
文献类型：
--
作者：
A. Zhang;G. Pasternak
多种阿片类药物和脑啡肽高亲和力结合的发展不同于低亲和力结合。在出生后的前2周内，脑和脊髓的低亲和力结合保持相对稳定，而高亲和力结合增加了3倍。对阿片类药物的镇痛和呼吸敏感性的发展也存在差异。吗啡、β-内啡肽和d - ala2 - met5 -脑啡肽在2日龄大鼠中抑制呼吸频率的剂量等于或低于14日龄大鼠，而吗啡的镇痛作用ed50在2日龄大鼠中比14日龄大鼠高40倍。同样，β-内啡肽和d - ala2 - met5 -脑啡肽对14日龄大鼠有镇痛作用，但对7日龄大鼠无镇痛作用。脊髓横断对14日龄大鼠吗啡镇痛的影响很小，这表明镇痛敏感性的改变是在脊柱节段水平上的，而不是下行通路的结果。这些结果提示高亲和力结合与镇痛作用之间以及低亲和力结合与呼吸作用之间存在有趣的相关性。
The development of the high affinity binding of a variety of opiates and enkephalins is distinct from low affinity binding. During the first 2 weeks after birth, low affinity binding in both brain and spinal cord remains relatively constant while high affinity binding increases up to 3-fold. Differences in the development of analgesic and respiratory sensitivity to opiates are also found. Whereas morphine, β-endorphin and D-Ala2-Met5-enkephalinamide depress respiratory rates in 2-day old rats at doses equal to or lower than those active in 14-day old rats, morphine's analgesic ED50is 40-fold greater in 2-day old than in 14-day old rats. Similarly, β-endorphin and D-Ala2-Met5-enkephalinamide are analgesic in 14-day old rats but not 7-day old rats. The small effect of spinal transections on morphine analgesia in 14-day old rats suggests that the change in analgesic sensitivity is at a segmental spinal level and not a result of descending pathways. These results suggestan interesting correlation between high affinity binding and analgesia and between low affinity binding and respiratory effects.