强啡肽相关肽通过非阿片类作用导致大鼠运动功能障碍。
Dynorphin-related peptides cause motor dysfunction in the rat through a non-opiate action.
作者信息
Faden A I, Jacobs T P
出版信息
Br J Pharmacol. 1984 Feb;81(2):271-6. doi: 10.1111/j.1476-5381.1984.tb10074.x.
Abstract
We compared effects on motor function of four peptides belonging to the dynorphin family--dynorphin-(1-17) (DYN-(1-17], dynorphin-(1-13) (DYN-(1-13], dynorphin-(1-8) (DYN-(1-8] and alpha-neo-endorphin (alpha NE). After intrathecal administration, each of these peptides produced dose-related, flaccid, hindlimb paralysis, with the order of potency being DYN-(1-17) greater than DYN-(1-13) greater than alpha NE congruent to DYN-(1-8). This motor dysfunction was not reversed or blocked by the opiate receptor antagonist naloxone and was not produced by a variety of other kappa-selective agonists. However, paralysis was produced by des-Tyr-dynorphin (DYN-(2-17], which does not act at the opioid receptor. Taken together, the present studies show that dynorphin-related peptides, uniquely amongst opioids, produce motor dysfunction, an action which does not appear to be mediated by opioid receptors.
摘要
我们比较了强啡肽家族的四种肽——强啡肽-(1-17)（DYN-(1-17)）、强啡肽-(1-13)（DYN-(1-13)）、强啡肽-(1-8)（DYN-(1-8)）和α-新内啡肽（αNE）对运动功能的影响。鞘内给药后，这些肽中的每一种都产生了剂量相关的、弛缓性的后肢麻痹，效力顺序为DYN-(1-17)＞DYN-(1-13)＞αNE≡DYN-(1-8)。这种运动功能障碍未被阿片受体拮抗剂纳洛酮逆转或阻断，并且多种其他κ选择性激动剂也未产生这种情况。然而，去酪氨酸强啡肽（DYN-(2-17)）可产生麻痹，它并不作用于阿片受体。综上所述，目前的研究表明，强啡肽相关肽在阿片类药物中独一无二地产生运动功能障碍，这种作用似乎不是由阿片受体介导的。
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