EFFECT OF MORPHINE AND NALOXONE ON A DEFENSIVE RESPONSE OF THE CRAB CHASMAGNATHUS-GRANULATUS
EFFECT OF MORPHINE AND NALOXONE ON A DEFENSIVE RESPONSE OF THE CRAB CHASMAGNATHUS-GRANULATUS
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DOI：
10.1016/0091-3057(88)90076-7
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发表时间：
1988-07-01
影响因子：
3.6
通讯作者：
MALDONADO, H
中科院分区：
文献类型：
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作者：
LOZADA, M;ROMANO, A;MALDONADO, H
雄蟹（Chasmagnathus granulatus）表现出防御反应（DR）的电击（8 V，50 Hz，1秒）。如此诱发的DR被用作研究吗啡的抗伤害感受作用的模型。注射吗啡-HCl（MP）（25、50、100和150 μ g/g），并在注射后2、7.5、15、30、45和75分钟检查DR。(a)MP产生了剂量依赖性的减少螃蟹的伤害性刺激的敏感性。(b)100 μ g/g剂量的MP引起50%的反应抑制，注射-休克间隔为30分钟，但当用1.6 μ g/g盐酸纳洛酮施用相同剂量时没有发生抑制，表明MP通过阿片受体起作用。(c)注射后2分钟的ED 50约为33 μ g/g，阈值剂量估计为6.8 μ g/g。这些剂量低于其它节肢动物报道的ED 50值（90 - 930 μ g/g），接近脊椎动物的ED 50值。(d)在注射后2分钟内迅速达到峰值MP效应。MP效应的持续时间根据剂量计算为45.0-75.0 min，半衰期消除的间接估计值为15.7 min。这些值明显低于脊椎动物报告的值。MP峰值效应的持续时间较短是由于节肢动物血脑屏障的渗透性比脊椎动物更高。
Male crabs (Chasmagnathus granulatus) exhibited a defensive response (DR) to an electric shock (8 V, 50 Hz, 1 sec). The DR so elicited was used as a model for studying the antinoiceptive effect of morphine. Injections of morphine-HCl (MP) (25, 50, 100 and 150 .mu.g/g) were administered and the DR was examined at 2, 7.5, 15, 30, 45 and 75 min post-injection. (a) MP produced a dose-dependent reduction of the crab''s sensitivity to the nociceptive stimulus. (b) A 100 .mu.g/g dose of MP caused a 50% response inhibition with an injection-shock interval of 30 minutes, but no inhibition occurred when the same dose was administered with 1.6 .mu.g/g of naloxone-HCl, suggesting that MP acts through an opiate receptor. (c) The ED50 at 2 min post-injection was roughly 33 .mu.g/g and the threshold dose was estimated to be 6.8 .mu.g/g. These doses are lower than ED50 values reported for other arthropods (90 to 930 .mu.g/g) and approach those of vertebrates. (d) The peak MP effect was reached quickly, within 2 min post-injection. The duration of the MP effect was calculated to be 45.0-75.0 min depending on the dose, and an indirect estimate of half-life elimination was 15.7 min. These values are remarkably lower than those reported for vertebrates. The shorter duration of the MP peak effect is attributable to a greater permeability of the arthropod blood-brain barrier as compared to that of vertebrates.