Methionine-enkephalin concentrations in discrete brain regions, spinal cord, pituitary gland and peripheral tissues of U-50,488H-tolerant and abstinent rats.
Methionine-enkephalin concentrations in discrete brain regions, spinal cord, pituitary gland and peripheral tissues of U-50,488H-tolerant and abstinent rats.
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U-50,488H 耐受和戒断大鼠的离散大脑区域、脊髓、垂体和外周组织中的蛋氨酸脑啡肽浓度。
DOI：
10.1159/000139183
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发表时间：
1994
期刊：
影响因子：
3.1
通讯作者：
Bhargava,HN
中科院分区：
文献类型：
--
作者：
Tejwani,GA;Rattan,AK;Koo,KL;Matwyshyn,GA;Bhargava,HN
测定了高选择性β-阿片受体激动剂U-50，488 H长期给药和停药对雄性Sprague-Dawley大鼠中枢和外周组织中甲硫氨酸-脑啡肽水平的影响。通过每天两次注射25 mg/kg的U-50，488 H，持续5天，使大鼠对U-50，488 H产生耐受性和身体依赖性。实验组大鼠连续4天注射该药物，第5天处死.蛋氨酸脑啡肽浓度增加的U-50，488 H耐受依赖大鼠的海马，而在禁欲大鼠，其水平升高，仅在下丘脑。U-50，488 H耐受依赖或戒断大鼠脑垂体中的甲硫氨酸脑啡肽水平无变化。在外周组织中，U-50，488 H耐受依赖大鼠肾上腺中的甲硫氨酸-脑啡肽浓度降低。在U-50，488 H-戒断大鼠中，心脏中甲硫氨酸-脑啡肽浓度升高。在吗啡和U-50，488 H耐受依赖和戒断大鼠的组织中，甲硫氨酸-脑啡肽浓度受到不同的影响，表明μ-和μ-阿片介导的耐受依赖和戒断过程存在固有差异。
Effects were determined of chronic administration and withdrawal of a highly selective ĸ-opioid receptor agonist, U-50,488H, on methionine-enkephalin levels in central and peripheral tissues of male Sprague-Dawley rats. Rats were rendered tolerant to and physically dependent on U-50,488H by twice daily injections of 25 mg/kg of this compound for 5 days. Rats deemed abstinent were injected with this drug for 4 days and sacrificed on 5 th day. Methionine-enkephalin concentration increased in the hippocampus of U-50,488H-tolerant-dependent rats, whereas in abstinent rats, its level was elevated only in the hypothalamus. Levels of methionine-enkephalin in the pituitary gland of U-50,488H-tolerant-dependent or abstinent rats were unchanged. Among peripheral tissues, methionine-enkephalin concentration decreased in the adrenal gland of U-50,488H-tolerant-dependent rats. In the U-50,488H-abstinent rats, methionine-enkephalin concentration was elevated in the heart. In tissues of morphine- and U-50,488H-tolerant-dependent and abstinent rats methionine-enkephalin concentrations were affected differentially, suggesting inherent differences in µ- and ĸ-opiate-mediated tolerance-dependence and abstinence processes.