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吗啡对小鼠输精管肾上腺素能传递的影响。麻醉性镇痛药激动剂和拮抗剂效能的评估。

Effect of morphine on adrenergic transmission in the mouse vas deferens. Assessment of agonist and antogonist potencies of narcotic analgesics.

作者信息

Hughes J, Kosterlitz H W, Leslie F M

出版信息

Br J Pharmacol. 1975 Mar;53(3):371-81. doi: 10.1111/j.1476-5381.1975.tb07373.x.

DOI:10.1111/j.1476-5381.1975.tb07373.x
PMID:236796
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1666422/
Abstract
  1. Morphine inhibits the electrically evoked (0.1-0.15 Hz, 1 ms) contractions of the longitudinal muscle of the mouse vas deferens but not of the rabbit, guinea-pig, rat, cat, hamster or gerbil. This effect is stereospecific and is antagonized by naloxone or naltrexone. 2. Normorphine is equiactive with morphine but its effects are more rapid in onset and decline. 3. In the mouse vas deferens, the resting outflow of tritium-labelled catecholamines is unaffected by morphine. The electrically evoked outflow is depressed by morphine or normorphine in a dose-dependent manner. The ID50 for inhibition of contraction and for depression of outflow is 0.5 muM. 4. The relative agonist potencies of compounds without antagonist component (codeine, pethidine, morphine, normorphine, heroin, levorphanol, Ba-20227, etorphine) show good correlation with the relative agonist potencies determined in the guinea-pig ileum and for analgesia in man. 5. For compounds with dual agonist and antagonist properties, the dose-response curves for agonist activity are shallow. When the lowest concentrations giving a depression of the contraction of the mouse vas deferens are used, a good correlation is obtained with the guinea-pig ileum. 6. The relative antagonist potencies of naloxone, nalorphine, levallorphan, and cyclazocine agree well with those obtained in the guinea-pig ileum; these, in turn, correlate well with the values obtained in the morphine-dependent monkey. 7. The fact that the agonist effects of drugs with dual agonist and antagonist action show little or no dependence on concentration, makes the mouse vas deferens particularly suitable for the assay of assay of antagonist activity. 8. As an assay preparation, the mouse vas deferens is less robust and consistent in its responses than the guinea-pig ileum.
摘要
  1. 吗啡可抑制电刺激诱发的(0.1 - 0.15赫兹,1毫秒)小鼠输精管纵肌收缩,但对兔、豚鼠、大鼠、猫、仓鼠或沙鼠的输精管纵肌收缩无抑制作用。此效应具有立体特异性,且可被纳洛酮或纳曲酮拮抗。2. 去甲吗啡与吗啡活性相当,但其起效和消退更快。3. 在小鼠输精管中,氚标记的儿茶酚胺的静息释放不受吗啡影响。电刺激诱发的释放则被吗啡或去甲吗啡以剂量依赖方式抑制。抑制收缩和抑制释放的半数抑制浓度(ID50)为0.5微摩尔。4. 无拮抗成分的化合物(可待因、哌替啶、吗啡、去甲吗啡、海洛因、左啡诺、Ba - 20227、埃托啡)的相对激动剂效价与在豚鼠回肠中测定的相对激动剂效价以及在人体中的镇痛效价显示出良好的相关性。5. 对于具有双重激动剂和拮抗剂特性的化合物,激动剂活性的剂量 - 反应曲线较平缓。当使用能使小鼠输精管收缩受到抑制的最低浓度时,与豚鼠回肠有良好的相关性。6. 纳洛酮、纳洛芬、左洛啡烷和环唑辛的相对拮抗剂效价与在豚鼠回肠中获得的效价吻合良好;这些效价又与在吗啡依赖猴中获得的值有很好的相关性。7. 具有双重激动剂和拮抗剂作用的药物的激动剂效应几乎不依赖或完全不依赖浓度这一事实,使得小鼠输精管特别适合用于拮抗剂活性的测定。8. 作为一种测定制剂,小鼠输精管的反应不如豚鼠回肠强健和稳定。

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HISTOCHEMICAL CORRELATIONS OF ACETYLCHOLINESTERASE AND CATECHOLAMINES IN POSTGANGLIONIC AUTONOMIC NERVES OF THE CAT, RABBIT, AND GUINEA PIG.猫、兔和豚鼠节后自主神经中乙酰胆碱酯酶与儿茶酚胺的组织化学相关性
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Acceleration of noradrenaline biosynthesis in the guinea-pig vas deferens by potassium.钾离子对豚鼠输精管去甲肾上腺素生物合成的加速作用。
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A new example of a morphine-sensitive neuro-effector junction: adrenergic transmission in the mouse vas deferens.吗啡敏感型神经效应器连接的一个新实例:小鼠输精管中的肾上腺素能传递。
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