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阿片受体亚型选择性激动剂对小鼠输精管神经源性收缩中嘌呤能和肾上腺素能成分的影响。

Effect of opioid receptor subtype-selective agonists on purinergic and adrenergic components of neurogenic contractions of mouse vas deferens.

作者信息

Driessen B, Bültmann R, von Kügelgen I, Starke K

机构信息

Pharmakologisches Institut, Universität Freiburg, Germany.

出版信息

Br J Pharmacol. 1993 Feb;108(2):443-7. doi: 10.1111/j.1476-5381.1993.tb12823.x.

Abstract
  1. Effects of opioid agonists on the purinergic and adrenergic components of neurogenic contractions and in some experiments on transmitter overflow were studied in the mouse isolated vas deferens. 2. When the vas deferens was stimulated every 2 min by pairs of pulses 2 s apart in the presence of prazosin 0.3 microM (to isolate the purinergic component) or alpha,beta-methylene-ATP 3 microM (to isolate the adrenergic component), each pulse elicited a separate twitch. The opioid agonists [D-Ala2,N-Me-Phe4,Gly5-ol]enkephalin (DAMGO, mu-receptor-selective), [D-Pen2,D-Pen5]enkephalin (DPDPE, delta-selective) and trans-(+/-)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]- benzeneacetamide (U-50488, kappa-selective) concentration-dependently reduced both purinergic and adrenergic contractions. For each agonist, maximal effects and concentrations causing half-maximal effects were very similar for inhibition of the purinergic component on the one hand and for inhibition of the adrenergic component on the other hand, although the adrenergic component was inhibited with a slight preference. Moreover, effects on contractions elicited by the first and the second pulse of the pairs were very similar. 3. When vasa deferentia preincubated with [3H]-noradrenaline were stimulated with trains of 100 pulses delivered at 20 Hz, morphine 10 microM reduced significantly both evoked tritium overflow and evoked contractions. Its effect was antagonized by naloxone. 4. It is concluded that, in contrast to drugs acting at some other presynaptic receptors, opioid mu-, delta- and kappa-agonists inhibit purinergic and adrenergic neurogenic contractions of the mouse vas deferens in a similar manner. In contrast to a previous report, no enhancement by morphine of the release of noradrenaline elicited by high frequency pulse trains was observed.
摘要
  1. 在小鼠离体输精管中研究了阿片类激动剂对神经源性收缩的嘌呤能和肾上腺素能成分的影响,以及在一些实验中对递质溢出的影响。2. 当输精管在存在0.3微摩尔哌唑嗪(以分离嘌呤能成分)或3微摩尔α,β-亚甲基三磷酸腺苷(以分离肾上腺素能成分)的情况下每隔2分钟用间隔2秒的双脉冲刺激时,每个脉冲都会引发一次单独的抽搐。阿片类激动剂[D - Ala2,N - Me - Phe4,Gly5 - ol]脑啡肽(DAMGO,μ受体选择性)、[D - Pen2,D - Pen5]脑啡肽(DPDPE,δ选择性)和反式-(+/-)-3,4 - 二氯 - N - 甲基 - N - [2 - (1 - 吡咯烷基) - 环己基] - 苯乙酰胺(U - 50488,κ选择性)浓度依赖性地降低嘌呤能和肾上腺素能收缩。对于每种激动剂,一方面对嘌呤能成分的抑制和另一方面对肾上腺素能成分的抑制,其最大效应和引起半数最大效应的浓度非常相似,尽管对肾上腺素能成分的抑制略有偏好。此外,对双脉冲中第一个和第二个脉冲引发的收缩的影响非常相似。3. 当用20赫兹的100个脉冲串刺激预先用[3H] - 去甲肾上腺素预孵育的输精管时,10微摩尔吗啡显著降低诱发的氚溢出和诱发的收缩。其作用被纳洛酮拮抗。4. 得出的结论是,与作用于其他一些突触前受体的药物不同,阿片类μ、δ和κ激动剂以相似的方式抑制小鼠输精管的嘌呤能和肾上腺素能神经源性收缩。与先前的报告相反,未观察到吗啡增强高频脉冲串引起的去甲肾上腺素释放。

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