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α-肾上腺素能受体激动剂和拮抗剂对大鼠离体输精管经壁刺激的前列腺和附睾段反应的影响。

The effects of alpha-adrenoceptor agonists and antagonists on responses of transmurally stimulated prostatic and epididymal portions of the isolated vas deferens of the rat.

作者信息

Brown C M, McGrath J C, Summers R J

出版信息

Br J Pharmacol. 1979 Aug;66(4):553-64. doi: 10.1111/j.1476-5381.1979.tb13694.x.

Abstract

1 The effects of alpha-adrenoceptor agonists and antagonists on contractile responses of transmurally stimulated prostatic and epididymal portions of the rat isolated vas deferens were examined. 2 Responses to single stimuli consisted of two phases, the first predominant in the prostatic and the second in the epididymal portion. The first phase was resistant to alpha-adrenoceptor antagonists but the second was reduced in a dose-related manner in the order of potency prazosin greater than azapetine greater than phentolamine greater than labetalol greater than yohimbine. 3 Both phases of the response to a single stimulus were reduced by clonidine but only the first could be reliably restored by yohimbine. 4 Trains of transmural stimuli produced biphasic responses, an early rapid component predominant in the prostatic and a slow secondary component predominant in the epididymal portion. The effects of alpha-adrenoceptor antagonists on these responses were complex. Prazosin produced the most straightforward inhibition of responses with relative resistance of the early rapid component. Only yohimbine and phentolamine produced increases in responses which could be pre-junctional in origin. 5 The alpha-adrenoceptor agonists, oxymetazoline and clonidine, reduced while phenylephrine increased responses to trains of stimuli. 6 These results are discussed in relation to the nature of the innervation of rat vas deferens and the usefulness of the preparation in pharmacological tests for activity at alpha-adrenoceptors.

摘要
  1. 研究了α-肾上腺素能受体激动剂和拮抗剂对大鼠离体输精管经壁刺激的前列腺部和附睾部收缩反应的影响。2. 对单次刺激的反应包括两个阶段,第一阶段在前列腺部占主导,第二阶段在附睾部占主导。第一阶段对α-肾上腺素能受体拮抗剂有抗性,但第二阶段以与剂量相关的方式降低,其效力顺序为哌唑嗪大于阿扎哌丁大于酚妥拉明大于拉贝洛尔大于育亨宾。3. 可乐定可降低对单次刺激的两个阶段的反应,但只有第一阶段可被育亨宾可靠地恢复。4. 经壁刺激串产生双相反应,早期快速成分在前列腺部占主导,缓慢的第二成分在附睾部占主导。α-肾上腺素能受体拮抗剂对这些反应的影响很复杂。哌唑嗪对反应的抑制最为直接,早期快速成分相对耐药。只有育亨宾和酚妥拉明可使反应增加,这可能源于突触前。5. α-肾上腺素能受体激动剂羟甲唑啉和可乐定可降低反应,而去氧肾上腺素可增加对刺激串的反应。6. 结合大鼠输精管的神经支配性质以及该制剂在α-肾上腺素能受体活性药理学试验中的实用性对这些结果进行了讨论。

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