Agonists at presynaptic receptors on sympathetic nerves differentially affect two phases of the contractile response in the rat vas deferens

David R. Mottram
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Abstract

A series of adrenoceptor agonists were investigated for their prejunctional effects on field stimulated rat vas deferens. Tissues were stimulated in 10 s trains of impulses, frequency to Hz, every 100 s. This produced a biphasic response comprising an initial twitch followed by a prolonged, plateau phase of contraction. The order of potency for a series of α2-agonists against the twitch phase of contractions was UK14304 > clonidine > noradrenaline = α-methyl noradrenaline > B-HT920. The same order of potency was observed against the plateau phase, but approximately 10 fold higher concentrations of agonist were needed. Surprisingly, B-HT920 was inactive against the plateau phase of contraction. Characteristic differences in the slopes and maximum responses of the dose-response curves to the imidazolines (UK14304 and clonidine) and the β-phenethylamines (noradrenaline and α-methyl noradrenaline) were seen against both phases of contraction. It is concluded that the two phases of contraction are influenced by activation of two distinct heterogeneous populations of prejunctional α2-adrenoceptors.

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交感神经突触前受体的激动剂对大鼠输精管收缩反应的两个阶段有不同的影响
研究了一系列肾上腺素能受体激动剂对场刺激大鼠输精管的预兴奋作用。每隔100秒对组织进行10秒脉冲刺激,频率为Hz。这产生了双相反应,包括最初的抽搐,随后是延长的平台期收缩。一系列α - 2激动剂对收缩抽动期的效价顺序为UK14304 >可乐定比;去甲肾上腺素= α-甲基去甲肾上腺素>B-HT920。在平台期观察到相同的效力顺序,但需要大约10倍高浓度的激动剂。令人惊讶的是,B-HT920在收缩平台期无活性。在两个收缩阶段,咪唑类药物(UK14304和可定)和β-苯乙胺类药物(去甲肾上腺素和α-甲基去甲肾上腺素)的剂量-反应曲线斜率和最大响应均有显著差异。结果表明,两种不同的α - 2肾上腺素受体异质群体的激活影响了两期收缩。
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