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豚鼠输精管中参与交感神经递质分泌反馈控制的突触前α受体对儿茶酚胺的选择性。

Selectivity for catecholamines of presynaptic alpha-receptors involved in feedback control of sympathetic neurotransmitter secretion in guinea-pig vas deferens.

作者信息

Stjärne L

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1975;288(2-3):296-303. doi: 10.1007/BF00500534.

Abstract

The aim of the study was to quantitatively compare the relative affinities of noradrenaline, adrenaline, dopamine and isoprenaline for the, probably neural, receptors mediating feedback control of sympathetic neurotransmitter secretion. The experiments were carried out in isolated superfused field stimulated guinea-pig vas deferens, in which the noradrenaline stores had been labelled by preincubation with tritiated (-)-noradrenaline. Desipramine and normetanephrine were added to prevent rebinding of transmitter. Exogenous noradrenaline was found to cause a dose-dependent and reversible depression of the secretion of tracer noradrenaline evoked by field stimulation. Since the depressing effect was not affected by a ten-fold rise in the desipramine concentration, it seems likely that it was not due to uptake and preferential secretion of unlabelled exogenous noradrenaline, but was truly due to depression of the secretory mechanism. Adrenaline was significantly more potent than noradrenaline, as inhibitor of the secretion of tracer transmitter, while dopamine, at the same molar concentration, was without effect. The beta-agonist isoprenaline did not depress, but rather tended to enhance, the secretion of tracer noradrenaline. It is concluded that the receptors controlling the secretion of noradrenaline from the sympathetic nerves of guinea-pig vas deferens quantitatively-with regard to sensitivity-as well as qualitatively-with regard to order of preference for different catecholamines-resemble the "classical" alpha-receptors of e.g. smooth muscle in the same tissue.

摘要

本研究的目的是定量比较去甲肾上腺素、肾上腺素、多巴胺和异丙肾上腺素对可能是神经的受体的相对亲和力,这些受体介导交感神经递质分泌的反馈控制。实验在分离的、经超灌流的、由场刺激的豚鼠输精管中进行,其中去甲肾上腺素储存已通过与氚化(-)-去甲肾上腺素预孵育进行标记。加入地昔帕明和去甲变肾上腺素以防止递质的再结合。发现外源性去甲肾上腺素会引起场刺激诱发的示踪去甲肾上腺素分泌呈剂量依赖性和可逆性降低。由于地昔帕明浓度升高十倍对抑制作用没有影响,所以似乎不太可能是由于未标记的外源性去甲肾上腺素的摄取和优先分泌,而确实是由于分泌机制的抑制。作为示踪递质分泌的抑制剂,肾上腺素比去甲肾上腺素的效力显著更强,而相同摩尔浓度的多巴胺则没有作用。β激动剂异丙肾上腺素并未抑制,反而倾向于增强示踪去甲肾上腺素的分泌。得出的结论是,控制豚鼠输精管交感神经去甲肾上腺素分泌的受体,在敏感性方面的定量以及在对不同儿茶酚胺的优先顺序方面的定性,类似于同一组织中例如平滑肌的“经典”α受体。

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