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犬隐静脉中色胺衍生物在节前和节后受体处的激动剂效力。

Agonist potencies of tryptamine derivatives at pre- and postjunctional receptors in canine saphenous vein.

作者信息

Müller-Schweinitzer E

出版信息

Postgrad Med J. 1981;57 Suppl 1:36-44.

PMID:7301710
Abstract

Strips form canine saphenous veins were incubated with (3H)-noradrenaline and mounted for superfusion. 5-Hydroxytryptamine (5-HT inhibited the release of tritium caused by sustained electrical stimulation (2 Hz, 150 mA, 0.1 msec) being about 10 times more potent than noradrenaline. 5-HT inhibited contractions induced by intermittent electrical stimulation at 2 Hz but increased the tone of the preparations in the absence of stimulation. Agonist potencies of tryptamine derivatives at prejunctional 5-HT receptors were determined by calculating those concentrations which would reduce the contractile effect of 2 Hz to that of 1 Hz, agonist potencies at postjunctional 5-HT receptors were determined by estimating the concentration which produces 50% of maximum response (pD2 values). Comparison of the agonist potencies at pre- and postjunctional receptors of various tryptamine derivatives suggest that in canine saphenous vein the two types of 5-HT receptor are structurally similar.

摘要

将犬隐静脉条与(3H)-去甲肾上腺素一起孵育,然后安装用于灌注。5-羟色胺(5-HT)抑制由持续电刺激(2Hz,150mA,0.1毫秒)引起的氚释放,其效力比去甲肾上腺素强约10倍。5-HT抑制2Hz间歇性电刺激诱导的收缩,但在无刺激时增加标本的张力。通过计算将2Hz收缩效应降低至1Hz收缩效应的浓度来确定色胺衍生物在前接头5-HT受体处的激动剂效力,通过估计产生最大反应50%的浓度(pD2值)来确定在后接头5-HT受体处的激动剂效力。各种色胺衍生物在前接头和后接头受体处激动剂效力的比较表明,在犬隐静脉中,两种类型的5-HT受体在结构上相似。

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