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[二氢麦角隐亭对大鼠离体输精管突触前和突触后α-肾上腺素能受体的作用]

[Action of dihydroergocristine at pre- and postsynaptic alpha-adrenoceptors in the rat isolated vas deferens].

作者信息

Roquebert J, Demichel P, Gomond P, Malek A

出版信息

J Pharmacol. 1983 Apr-Jun;14(2):151-9.

PMID:6134866
Abstract
  1. The action of dihydroergocristine at pre- and postsynaptic alpha-adrenoceptors has been studied in the rat isolated vas deferens. 2. Postsynaptic alpha-adrenoceptor antagonist activity was assessed by comparing cumulative noradrenaline and phenylephrine dose-response curves in the absence and in the presence of increasing concentrations of antagonist. 3. Presynaptic alpha-adrenoceptor activity was assessed by studying the effects of drugs on contractions induced by electrical stimulation of the rat vas deferens. 4. At postsynaptic alpha-adrenoceptor dihydroergocristine antagonized the contraction induced by noradrenaline and phenylephrine with competitive mechanism (pA2 = 7.78 towards noradrenaline; pA2 = 7.76 towards phenylephrine). 5. At presynaptic alpha-adrenoceptors dihydroergocristine acts as partial agonist (pD2 = 5.70).
摘要
  1. 已在大鼠离体输精管中研究了双氢麦角隐亭对突触前和突触后α-肾上腺素能受体的作用。2. 通过比较在不存在和存在递增浓度拮抗剂的情况下去甲肾上腺素和苯肾上腺素的累积剂量-反应曲线,评估突触后α-肾上腺素能受体拮抗剂活性。3. 通过研究药物对大鼠输精管电刺激诱导的收缩的影响,评估突触前α-肾上腺素能受体活性。4. 在突触后α-肾上腺素能受体处,双氢麦角隐亭以竞争性机制拮抗去甲肾上腺素和苯肾上腺素诱导的收缩(对去甲肾上腺素的pA2 = 7.78;对苯肾上腺素的pA2 = 7.76)。5. 在突触前α-肾上腺素能受体处,双氢麦角隐亭作为部分激动剂(pD2 = 5.70)。

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