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拉贝洛尔对大鼠离体子宫的β-肾上腺素能受体激动剂活性。

Beta-adrenoceptor agonist activity of labetolol on the isolated uterus of the rat.

作者信息

Carey B, Whalley E T

出版信息

Br J Pharmacol. 1979 Sep;67(1):13-5.

PMID:40642
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2043602/
Abstract

Isoprenaline produced dose-dependent reductions of responses of the isolated uterus of the rat produced by an EC(80) of acetylcholine. Propranolol acted as a competitive antagonist to isoprenaline. Labetolol also reduced the acetylcholine-induced contractions but was much less potent than isoprenaline. The greatest reduction was smaller than that produced by isoprenaline. Propranolol antagonized the lower doses of labetolol. It is suggested that labetolol possesses partial agonist activity at the beta-adrenoceptors of the rat isolated uterus.

摘要

异丙肾上腺素能使乙酰胆碱的EC(80)所引起的大鼠离体子宫反应呈剂量依赖性降低。普萘洛尔对异丙肾上腺素起竞争性拮抗作用。拉贝洛尔也能降低乙酰胆碱诱导的收缩,但效力远低于异丙肾上腺素。其最大降低幅度小于异丙肾上腺素所产生的降低幅度。普萘洛尔能拮抗较低剂量的拉贝洛尔。提示拉贝洛尔在大鼠离体子宫的β肾上腺素受体上具有部分激动剂活性。

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引用本文的文献

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Some further evidence for partial agonist activity of labetalol.关于拉贝洛尔部分激动剂活性的一些进一步证据。
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Failure of enhancement by labetalol of bronchopulmonary effects of histamine in guinea-pigs: independence of alpha-adrenoceptor antagonism.拉贝洛尔未能增强组胺对豚鼠支气管肺的效应:α-肾上腺素能受体拮抗作用的独立性。
Br J Pharmacol. 1987 Jul;91(3):487-92. doi: 10.1111/j.1476-5381.1987.tb11241.x.

本文引用的文献

1
THE ADRENERGIC RECEPTIVE MECHANISM OF THE RAT UTERUS.大鼠子宫的肾上腺素能受体机制
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2
The mechanism of uterine inhibitory action of relaxin-containing ovarian extracts.含松弛素的卵巢提取物对子宫的抑制作用机制。
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Differentiation of receptor systems activated by sympathomimetic amines.拟交感胺激活的受体系统的分化
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Investigation of adrenaline reversal in the rat uterus by the induction of resistance to isoprenaline.通过诱导大鼠子宫对异丙肾上腺素产生抗性来研究肾上腺素逆转作用。
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The effects of alpha- and beta-adrenoceptor blocking agents on the responses of the rat uterus to catecholamines throughout the oestrus cycle.α-和β-肾上腺素能受体阻断剂对大鼠子宫在整个发情周期中对儿茶酚胺反应的影响。
Br J Pharmacol. 1970 Sep;40(1):160P-161P.
6
Perspectives in adrenergic beta-receptor blockade.肾上腺素能β受体阻滞剂的展望
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7
Pharmacology of AH 5158; a drug which blocks both - and -adrenoceptors.AH 5158的药理学;一种能阻断α和β肾上腺素能受体的药物。
Br J Pharmacol. 1972 Aug;45(4):660-75. doi: 10.1111/j.1476-5381.1972.tb08125.x.
8
Labetalol in long-term treatment of hypertension.拉贝洛尔用于高血压的长期治疗。
Br J Clin Pharmacol. 1976 Aug;3(4 Suppl 3):743-50.
9
A review of the animal pharmacology of labetalol, a combined alpha- and beta-adrenoceptor-blocking drug.拉贝洛尔(一种α和β肾上腺素受体阻断联合药物)的动物药理学综述。
Br J Clin Pharmacol. 1976 Aug;3(4 Suppl 3):681-4.
10
The mechanism of the utero-inhibitory effect of beta-sympathomimetics.β-拟交感神经药的子宫抑制作用机制。
Pharmacol Ther B. 1975;1(2):277-96. doi: 10.1016/0306-039x(75)90008-2.