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.
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。
相似文献
1
Beta-adrenoceptor agonist activity of labetolol on the isolated uterus of the rat.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。
Br J Pharmacol. 1979 Sep;67(1):13-5.
2
Labetalol possesses beta-adrenoceptor agonist action on the rat isolated uterus.拉贝洛尔对大鼠离体子宫具有β-肾上腺素能受体激动作用。
J Pharm Pharmacol. 1979 Nov;31(11):791-2. doi: 10.1111/j.2042-7158.1979.tb13663.x.
3
Pharmacological studies of mabuterol, a new selective beta 2-stimulant. II: Effects on the cardiovascular system and smooth muscle organs.新型选择性β2激动剂马布特罗的药理学研究。II：对心血管系统和平滑肌器官的影响。
Arzneimittelforschung. 1984;34(11A):1641-51.
4
Uterine relaxant effects of Curcuma aeruginosa Roxb. rhizome extracts.莪术根茎提取物的子宫松弛作用。
J Ethnopharmacol. 2009 Jan 30;121(3):433-43. doi: 10.1016/j.jep.2008.10.022. Epub 2008 Nov 5.
5
[Effect of izadrin, inderal and netalid on the periodic activity of the rabbit myometrium].[伊扎德林、心得安和奈塔利德对兔子宫肌层周期性活动的影响]
Farmakol Toksikol. 1976 Mar-Apr;39(2):155-9.
6
Comparative analysis of beta-1 adrenoceptor agonist and antagonist potency and selectivity of cicloprolol, xamoterol and pindolol.环丙洛尔、扎莫特罗和吲哚洛尔对β-1肾上腺素能受体激动剂及拮抗剂效能和选择性的比较分析
J Pharmacol Exp Ther. 1987 Sep;242(3):1025-34.
7
The cardiovascular and uterine effects of labetolol in conscious normotensive pregnant rats [proceedings].拉贝洛尔对清醒正常血压妊娠大鼠的心血管及子宫影响[会议论文集]
Br J Pharmacol. 1977 Nov;61(3):505P.
8
Beta-adrenoceptor-mediated inhibition of alpha 1-adrenoceptor-mediated and field stimulation-induced contractile responses in the prostate of the guinea pig.β-肾上腺素能受体介导的对豚鼠前列腺中α1-肾上腺素能受体介导的和场刺激诱导的收缩反应的抑制作用。
Br J Pharmacol. 1997 Nov;122(6):1067-74. doi: 10.1038/sj.bjp.0701494.
9
The selectivity in vitro of the stereoisomers of the beta-3 adrenoceptor agonist BRL 37344.
J Pharmacol Exp Ther. 1996 Apr;277(1):22-7.
10
beta 2-Adrenergic agonist effects of medroxalol and labetalol on rat and mouse uterine muscle.美多心安和拉贝洛尔对大鼠和小鼠子宫肌的β2-肾上腺素能激动剂作用。
J Pharm Pharmacol. 1982 Mar;34(3):193-5. doi: 10.1111/j.2042-7158.1982.tb04221.x.
引用本文的文献
1
Circulatory and metabolic effects of a combined alpha- and beta-adrenoceptor blocker (labetalol) in hypertension of pregnancy.联合α和β肾上腺素能受体阻滞剂（拉贝洛尔）对妊娠期高血压的循环和代谢影响
Br J Clin Pharmacol. 1981 Sep;12(3):345-8. doi: 10.1111/j.1365-2125.1981.tb01224.x.
2
Pharmacology of combined alpha-beta-blockade. I.α-β联合阻滞的药理学。I.
Drugs. 1984;28 Suppl 2:16-34. doi: 10.2165/00003495-198400282-00003.
3
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。
Br J Clin Pharmacol. 1980 May;9(5):517-8. doi: 10.1111/j.1365-2125.1980.tb05849.x.
4
Properties of labetalol, a combined alpha- and beta-blocking agent, relevant to the treatment of myocardial ischemia.拉贝洛尔（一种兼具α和β受体阻滞作用的药物）与心肌缺血治疗相关的特性。
Cardiovasc Drugs Ther. 1988 Sep;2(3):343-53. doi: 10.1007/BF00054642.
5
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
J Pharmacol Exp Ther. 1963 Nov;142:178-84.
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。
J Pharmacol Exp Ther. 1962 Oct;138:82-7.
3
Differentiation of receptor systems activated by sympathomimetic amines.拟交感胺激活的受体系统的分化
Nature. 1967 May 6;214(5088):597-8. doi: 10.1038/214597a0.
4
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。
Br J Pharmacol Chemother. 1967 Mar;29(3):291-301. doi: 10.1111/j.1476-5381.1967.tb01960.x.
5
6
Perspectives in adrenergic beta-receptor blockade.肾上腺素能β受体阻滞剂的展望
Clin Pharmacol Ther. 1969 May-Jun;10(3):292-306. doi: 10.1002/cpt1969103292.
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.
Zotero 插件