ICI 118,587的心血管效应：一种β1肾上腺素能受体部分激动剂。
The cardiovascular effects of ICI 118,587: A beta 1-adrenoceptor partial agonist.
作者信息
Nuttall A, Snow H M
出版信息
Br J Pharmacol. 1982 Oct;77(2):381-8. doi: 10.1111/j.1476-5381.1982.tb09309.x.
Abstract
1 In a preparation in which cardiovascular reflexes were prevented from occurring, ICI 118,587 (1-(p-hydroxyphenoxy)-3-beta-(morpholinocarbonamido) ethylamino-2-propranol fumarate) caused dose-dependent positive chronotropic and inotropic effects upon the dog heart. 2 The increase in heart rate brought about by ICI 118,587 was about 43% of the maximum increase produced by isoprenaline. 3 For a given chronotropic effect produced by either ICI 118,587 or isoprenaline, each compound produced a similar inotropic effect as indicated by an increase in LV dp/dtmax. 4 In contrast to the direct stimulant action of ICI 118,587 on the heart no direct effects on vascular smooth muscle were observed. 5 ICI 118,587 was shown to be a competitive antagonist of the chronotropic and vasodilator effects of isoprenaline on the heart and blood vessels and of the chronotropic effects of noradrenaline on the heart. 6 It is concluded that ICI 118,587 is a selective beta 1-adrenoceptor partial agonist.
摘要
在一种阻止心血管反射发生的制剂中，ICI 118,587（1-(对羟基苯氧基)-3-β-(吗啉甲酰胺基)乙氨基-2-丙醇富马酸盐）对犬心脏产生剂量依赖性的正性变时和变力作用。
ICI 118,587引起的心率增加约为异丙肾上腺素产生的最大增加量的43%。
对于由ICI 118,587或异丙肾上腺素产生的给定变时效应，每种化合物产生的变力效应相似，如左心室dp/dtmax增加所示。
与ICI 118,58对心脏的直接刺激作用相反，未观察到对血管平滑肌的直接作用。
ICI 118,587被证明是异丙肾上腺素对心脏和血管的变时和血管舒张作用以及去甲肾上腺素对心脏的变时作用的竞争性拮抗剂。
得出结论，ICI 118,587是一种选择性β1-肾上腺素能受体部分激动剂。
相似文献
1
The cardiovascular effects of ICI 118,587: A beta 1-adrenoceptor partial agonist.ICI 118,587的心血管效应：一种β1肾上腺素能受体部分激动剂。
Br J Pharmacol. 1982 Oct;77(2):381-8. doi: 10.1111/j.1476-5381.1982.tb09309.x.
2
The cardiovascular pharmacology of ICI 170777 ((6RS)-6-methyl-5-(pyrid-4-yl)-3H,6H-1,3,4- thiadiazin-2-one) a novel compound with positive inotropic and vasodilator effects.ICI 170777（(6RS)-6-甲基-5-(吡啶-4-基)-3H,6H-1,3,4-噻二嗪-2-酮）的心血管药理学，一种具有正性肌力和血管舒张作用的新型化合物。
Br J Pharmacol. 1989 Jun;97(2):409-18. doi: 10.1111/j.1476-5381.1989.tb11968.x.
3
Pharmacological analysis of the cardiac actions of xamoterol, a beta adrenoceptor antagonist with partial agonistic activity, in guinea pig heart: evidence for involvement of adenylate cyclase system in its cardiac stimulant actions.对具有部分激动活性的β肾上腺素能受体拮抗剂扎莫特罗在豚鼠心脏中的心脏作用进行药理学分析：腺苷酸环化酶系统参与其心脏兴奋作用的证据。
J Pharmacol Exp Ther. 1987 Sep;242(3):1077-85.
4
Selective and full beta 1-adrenoceptor agonist action of a catechol derivative of denopamine (T-0509) in the guinea-pig cardiac muscle and trachea: comparison with denopamine, xamoterol and isoprenaline.多巴胺（T-0509）的儿茶酚衍生物在豚鼠心肌和气管中的选择性及完全β1-肾上腺素能受体激动作用：与多巴胺、扎莫特罗和异丙肾上腺素的比较
Br J Pharmacol. 1992 Jun;106(2):335-41. doi: 10.1111/j.1476-5381.1992.tb14337.x.
5
6
Cardiostimulant and cardiodepressant effects through overexpressed human beta2-adrenoceptors in murine heart: regional differences and functional role of beta1-adrenoceptors.通过在小鼠心脏中过表达人β2肾上腺素能受体产生的心脏刺激和心脏抑制作用：β1肾上腺素能受体的区域差异和功能作用
Naunyn Schmiedebergs Arch Pharmacol. 2003 Apr;367(4):380-90. doi: 10.1007/s00210-002-0681-4. Epub 2003 Mar 4.
7
Comparisons of the inotropic effects of the beta 1-adrenoceptor partial agonists SL 75.177.10 and ICI 118,587 with digoxin on the intact canine heart.β1 -肾上腺素能受体部分激动剂SL 75.177.10和ICI 118,587与地高辛对完整犬心的变力作用比较。
J Cardiovasc Pharmacol. 1984 Jul-Aug;6(4):720-6. doi: 10.1097/00005344-198407000-00027.
8
The in vitro pharmacology of xamoterol (ICI 118,587).扎莫特罗（ICI 118,587）的体外药理学
Br J Pharmacol. 1985 May;85(1):179-87. doi: 10.1111/j.1476-5381.1985.tb08845.x.
9
The partial agonist activity of xamoterol (ICI 118,587) studied by heart rate response in pithed rats.通过脊髓损毁大鼠的心率反应研究了扎莫特罗（ICI 118,587）的部分激动剂活性。
Jpn Circ J. 1988 Jan;52(1):60-5. doi: 10.1253/jcj.52.60.
10
Changes in cardiovascular responsiveness to dopexamine and beta 1- and beta 2-adrenoceptor function after the chronic treatment of beta-adrenoceptor antagonists and agonists in anaesthetized dogs.麻醉犬长期使用β-肾上腺素能拮抗剂和激动剂治疗后，心血管系统对多培沙明及β1和β2肾上腺素能受体功能的变化。
J Auton Pharmacol. 1996 Oct;16(5):269-79. doi: 10.1111/j.1474-8673.1996.tb00361.x.
引用本文的文献
1
A polymorphism within a conserved beta(1)-adrenergic receptor motif alters cardiac function and beta-blocker response in human heart failure.保守的β1 - 肾上腺素能受体基序内的多态性改变人类心力衰竭中的心脏功能和β受体阻滞剂反应。
Proc Natl Acad Sci U S A. 2006 Jul 25;103(30):11288-93. doi: 10.1073/pnas.0509937103. Epub 2006 Jul 14.
2
Ketotifen and cardiovascular effects of xamoterol following single and chronic dosing in healthy volunteers.健康志愿者单次及长期给药后酮替芬与克仑特罗的心血管效应。
Br J Clin Pharmacol. 1999 Jan;47(1):59-66. doi: 10.1046/j.1365-2125.1999.00854.x.
3
Renal effects of xamoterol in patients with moderate heart failure.Xamoterol对中度心力衰竭患者的肾脏影响。
Cardiovasc Drugs Ther. 1993 Feb;7(1):111-6. doi: 10.1007/BF00878318.
4
The lipolytic effect of beta 1- and beta 2-adrenoceptor activation in healthy human volunteers.β1-和β2-肾上腺素能受体激活对健康人类志愿者的脂解作用。
Br J Clin Pharmacol. 1993 Jan;35(1):35-9. doi: 10.1111/j.1365-2125.1993.tb05667.x.
5
Pharmacokinetic drug interactions with ACE inhibitors.与血管紧张素转换酶抑制剂的药代动力学药物相互作用。
Clin Pharmacokinet. 1993 Jul;25(1):20-58. doi: 10.2165/00003088-199325010-00003.
6
Lack of pharmacodynamic interactions between acute dose flosequinan and xamoterol. A pilot study in healthy subjects.急性剂量氟司喹南与扎莫特罗之间不存在药效学相互作用。一项针对健康受试者的初步研究。
Eur J Clin Pharmacol. 1994;46(4):361-5. doi: 10.1007/BF00194406.
7
Preliminary study of the efficacy of xamoterol in bradycardia-tachycardia syndrome.Xamoterol治疗心动过缓-心动过速综合征疗效的初步研究。
Br J Clin Pharmacol. 1994 Sep;38(3):285-7. doi: 10.1111/j.1365-2125.1994.tb04356.x.
8
Inotropic support of the critically ill patient. A review of the agents.危重症患者的正性肌力支持。药物综述。
Drugs. 1993 May;45(5):654-67. doi: 10.2165/00003495-199345050-00003.
9
The effects of ICI 118,587 and atenolol on the responses to exercise and on breathlessness in healthy subjects.ICI 118,587和阿替洛尔对健康受试者运动反应及呼吸困难的影响。
Br J Clin Pharmacol. 1984 Jan;17(1):37-41. doi: 10.1111/j.1365-2125.1984.tb04996.x.
10
Initial clinical experience with ICI 141,292 (Visacor), a new selective beta 1-adrenoceptor blocker with ISA--a multicentre trial in 59 patients.ICI 141,292（Visacor）的初步临床经验，一种具有内源性拟交感活性的新型选择性β1肾上腺素受体阻滞剂——一项针对59例患者的多中心试验。
Br J Clin Pharmacol. 1984 Dec;18(6):831-6. doi: 10.1111/j.1365-2125.1984.tb02552.x.
本文引用的文献
1
Circulatory, respiratory and metabolic responses to isopropylnoradrenaline in man.人体对异丙肾上腺素的循环、呼吸及代谢反应。
J Physiol. 1960 Jun;151(3):539-50. doi: 10.1113/jphysiol.1960.sp006458.
2
Beta-adrenoceptor stimulant properties of amidoalkylamino-substituted 1-aryl-2-ethanols and 1-(aryloxy)-2-propanols.氨基烷基氨基取代的1-芳基-2-乙醇和1-（芳氧基）-2-丙醇的β-肾上腺素能受体刺激特性
J Med Chem. 1981 Mar;24(3):315-22. doi: 10.1021/jm00135a015.
3
The inotropic and chronotropic effects of catecholamines on the dog heart.儿茶酚胺对犬心脏的变力性和变时性作用。
J Physiol. 1971 Apr;214(1):15-28. doi: 10.1113/jphysiol.1971.sp009416.
4
Assessment of cardiac contractility. The relation between the rate of pressure rise and ventricular pressure during isovolumic systole.心脏收缩力评估。等容收缩期压力上升速率与心室压力之间的关系。
Circulation. 1971 Jul;44(1):47-58. doi: 10.1161/01.cir.44.1.47.
5
Inotropic changes in the left ventricle: the effect of changes in heart rate, aortic pressure and end-diastolic pressure.左心室的变力性变化：心率、主动脉压和舒张末期压力变化的影响。
J Physiol. 1970 Dec;211(2):359-87. doi: 10.1113/jphysiol.1970.sp009283.
6
In vivo analysis of adrenergic receptor activity of dobutamine.多巴酚丁胺肾上腺素能受体活性的体内分析。
Circ Res. 1974 May;34(5):663-71. doi: 10.1161/01.res.34.5.663.
7
Action of propranolol on the dog heart.普萘洛尔对犬心脏的作用。
Cardiovasc Res. 1973 Nov;7(6):729-39. doi: 10.1093/cvr/7.6.729.
8
Inotropic and chronotropic responses of the in vivo denervated dog myocardium to dobutamine.体内去神经支配犬心肌对多巴酚丁胺的变力性和变时性反应。
Can J Physiol Pharmacol. 1976 Aug;54(4):618-21. doi: 10.1139/y76-085.
9
The cardiovascular acitivity of ICI 118,587 a novel beta-adrenoceptor partial agonist [proceedings].新型β-肾上腺素能受体部分激动剂ICI 118,587的心血管活性[会议论文]
Br J Pharmacol. 1979 Nov;67(3):412P.
10
A study of the relationship between cardiac beta-adrenoceptor blockade and intrinsic sympathomimetic activity in rats depleted of catecholamines.一项关于去甲肾上腺素耗竭大鼠心脏β-肾上腺素能受体阻断与内在拟交感活性之间关系的研究。
Clin Exp Pharmacol Physiol. 1979 Jan-Feb;6(1):1-9. doi: 10.1111/j.1440-1681.1979.tb00001.x.
Zotero 插件