豚鼠体内与异丙肾上腺素和奥西那林相关的化合物对β-肾上腺素能受体的体外效力和选择性
Potency and selectivity in vitro of compounds related to isoprenaline and orciprenaline on beta-adrenoceptors in the guinea-pig.
作者信息
O'Donnell S R, Wanstall J C
出版信息
Br J Pharmacol. 1974 Nov;52(3):407-17. doi: 10.1111/j.1476-5381.1974.tb08610.x.
Abstract
1 Amines related in structure to either isoprenaline (catechol series) or orciprenaline (resorcinol series) were examined for activity on isolated trachea (relaxation), atria (chronotropic action) and perfused hind-limb (vasodilatation) of the guinea-pig.2 Compounds with a resorcinol nucleus were less potent on all three preparations but more selective for trachea than were compounds with a catechol nucleus.3 In both catechol and resorcinol compounds potency on trachea was enhanced by and selectivity for trachea was favoured by substitution of a p-OH phenyl group in the N-iso propyl, or by replacement of the N-iso propyl with an N-t-butyl, with or without a p-OH phenyl group.4 Most of the compounds, particularly the resorcinols, had much lower potencies, relative to isoprenaline, on hind-limb than on trachea.5 Some of the problems associated with the quantitative measurement of selectivity and with sub-classification of beta-adrenoceptors are discussed.
摘要
研究了结构上与异丙肾上腺素（儿茶酚系列）或奥西那林（间苯二酚系列）相关的胺类对豚鼠离体气管（舒张作用）、心房（变时作用）和灌注后肢（血管舒张）的活性。
具有间苯二酚核的化合物在所有三种制剂上的效力较低，但对气管的选择性高于具有儿茶酚核的化合物。
在儿茶酚和间苯二酚化合物中，在N-异丙基中取代对羟基苯基，或用N-叔丁基取代N-异丙基（有无对羟基苯基），可增强对气管的效力并有利于对气管的选择性。
相对于异丙肾上腺素，大多数化合物，尤其是间苯二酚类化合物，在后肢上的效力远低于在气管上的效力。
讨论了与β-肾上腺素能受体选择性的定量测量和亚分类相关的一些问题。
相似文献
1
Potency and selectivity in vitro of compounds related to isoprenaline and orciprenaline on beta-adrenoceptors in the guinea-pig.豚鼠体内与异丙肾上腺素和奥西那林相关的化合物对β-肾上腺素能受体的体外效力和选择性
Br J Pharmacol. 1974 Nov;52(3):407-17. doi: 10.1111/j.1476-5381.1974.tb08610.x.
2
The influence of atrial temperature on the in vitro selectivity of isoprenaline for atria and of orciprenaline for trachea.心房温度对异丙肾上腺素对心房的体外选择性以及奥西那林对气管的体外选择性的影响。
J Pharm Pharmacol. 1974 Oct;26(10):826-8. doi: 10.1111/j.2042-7158.1974.tb09183.x.
3
A comparison of the beta-adrenoreceptor stimulant properties of isoprenaline, with those of orciprenaline, salbutamol, soterenol and trimetoquinol on isolated atria and trachea of the guinea pig.异丙肾上腺素与奥西那林、沙丁胺醇、索布特罗和曲美托喹啉对豚鼠离体心房和气管的β-肾上腺素能受体刺激特性比较。
J Pharm Pharmacol. 1970 Jan;22(1):61-3. doi: 10.1111/j.2042-7158.1970.tb08388.x.
4
Comparison of the bronchodilator and cardiovascular actions of salbutamol, isoprenaline and orciprenaline in guinea-pigs and dogs.沙丁胺醇、异丙肾上腺素和奥西那林对豚鼠和犬支气管扩张及心血管作用的比较
Br J Pharmacol. 1971 Nov;43(3):624-38. doi: 10.1111/j.1476-5381.1971.tb07192.x.
5
The contribution of extraneuronal uptake to the trachea-blood vessel selectivity of beta-adrenoceptor stimulants in vitro in guinea-pigs.在豚鼠体外实验中，非神经元摄取对β-肾上腺素能受体兴奋剂气管-血管选择性的作用。
Br J Pharmacol. 1976 Jul;57(3):369-73. doi: 10.1111/j.1476-5381.1976.tb07675.x.
6
Hexoprenaline: beta-adrenoreceptor selectivity in isolated tissues from the guinea-pig.己双肾上腺素：豚鼠离体组织中的β-肾上腺素能受体选择性
Clin Exp Pharmacol Physiol. 1975 Nov-Dec;2(6):541-7. doi: 10.1111/j.1440-1681.1975.tb01859.x.
7
Assessment of the selectivity of OPC-2009, a new beta2-adrenoceptor stimulatn, by the use of the blood-perfused trachea in situ and of the isolated blood-perfused papillary muscle of the dog.通过使用原位血液灌注气管和犬离体血液灌注乳头肌来评估新型β2肾上腺素能激动剂OPC-2009的选择性。
Br J Pharmacol. 1977 Sep;61(1):9-17. doi: 10.1111/j.1476-5381.1977.tb09734.x.
8
[Effect of a new bronchodilator, S-1540 (Bitolterol) and S-1541 on the tracheo-bronchial and cardiovascular system].[新型支气管扩张剂S - 1540（双甲苯喘定）和S - 1541对气管支气管及心血管系统的作用]
Nihon Yakurigaku Zasshi. 1975 Oct;71(7):739-52. doi: 10.1254/fpj.71.739.
9
The use of functional antagonism to determine whether beta-adrenoceptor agonists must have a lower efficacy than isoprenaline to be trachea-atria selective in vitro in guinea-pigs.利用功能拮抗作用来确定β-肾上腺素能受体激动剂在豚鼠体外实验中对气管-心房具有选择性时，其效能是否必定低于异丙肾上腺素。
Br J Pharmacol. 1977 Jun;60(2):255-62. doi: 10.1111/j.1476-5381.1977.tb07748.x.
10
Beta-adrenoceptor antagonist activity of 3-methoxyisoprenaline.3-甲氧基异丙肾上腺素的β-肾上腺素能受体拮抗活性。
Br J Pharmacol. 1971 Jan;41(1):113-21. doi: 10.1111/j.1476-5381.1971.tb09941.x.
引用本文的文献
1
Actions of locally administered adrenoceptor agonists on increased plasma protein extravasation and blood flow in guinea-pig skin.局部应用肾上腺素能受体激动剂对豚鼠皮肤血浆蛋白外渗增加和血流的作用。
Br J Pharmacol. 1980 Nov;70(3):461-7. doi: 10.1111/j.1476-5381.1980.tb08724.x.
2
A study of some propranolol analogues for selective beta-adrenoceptor antagonism using A2 values on isolated trachea and atria from guinea-pig.一项使用豚鼠离体气管和心房的A2值对某些普萘洛尔类似物进行选择性β-肾上腺素能受体拮抗作用的研究。
Br J Pharmacol. 1980 Apr;68(4):705-10. doi: 10.1111/j.1476-5381.1980.tb10863.x.
3
In vitro inhibition of intestinal motility by phenylethanolaminotetralines: evidence of atypical beta-adrenoceptors in rat colon.苯乙醇胺四氢萘对肠道运动的体外抑制作用：大鼠结肠中非典型β-肾上腺素能受体的证据
Br J Pharmacol. 1990 Aug;100(4):831-9. doi: 10.1111/j.1476-5381.1990.tb14100.x.
4
Inhaled beta 2-adrenoceptor agonists in asthma: help or hindrance?吸入性β2肾上腺素能受体激动剂在哮喘治疗中：是助力还是阻碍？
Br J Clin Pharmacol. 1992 Feb;33(2):129-38. doi: 10.1111/j.1365-2125.1992.tb04014.x.
5
Risks versus benefits of inhaled beta 2-agonists in the management of asthma.吸入性β2受体激动剂在哮喘管理中的风险与获益
Drug Saf. 1992 Jan-Feb;7(1):54-70. doi: 10.2165/00002018-199207010-00007.
6
The opposed influences of beta-adrenergic stimulation and adenosine on the frequency-force relationship of isolated left atria of guinea-pigs.β-肾上腺素能刺激和腺苷对豚鼠离体左心房频率-张力关系的相反影响。
Experientia. 1977 Dec 15;33(12):1629-31. doi: 10.1007/BF01934040.
7
The importance of choice of agonist in studies designed to predict beta 2 : beta 1 adrenoceptor selectivity of antagonists from pA2 values on guinea-pig trachea and atria.在旨在根据豚鼠气管和心房上的pA2值预测拮抗剂的β2:β1肾上腺素能受体选择性的研究中，激动剂选择的重要性。
Naunyn Schmiedebergs Arch Pharmacol. 1979 Sep;308(3):183-90. doi: 10.1007/BF00501381.
8
The acute effects of the administration of rimiterol aerosol in asthmatic children.间羟喘息定气雾剂对哮喘患儿的急性作用。
Br J Clin Pharmacol. 1978 Jul;6(1):59-62. doi: 10.1111/j.1365-2125.1978.tb01682.x.
9
An in vitro comparison of beta-adrenoceptor stimulants on potassium-depolarized uterine preparations from guinea-pigs.β-肾上腺素能兴奋剂对豚鼠低钾去极化子宫标本的体外比较
Br J Pharmacol. 1978 Feb;62(2):227-33. doi: 10.1111/j.1476-5381.1978.tb08450.x.
10
The use of functional antagonism to determine whether beta-adrenoceptor agonists must have a lower efficacy than isoprenaline to be trachea-atria selective in vitro in guinea-pigs.利用功能拮抗作用来确定β-肾上腺素能受体激动剂在豚鼠体外实验中对气管-心房具有选择性时，其效能是否必定低于异丙肾上腺素。
Br J Pharmacol. 1977 Jun;60(2):255-62. doi: 10.1111/j.1476-5381.1977.tb07748.x.
本文引用的文献
1
Differentiation of receptors responsive to isoproterenol.对异丙肾上腺素产生反应的受体的分化
Life Sci. 1967 Nov 1;6(21):2241-9. doi: 10.1016/0024-3205(67)90031-8.
2
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.
3
Salbutamol: a new, selective beta-adrenoceptive receptor stimulant.沙丁胺醇：一种新型的选择性β-肾上腺素能受体兴奋剂。
Br J Pharmacol. 1969 Jan;35(1):141-51. doi: 10.1111/j.1476-5381.1969.tb07975.x.
4
New sympathomimetic amines: actions on catecholamine receptors.新型拟交感胺类：对儿茶酚胺受体的作用。
Br J Pharmacol. 1968 Nov;34(3):698P.
5
Pharmacologic potency and selectivity of a new bronchodilator agent: soterenol (MJ 1992).一种新型支气管扩张剂的药理效力和选择性：索特仑（MJ 1992）。
J Pharmacol Exp Ther. 1968 Dec;164(2):290-301.
6
The interaction of cocaine and propranolol with catecholamines on guinea pig trachea.可卡因与普萘洛尔在豚鼠气管上与儿茶酚胺的相互作用。
Eur J Pharmacol. 1967 Nov;2(2):77-82. doi: 10.1016/0014-2999(67)90028-3.
7
The pharmacological differentiation of adrenergic receptors.肾上腺素能受体的药理学分化
Ann N Y Acad Sci. 1967 Feb 10;139(3):553-70. doi: 10.1111/j.1749-6632.1967.tb41229.x.
8
Actions of the sympathomimetic bronchodilator, rimiterol (R798), on the cardiovascular, respiratory and skeletal muscle systems of the anaesthetized cat.拟交感神经支气管扩张剂瑞米特罗（R798）对麻醉猫的心血管、呼吸和骨骼肌系统的作用。
Br J Pharmacol. 1972 Aug;45(4):574-83. doi: 10.1111/j.1476-5381.1972.tb08115.x.
9
The beta-adrenoceptor blocking properties of the alpha-methyl analogues of propranolol and practolol in the anaesthetized dog.普萘洛尔和普拉洛尔的α-甲基类似物在麻醉犬体内的β-肾上腺素能受体阻断特性
Br J Pharmacol. 1973 Nov;49(3):514-26. doi: 10.1111/j.1476-5381.1973.tb17262.x.
10
An examination of some -adrenoreceptor stimulants for selectivity using the isolated trachea and atria of the guinea pig.使用豚鼠离体气管和心房对某些β-肾上腺素受体激动剂的选择性进行研究。
Eur J Pharmacol. 1972 Sep;19(3):371-9. doi: 10.1016/0014-2999(72)90104-5.
Zotero 插件