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β-肾上腺素能受体拮抗剂的比较性部分激动剂活性。

Comparative partial agonist activity of -adrenoceptor antagonists.

作者信息

Nayler W G

出版信息

Br J Pharmacol. 1972 Jun;45(2):382-4. doi: 10.1111/j.1476-5381.1972.tb08094.x.

DOI:10.1111/j.1476-5381.1972.tb08094.x
PMID:4403104
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1666140/
Abstract

Inotropic dose-response curves were constructed for a series of beta-adrenoceptor antagonists, based on the inotropic responses of isolated dog trabecular muscles stimulated to contract at a regular rate. Propranolol exerted only a negative inotropic effect but K01366, LB46, oxprenolol and practolol all evoked a positive inotropic response, whether or not catecholamine-depleted muscles were used. The order of potency for this positive inotropic activity was K01366>LB46>oxprenolol>practolol. The duration of the positive inotropic response to the antagonists was more prolonged than that due to isoprenaline. Propranolol significantly reduced the positive inotropic response to K01366, LB46, oxprenolol and practolol.

摘要

基于以恒定速率刺激收缩的离体犬小梁肌的变力反应，构建了一系列β-肾上腺素能受体拮抗剂的变力剂量反应曲线。普萘洛尔仅产生负性变力作用，但无论是否使用去甲肾上腺素耗竭的肌肉，K01366、LB46、氧烯洛尔和普拉洛尔均能引发正性变力反应。这种正性变力活性的效价顺序为K01366>LB46>氧烯洛尔>普拉洛尔。拮抗剂产生的正性变力反应持续时间比异丙肾上腺素引起的更长。普萘洛尔显著降低了对K01366、LB46、氧烯洛尔和普拉洛尔的正性变力反应。

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Comparative partial agonist activity of -adrenoceptor antagonists.β-肾上腺素能受体拮抗剂的比较性部分激动剂活性。
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引用本文的文献

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beta-Adrenoceptor blocking agents as partial agonists in isolated heart muscle: dissociation of stimulation and blockade.β-肾上腺素能受体阻断剂在离体心肌中作为部分激动剂：刺激与阻断的解离
Naunyn Schmiedebergs Arch Pharmacol. 1980 Apr;311(3):237-48. doi: 10.1007/BF00569403.
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The effects of three beta-adrenoceptor blocking drugs on isolated preparations of skeletal and cardiac muscle.三种β-肾上腺素能受体阻断药物对骨骼肌和心肌离体标本的作用。
Br J Pharmacol. 1974 Oct;52(2):275-81. doi: 10.1111/j.1476-5381.1974.tb09710.x.
3
Haemodynamic response to graded exercise during chronic beta-adrenergic blockade with bunitrolol, an agent with intrinsic sympathomimetic activity.在使用具有内在拟交感活性的药物布尼洛尔进行慢性β-肾上腺素能阻滞剂治疗期间，对分级运动的血流动力学反应。
Eur J Clin Pharmacol. 1977 Dec 16;12(5):333-9. doi: 10.1007/BF00562447.

本文引用的文献

1
Effect of o-2-hydroxy-3-(tert.-butylamino) propoxybenzonitrile HCl (KO 1366) on beta adrenergic receptors in the cardiovascular system.盐酸邻-2-羟基-3-（叔丁氨基）丙氧基苯甲腈（KO 1366）对心血管系统中β肾上腺素能受体的作用。
J Pharmacol Exp Ther. 1972 Feb;180(2):302-16.
2
Comparative chronotropic activity of beta-adrenoceptive antagonists.β-肾上腺素能拮抗剂的比较变时活性
Br J Pharmacol. 1970 Nov;40(3):373-81. doi: 10.1111/j.1476-5381.1970.tb10619.x.
3
Evaluation of the cardiac effects of several beta adrenergic blocking agents.几种β-肾上腺素能阻滞剂的心脏效应评估。
Ann N Y Acad Sci. 1967 Feb 10;139(3):673-85. doi: 10.1111/j.1749-6632.1967.tb41237.x.
4
The effect of beta adrenergic antagonists on cardiac contractions, myofibrillar ATPase activity, high-energy phosphate stores and lipid-facilitated transfort of calciumiones.
J Pharmacol Exp Ther. 1969 Feb;165(2):225-33.

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