普萘洛尔诱发支气管收缩机制的研究
Investigation of the mechanism of propranolol-induced bronchoconstriction.
作者信息
Maclagan J, Ney U M
出版信息
Br J Pharmacol. 1979 Jul;66(3):409-18. doi: 10.1111/j.1476-5381.1979.tb10846.x.
Abstract
1 Dose-related increases in airways resistance (Raw) and decreases in dynamic lung compliance (Cdyn) were recorded in guinea-pigs and rats following intravenous injection of propranolol and of the cardioselective beta-adrenoceptor blocking drugs, atenolol and practolol. 2 The bronchoconstriction reached a peak in 2 to 4 min and subsided within 15 min. Repeated injections caused identical responses in the airways. 3 The isomer (+)-propranolol, which has only weak beta-adrenoceptor blocking activity, produced identical responses when given alone or when given after a dose of the racemate, sufficient to cause measurable beta-adrenoceptor blockade in the lungs. 4 After the initial bronchospasm had subsided, the beta-adrenoceptor blocking drugs and the isomer, (+)-propranolol, produced potentiation of the bronchoconstrictor effects of 5-hydroxytryptamine and histamine. 5 Both the bronchospasm and the potentiation occurred in adrenal demedullated rats. 6 The results indicate that the bronchoconstrictor effects of these drugs are unrelated to beta-adrenoceptor blockade in the airway smooth muscle.
摘要
- 在豚鼠和大鼠静脉注射普萘洛尔以及心脏选择性β - 肾上腺素受体阻断药阿替洛尔和美多心安后，记录到气道阻力（Raw）呈剂量相关性增加，动态肺顺应性（Cdyn）降低。2. 支气管收缩在2至4分钟内达到峰值，并在15分钟内消退。重复注射在气道中引起相同的反应。3. 仅具有弱β - 肾上腺素受体阻断活性的异构体（+） - 普萘洛尔，单独给药或在给予足以在肺部引起可测量的β - 肾上腺素受体阻断的外消旋体剂量后给药时，产生相同的反应。4. 在初始支气管痉挛消退后，β - 肾上腺素受体阻断药和异构体（+） - 普萘洛尔增强了5 - 羟色胺和组胺的支气管收缩作用。5. 支气管痉挛和增强作用均发生在肾上腺髓质切除的大鼠中。6. 结果表明，这些药物的支气管收缩作用与气道平滑肌中的β - 肾上腺素受体阻断无关。
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