Intrinsic sympathomimetic activity of β-adrenoceptor blocking drugs at cardiac and vascular β-adrenoceptors
Intrinsic sympathomimetic activity of β-adrenoceptor blocking drugs at cardiac and vascular β-adrenoceptors
复制标题
β-肾上腺素受体阻滞药物对心脏和血管 β-肾上腺素受体的内在拟交感活性
DOI：
10.1016/0024-3205(78)90516-7
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发表时间：
1978
期刊：
影响因子：
6.1
通讯作者：
V. Chapman
中科院分区：
文献类型：
--
作者：
T. C. Hamilton;V. Chapman
在麻醉后，利血平化的大鼠异丙肾上腺素引起心动过速和抑制反应：这些作用是由于β1（心脏）和β2（血管）肾上腺素受体的刺激。沙丁胺醇也会引起心动过速和抑制反应。（±）和（−）丁胺醇及其甲醇和酮代谢物产生类似的反应，表明β1和β2肾上腺素受体的内在拟交感神经活性（ISA）；（+） bufuralol缺乏ISA。品多洛尔和奥普萘洛尔也会引起心动过速和抑制作用；奥普萘洛尔产生后一种反应的活性较弱。心得安不含ISA；4-羟基心得安可引起心动过速，血压下降可忽略不计。Practolol只会引起心动过速。这些结果表明利血平化大鼠是证明ISA β1和β2肾上腺素受体的合适实验模型。非选择性β-肾上腺素受体阻断药物产生β2（血管）肾上腺素受体和β1（心脏）肾上腺素受体的刺激。
In the anaesthetised, reserpinised rat isoprenaline causes tachycardia and depressor responses: these effects are due to stimulation ofβ1(cardiac) andβ2(vascular) adrenoceptors. Salbutamol also produces tachycardia and depressor responses. (±) and (−) bufuralol, and its carbinol and ketone metabolites, produce similar responses indicating intrinsic sympathomimetic activity (ISA) atβ1andβ2adrenoceptors; (+) bufuralol lacks ISA. Pindolol and oxprenolol also cause tachycardia and a depressor effect; oxprenolol is weakly active in producing the latter response. Propranolol is devoid of ISA; 4-hydroxypropranolol causes tachycardia with a negligible fall in blood pressure. Practolol causes only tachycardia. These results demonstrate that the reserpinised rat is a suitable experimental model for the demonstration of ISA atβ1andβ2adrenoceptors. Non-selective β-adrenoceptor blocking drugs produce stimulation atβ2(vascular) adrenoceptors as well asβ1(cardiac) adrenoceptors.