盐酸 1 -（对 - 烯丙基苯氧基）- 3 - 异丙氨基 - 2 - 丙醇（h 64 - 52）对麻醉犬β - 肾上腺素能受体的选择性阻断作用

Selective blockade of beta-adrenoceptors by 1-(p-allylphenoxy)-3-isopropylamino-2 propanol hydrochloride (h 64-52) in the anaesthetized dog.

Levy B

Br J Pharmacol. 1973 Feb;47(2):398-407. doi: 10.1111/j.1476-5381.1973.tb08337.x.

Abstract

The beta-adrenoceptor blocking properties of 1-(p-allylphenoxy)-3-isopropylamino-2-propanol hydrochloride (H 64/52) on the cardiovascular and bronchomotor responses to isoprenaline have been determined in the anaesthetized dog.2. H 64/52 selectively blocked the isoprenaline-induced increase in heart rate, contractile force and reduction in airway pressure in the same dose range.3. H 64/52 produced a minimal blockade of vascular beta-adrenoceptors which was apparent only when the isoprenaline-induced fall in diastolic pressure was considered. No significant vascular beta-adrenoceptor blockade with H 64/52 could be shown with the femoral arterial flow or hind-limb perfusion studies.4. These results further support the hypothesis that several different beta-adrenoceptor subtypes exist in the dog. The beta-adrenoceptors subserving cardiac stimulation and bronchodilation appear to be similar and both differ from the beta-adrenoceptor subserving vasodilatation.

摘要

在麻醉犬中测定了1-（对烯丙基苯氧基）-3-异丙氨基-2-丙醇盐酸盐（H 64/52）对心血管及支气管运动对异丙肾上腺素反应的β-肾上腺素受体阻断特性。
H 64/52在相同剂量范围内选择性地阻断了异丙肾上腺素诱导的心率增加、收缩力增强及气道压力降低。
H 64/52对血管β-肾上腺素受体产生的阻断作用极小，仅在考虑异丙肾上腺素诱导的舒张压下降时才明显。在股动脉血流或后肢灌注研究中，未显示H 64/52对血管β-肾上腺素受体有明显阻断作用。
这些结果进一步支持了犬体内存在几种不同β-肾上腺素受体亚型的假说。介导心脏兴奋和支气管舒张的β-肾上腺素受体似乎相似，且均与介导血管舒张的β-肾上腺素受体不同。