普萘洛尔与MJ 1999对人体心脏β-肾上腺素能受体作用的比较。
Comparison of the effects of propranolol and MJ 1999 on cardiac beta-adrenoceptors in man.
作者信息
Kofi Ekue J M, Lowe D C, Shanks R G
出版信息
Br J Pharmacol. 1970 May;38(3):546-53. doi: 10.1111/j.1476-5381.1970.tb10596.x.
Abstract
- Propranolol, a beta-adrenoceptor blocking drug with local anaesthetic and a direct myocardial depressant action, and MJ 1999, a beta-adrenoceptor blocking drug which has no local anaesthetic or intrinsic sympathomimetic action, were compared for beta-adrenoceptor blocking activity in man.2. Propranolol was 2.67 times more active than MJ 1999 in reducing by 50% the tachycardia produced by the intravenous infusion of isoprenaline in healthy volunteers.3. Propranolol and MJ 1999 intravenously both reduced resting heart rate in the standing position and an exercise tachycardia, but there was no qualitative or quantitative difference between them.4. On oral administration, both propranolol and MJ 1999 reduced resting heart rate and an exercise induced tachycardia; propranolol was only slightly more active than MJ 1999.5. In patients with thyrotoxicosis propranolol was about twice as active as MJ 1999 in reducing the heart rate.
摘要
普萘洛尔是一种具有局部麻醉和直接心肌抑制作用的β-肾上腺素能受体阻断药物，MJ 1999是一种无局部麻醉或内在拟交感神经活性的β-肾上腺素能受体阻断药物，对二者在人体中的β-肾上腺素能受体阻断活性进行了比较。
在健康志愿者中，静脉输注异丙肾上腺素所诱发的心动过速，普萘洛尔使其降低50%的活性比MJ 1999高2.67倍。
普萘洛尔和MJ 1999静脉给药均能降低站立位静息心率和运动性心动过速，但二者之间在质或量上均无差异。
口服给药时，普萘洛尔和MJ 1999均能降低静息心率和运动诱发的心动过速；普萘洛尔的活性仅比MJ 1999略高。
在甲状腺毒症患者中，普萘洛尔降低心率的活性约为MJ 1999的两倍。
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