新型β-肾上腺素能受体激动剂MJ-9184-1在麻醉猫体内的药理作用。
Pharmacological actions of a new -adrenoceptor agonist, MJ-9184-1, in anaesthetized cats.
作者信息
Gwee M C, Nott M W, Raper C, Rodger I W
出版信息
Br J Pharmacol. 1972 Nov;46(3):375-85. doi: 10.1111/j.1476-5381.1972.tb08134.x.
Abstract
- The effects of (-)-isoprenaline and the new beta-adrenoceptor agonist, MJ-9184-1, on the lungs, on the cardiovascular system, and on slow contracting skeletal muscle have been compared in cats under chloralose anaesthesia.2. Both amines reduced the increases in airways resistance produced by 5-HT, depressed incomplete tetanic contractions of the soleus muscle, lowered the blood pressure and produced an increase in heart rate. In comparison with (-)-isoprenaline, MJ-9184-1 had a long duration of action.3. The effects of MJ-9184-1 and (-)-isoprenaline were antagonized by the beta-adrenoceptor antagonist, propranolol.4. MJ-9184-1 was approximately half as potent as (-)-isoprenaline in its effects on pulmonary resistance and soleus muscle contractility, and one seventh as potent in producing chronotropic effects in the heart.5. These results suggest that MJ-9184-1 possesses some specificity as a beta(2) receptor stimulant.
摘要
在氯醛糖麻醉的猫身上，比较了（-）-异丙肾上腺素和新型β-肾上腺素能受体激动剂MJ-9184-1对肺、心血管系统和慢收缩骨骼肌的作用。
两种胺类药物均能减轻5-羟色胺引起的气道阻力增加，抑制比目鱼肌的不完全强直收缩，降低血压并使心率加快。与（-）-异丙肾上腺素相比，MJ-9184-1的作用持续时间较长。
β-肾上腺素能受体拮抗剂普萘洛尔可拮抗MJ-9184-1和（-）-异丙肾上腺素的作用。
MJ-9184-1对肺阻力和比目鱼肌收缩力的作用约为（-）-异丙肾上腺素的一半，对心脏产生变时作用的效力为（-）-异丙肾上腺素的七分之一。
这些结果表明，MJ-9184-1作为一种β₂受体兴奋剂具有一定的特异性。
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