利用功能拮抗作用来确定β-肾上腺素能受体激动剂在豚鼠体外实验中对气管-心房具有选择性时，其效能是否必定低于异丙肾上腺素。
The use of functional antagonism to determine whether beta-adrenoceptor agonists must have a lower efficacy than isoprenaline to be trachea-atria selective in vitro in guinea-pigs.
作者信息
O'Donnell S R, Wanstall J C
出版信息
Br J Pharmacol. 1977 Jun;60(2):255-62. doi: 10.1111/j.1476-5381.1977.tb07748.x.
Abstract
1 The relative efficacies of three trachea-atria selective beta-adrenoceptor agonists, fenoterol, Me 506 and Me 454, compared to isoprenaline, were determined on both trachea and atria of guinea-pigs. 2 On tracheal preparations the beta-adrenoceptor agonists were used as functional antagonists of carbachol and a comparison of the maximum shifts in the carbachol concentration-response line produced by each of the beta-adrenoceptor agonists provided a comparison of their efficacies. 3 On atrial preparations carbachol was used as a functional antagonist of the beta-adrenoceptor agonists and comparison of the maximum responses to the beta-adrenoceptor agonists in the presence of carbachol provided a comparison of their efficacies. 4 On trachea and atria the order of efficacy of the compounds was Me454 greater than Me506 greater than or equal to isoprenaline=fenoterol. 5. The results indicated that high efficacy in a non-catechol beta-adrenoceptor agonist is possible provided there is a favourable N-substituent group. 6 Since Me 454, Me 506 and fenoterol, which are trachea-atria selective, have effficacies equal to or greater than that of isoprenaline, which is non-selective, it is concluded that low efficacy in a compound is not essential for it to show trachea-atria selectivity in vitro in guinea-pigs.
摘要
- 测定了三种气管 - 心房选择性β - 肾上腺素能受体激动剂非诺特罗、Me 506和Me 454与异丙肾上腺素相比，对豚鼠气管和心房的相对效能。2. 在气管制备物上，β - 肾上腺素能受体激动剂用作卡巴胆碱的功能性拮抗剂，比较每种β - 肾上腺素能受体激动剂引起的卡巴胆碱浓度 - 反应线的最大位移，可对它们的效能进行比较。3. 在心房制备物上，卡巴胆碱用作β - 肾上腺素能受体激动剂的功能性拮抗剂，比较在有卡巴胆碱存在时对β - 肾上腺素能受体激动剂的最大反应，可对它们的效能进行比较。4. 在气管和心房上，化合物的效能顺序为Me454大于Me506大于或等于异丙肾上腺素 = 非诺特罗。5. 结果表明，只要有合适的N - 取代基团，非儿茶酚β - 肾上腺素能受体激动剂就可能具有高效能。6. 由于具有气管 - 心房选择性的Me 454、Me 506和非诺特罗的效能等于或大于非选择性的异丙肾上腺素，因此得出结论，化合物的低效能并非其在豚鼠体外显示气管 - 心房选择性所必需。
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