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大鼠脂解β-肾上腺素能受体:使用新型β-肾上腺素能受体激动剂的研究

The rat lipolytic beta-adrenoceptor: studies using novel beta-adrenoceptor agonists.

作者信息

Wilson C, Wilson S, Piercy V, Sennitt M V, Arch J R

出版信息

Eur J Pharmacol. 1984 May 4;100(3-4):309-19. doi: 10.1016/0014-2999(84)90007-4.

Abstract

EC50 and relative intrinsic activity values were obtained for isoprenaline, fenoterol, salbutamol, prenalterol and three new beta-adrenoceptor agonists, BRL 28410, BRL 35113 and BRL 35135 on rat white adipocyte lipolysis, rat atrial rate and tension, rat uterus tension and guinea-pig tracheal tension. Fenoterol and salbutamol were selective for tracheal and uterine responses, prenalterol was selective for atrial responses, but BRL 28410, BRL 35113 and BRL 35135 were selective for the adipocyte lipolytic response. pA2 values for propranolol, practolol, ICI 118,551 and sotalol were obtained on adipocytes, atria and trachea. pA2 values for propranolol and sotalol were much lower on adipocytes than on atria or trachea. The pA2 value for practolol was lower on adipocytes than on atria and the pA2 value for ICI 118,551 was lower on adipocytes than on trachea. Both agonist and antagonist studies therefore suggest that the rat adipocyte lipolytic receptor does not fit into the current beta 1/beta 2-adrenoceptor classification.

摘要

获得了异丙肾上腺素、非诺特罗、沙丁胺醇、普瑞特罗以及三种新型β-肾上腺素能受体激动剂BRL 28410、BRL 35113和BRL 35135对大鼠白色脂肪细胞脂解作用、大鼠心房率和张力、大鼠子宫张力以及豚鼠气管张力的半数有效浓度(EC50)和相对内在活性值。非诺特罗和沙丁胺醇对气管和子宫反应具有选择性,普瑞特罗对心房反应具有选择性,但BRL 28410、BRL 35113和BRL 35135对脂肪细胞脂解反应具有选择性。获得了普萘洛尔、醋丁洛尔、ICI 118,551和索他洛尔在脂肪细胞、心房和气管上的拮抗参数(pA2)值。普萘洛尔和索他洛尔在脂肪细胞上的pA2值远低于在心房或气管上的pA2值。醋丁洛尔在脂肪细胞上的pA2值低于在心房上的pA2值,ICI 118,551在脂肪细胞上的pA2值低于在气管上的pA2值。因此,激动剂和拮抗剂研究均表明,大鼠脂肪细胞脂解受体不符合当前的β1/β2-肾上腺素能受体分类。

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