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十种β-肾上腺素能受体阻滞剂和两种β-肾上腺素能受体激动剂的药理学和结合试验比较。

Comparison of pharmacological and binding assays for ten beta-adrenoceptor blocking agents and two beta-adrenoceptor agonists.

作者信息

Bieth N, Rouot B, Schwartz J, Velly J

出版信息

Br J Pharmacol. 1980 Mar;68(3):563-9. doi: 10.1111/j.1476-5381.1980.tb14572.x.

Abstract

1 The inhibition constants evaluated by binding assays for ten beta-adrenoceptor blocking agents and two beta-adrenoceptor agonists, were compared with the pA2 and pD2 values determined in vitro and in vivo. 2 There was only a limited correlation between beta 1 or beta 2 selectivities observed with the different methods. 3 Selectivity is generally less pronounced in binding assays than for in vivo and in vitro experiments.

摘要

1 通过结合试验评估的10种β-肾上腺素受体阻滞剂和2种β-肾上腺素受体激动剂的抑制常数,与在体外和体内测定的pA2和pD2值进行了比较。2 不同方法观察到的β1或β2选择性之间只有有限的相关性。3 与体内和体外实验相比,结合试验中的选择性通常不那么明显。

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