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β1和β2肾上腺素能受体不同的空间特征。

Different steric characteristics of beta 1- and beta 2-adrenoceptors.

作者信息

Morris T H, Kaumann A J

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1984 Sep;327(2):176-9. doi: 10.1007/BF00500913.

Abstract

beta-Adrenoceptors of lung (75% beta 2) and heart (95% beta 1) of calf were labelled with 3H-(-)-propranolol. The stereoisomers of 10 ligands were used to inhibit the binding of 3H-(-)-propranolol to membrane particles. The affinity ratio of stereoisomers is consistently greater for beta 1-adrenoceptors than for beta 2-adrenoceptors, regardless of whether the ligands are agonists, partial agonists or antagonists. The beta 1-adrenoceptor appears to possess stricter steric requirements than the beta 2-adrenoceptor. This property may prove helpful in differentiating the beta-adrenoceptor subtypes during receptor solubilization and purification.

摘要

用³H-(-)-普萘洛尔标记小牛肺(75%为β₂)和心脏(95%为β₁)的β-肾上腺素能受体。使用10种配体的立体异构体抑制³H-(-)-普萘洛尔与膜颗粒的结合。无论配体是激动剂、部分激动剂还是拮抗剂,β₁-肾上腺素能受体的立体异构体亲和力比始终大于β₂-肾上腺素能受体。β₁-肾上腺素能受体似乎比β₂-肾上腺素能受体具有更严格的空间要求。这一特性可能有助于在受体溶解和纯化过程中区分β-肾上腺素能受体亚型。

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