Human cardiac beta-adrenergic receptors: subtype heterogeneity delineated by direct radioligand binding.
Human cardiac beta-adrenergic receptors: subtype heterogeneity delineated by direct radioligand binding.
复制标题
人心脏β-肾上腺素能受体：通过直接放射性配体结合描绘的亚型异质性。
DOI：
10.1016/0024-3205(83)90796-8
复制
发表时间：
1983
期刊：
影响因子：
6.1
通讯作者：
Lefkowitz,RJ
中科院分区：
文献类型：
--
作者：
Stiles,GL;Taylor,S;Lefkowitz,RJ
人心肌β-肾上腺素能受体直接识别和特点使用高亲和力拮抗剂放射性配体[125 I]碘氰基吲哚洛尔。β 1和β 2肾上腺素能受体共存于左心室和右心房。通过使用竞争性放射性配体结合和计算机建模技术，采用亚型选择性药物阿替洛尔（β 1选择性）和锌特罗（β 2选择性），确定两种受体亚型的相对比例。左心室含有86 ± 1% β 1和14 ± 1% β 2肾上腺素能受体，而右心房含有74 ± 6% β 1和26 ± 6% β 2肾上腺素能受体。β 2肾上腺素能受体在人心脏中的直接证明，在右心房中的比例较高，这与药理学数据一致，并支持人体中肾上腺素能受体激动剂的变时作用可能由β 1和β 2肾上腺素能受体介导的观点。
Human myocardial beta-adrenergic receptors were directly identified and characterized using the high affinity antagonist radioligand [125I] iodocyanopindolol. Beta1and beta2adrenergic receptors were found to coexist in both the left ventricle and right atrium. The relative proportions of the two receptor subtypes were determined by the use of competition radioligand binding and computer modelling techniques employing the subtype selective agents atenolol (beta1selective) and zinterol (beta2selective). The left ventricle contains 86 ± 1% beta1and 14 ± 1% beta2adrenergic receptors while the right atrium contains 74 ± 6% beta1and 26 ± 6% beta2adrenergic receptors. The direct demonstration of beta2adrenergic receptors in the human heart, with a higher proportion in the right atrium agrees with pharmacologic data and supports the notion that chronotropic effects of adrenergic agonists in man may be mediated by both beta1and beta2adrenergic receptors.