Jarrott B, Louis W J, Summers R J
Chest. 1983 Feb;83(2 Suppl):339-40.
alpha-Adrenoceptors in brain can be studied readily by radioligand binding techniques. This provides valuable information not only on the distribution of receptors in brain regions, but also on the regulation of receptors. The usefulness of this technique is dependent in part on a radioligand with high specificity for the receptor under study. Our studies have shown that 3H-clonidine does not bind exclusively to alpha 2-adrenoceptor subtypes, but also interacts with alpha 1-adrenoceptors. In contrast, 3H-guanfacine labels a high affinity alpha 2 subtype with good selectivity, but 3H-lofexidine probably labels with both alpha 2 and alpha 1-adrenoceptor binding sites.
大脑中的α-肾上腺素能受体可以通过放射性配体结合技术轻松进行研究。这不仅提供了关于受体在脑区分布的有价值信息，还提供了关于受体调节的信息。该技术的实用性部分取决于对所研究受体具有高特异性的放射性配体。我们的研究表明，3H-可乐定并非仅与α2-肾上腺素能受体亚型结合，还与α1-肾上腺素能受体相互作用。相比之下，3H-胍法辛能高亲和力且选择性良好地标记α2亚型，但3H-洛非西定可能同时标记α2和α1-肾上腺素能受体结合位点。
