The synthesis and preliminary characterization of three radioiodinated α1-adrenergic receptor ligands [125I]5a–c are described. These tracers are analogs of L-760,478, 1b, itself an analog of prazosin, 1a. The highest affinity tracer, [125I]5a, has six fold higher affinity for the α1 receptor subtypes than prazosin. These ligands could be useful for autoradiographic studies of the α1 receptor subtypes. Copyright © 2001 John Wiley & Sons, Ltd.
本文描述了三种放射性
碘化α1-
肾上腺素能受体
配体[125I]5a-c的合成和初步表征。这些示踪剂是L-760,478,1b的类似物,而L-760,478,1b本身是
哌唑嗪1a的类似物。最高亲和力的示踪剂[125I]5a对α1受体亚型的亲和力比
哌唑嗪高六倍。这些
配体可用于α1受体亚型的自动放射研究。版权所有 © 2001 John Wiley & Sons, Ltd.