The synthesis and preliminary characterization of three radioiodinated alph
a (1) adrenergic receptor ligands [I-125]5a-c are described. These tracers
are analogs of L-760,478, 1b, itself an analog of prazosin, 1a. The highest
affinity tracer, [I-125]5a, has six fold higher affinity for the alpha (1)
receptor subtypes than prazosin. These ligands could be useful for autorad
iographic studies of the alpha (1) receptor subtypes.