The synthesis and biodistribution of 3‐(4′‐[125I]‐iodophenyl)‐4‐aminobutyric acid, a radioiodinated analogue of baclofen

Abstract Baclofen has been found to bind to receptors in the central nervous system that are specific for γ‐aminobutyric acid (GABA), a well known inhibitory neurotransmitter. This paper describes the synthesis of a radioiodinated analog of baclofen as part of an effort to develop receptor probes useful in single photon emission computed tomography. Preliminary biodistribution studies showed the radioiodinationed analog to be essentially stable to in vivo deiodination and have a distribution profile similar to that of baclofen.