2-((2-((Dimethylamino)methyl)phenyl)thio)-5-[123I]iodophenylamine

Excerpt

Serotonin (5-HT) is now known to serve as the gastrointestinal signaling molecule and participate in the development of alcohol dependence (1, 2). It is also involved in a variety of physiological functions such as the post-meal satiety process, as well as the pathogenesis of Alzheimer’s and Parkinson’s diseases, anxiety, and depression (1-3). Imaging and data obtained by the analysis of resected tissue of epileptic patients and studies in animal models have provided much evidence that endogenous 5-HT, the activity of its receptors, and pharmaceuticals with 5-HT agonist and/or antagonist activities are believed to be involved in the pathogenesis of epilepsy (4). Thus, imaging of the 5-HT system (SERT) is considered important to understand a variety of neurological and psychiatric functions and disorders.

A variety of drugs have been labeled with radioactive iodine (¹²³I), carbon (¹¹C), or fluorine (¹⁸F) for imaging of the 5-HT receptor or transporter using positron emission tomography (PET) or single-photon emission computed tomography (SPECT) (5). In general, these compounds are either nonselective or have a low specificity for SERT (6). Subsequently, a new drug, 2-((2-((dimethylamino)methyl)phenyl)thio)-5-iodophenylamine (ADAM), radioiodinated with ¹²³I or ¹²⁵I, has been evaluated by several investigators for imaging of SERT.