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Ahern DG, Seguin RJ, Filer CN. 
“Serotonin receptor agonists buspirone and (+/-)-DOB: Tritiation at high specific activity”. 
Journal of Radioanalytical and Nuclear Chemistry. 2004 Jan 10;261(2):465-7.
The serotonin receptor has been one of the most actively studied neurochemical systems because of its key role in so many diverse biological processes and disorders such as anxiety, obesity, sleep apnea and schizophrenia. With clarified understanding, this receptor class has been further subdivided into a complex array of multiple binding sites based on biochemical and pharmacological evidence.1 To better understand the location and function of these specific subclasses and accelerate the nomination of effective drug candidates for serotonergic ailments, neuroscientists have labored to identify high affinity agonists and antagonists for them.

Our laboratories have had a long-standing commitment to radiolabeling such ligands as tools for receptor binding assay studies,2,3 and we now report the tritiation of the serotonin receptor agonists buspirone 1 and (+/-)-DOB 4. Indeed, the contrasting structures of 1 and 4 well illustrate the rich architectural diversity within the serotonin receptor ligand family and the varied strategies often required to label them with tritium (Scheme 1).
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