Title:Fluorinated Diaryl Sulfides
VOLUME: 13 ISSUE: 8
Author(s):Nashwa Jarkas
Affiliation:Emory University School of Medicine, Center for Systems Imaging, Wesley Woods Health Center, 1841 Clifton Road, NE, Dpt. of Radiology and Imaging Sciences, 2nd Floor, Room # 212, Atlanta, GA 30329.
Keywords:Biphenylthiols, Diaryl Sulfides, Diphenyl Sulfides, Fluorine-18, Phenylthiobenzylamines, Serotonin Transporter.
Abstract:Diaryl sulfides also known as diphenyl sulfides, phenylthiobenzylamines, and biphenylthiols are a class of
compounds with phenylthiophenyl scaffold that have been validated as biomarkers to label the brain serotonin transporter
(SERT), in vivo. The development of those synthetic and non-natural compounds started more than a decade ago when the
observation that 5-chloro-((2-((dimethylamino)methyl)phenyl)thio)benzene-methanol hydrochloride also called 403U76
inhibited the serotonin and norepinephrine uptake into rat brain synaptosomes, led to the preparation of few derivatives
based on 403U76 chemical structure. The new class of compounds, called the diaryl sulfide family, was investigated as
biomarkers for the brain SERT. The promising data demonstrated by the carbon-11 labeled diaryl sulfides led to the translation
of few of them into humans and the further evaluation of the phenylthiophenyl core structure by developing some
fluorinated derivatives. This review will mainly focus on the fluorinated diaryl sulfides as fluorine-containing tracers validated
to image the human brain SERT using positron emission tomography.
