Abstract
As the serotonin transporter (SERT) is involved in several neurodegenerative and psychiatric disorders; radiopharmaceuticals to image the SERT by PET would be valuable in studying these diseases. To this end we synthesized diphenyloxide derivatives and sulfide analogs, as new tracers, incorporating a fluorine or oxyalkyl fluorinated group on 4' or 5'-position on phenyl ring B. Three of these exhibited good to high in vitro affinity (7<K(i)<8 nM) and selectivity for the SERT over the other monoamine transporters.
Copyright (c) 2009 Elsevier Ltd. All rights reserved.
Publication types
-
Research Support, N.I.H., Extramural
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Binding, Competitive
-
Cell Line, Tumor
-
Dopamine Plasma Membrane Transport Proteins / metabolism
-
Halogenation
-
Humans
-
Ligands
-
Norepinephrine Plasma Membrane Transport Proteins / metabolism
-
Phenyl Ethers / chemical synthesis
-
Phenyl Ethers / chemistry*
-
Phenyl Ethers / pharmacology*
-
Serotonin Plasma Membrane Transport Proteins / metabolism*
-
Sulfides / chemical synthesis
-
Sulfides / chemistry
-
Sulfides / pharmacology
Substances
-
Dopamine Plasma Membrane Transport Proteins
-
Ligands
-
Norepinephrine Plasma Membrane Transport Proteins
-
Phenyl Ethers
-
SLC6A2 protein, human
-
Serotonin Plasma Membrane Transport Proteins
-
Sulfides