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Novel and high affinity fluorescent ligands for the serotonin transporter based on (s)-citalopram.

ABSTRACT: Novel rhodamine-labeled ligands, based on (S)-citalopram, were synthesized and evaluated for uptake inhibition at the human serotonin, dopamine, and norepinephrine transporters (hSERT, hDAT, and hNET, respectively) and for binding at SERT, in transiently transfected COS7 cells. Compound 14 demonstrated high affinity binding and selectivity for SERT (K i = 3 nM). Visualization of SERT, using confocal laser scanning microscopy, validated compound 14 as a novel tool for studying SERT expression and distribution in living cells.

SUBMITTER: Kumar V

PROVIDER: S-EPMC4060933 | biostudies-literature | 2014 Jun

REPOSITORIES: biostudies-literature

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Novel and high affinity fluorescent ligands for the serotonin transporter based on (s)-citalopram.

Kumar Vivek V Rahbek-Clemmensen Troels T Billesbølle Christian B CB Jorgensen Trine Nygaard TN Gether Ulrik U Newman Amy Hauck AH

ACS medicinal chemistry letters 20140327 6

Novel rhodamine-labeled ligands, based on (S)-citalopram, were synthesized and evaluated for uptake inhibition at the human serotonin, dopamine, and norepinephrine transporters (hSERT, hDAT, and hNET, respectively) and for binding at SERT, in transiently transfected COS7 cells. Compound 14 demonstrated high affinity binding and selectivity for SERT (K i = 3 nM). Visualization of SERT, using confocal laser scanning microscopy, validated compound 14 as a novel tool for studying SERT expression and ...[more]

PMID: 24944746

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