Novel and High Affinity Fluorescent Ligands for the Serotonin Transporter Based on (S)-Citalopram | Zendy

Vivek Kumar | Zendy; Troels RahbekClemmensen | Zendy; Christian B. Billesbølle | Zendy; Trine N. Jørgensen | Zendy; Ulrik Gether | Zendy; Amy Hauck Newman | Zendy

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Novel and High Affinity Fluorescent Ligands for the Serotonin Transporter Based on (S)-Citalopram

Author(s) -

Vivek Kumar,

Troels RahbekClemmensen,

Christian B. Billesbølle,

Trine N. Jørgensen,

Ulrik Gether,

Amy Hauck Newman

Publication year - 2014

Publication title -

acs medicinal chemistry letters

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.065

H-Index - 66

ISSN - 1948-5875

DOI - 10.1021/ml5000806

Subject(s) - citalopram , serotonin transporter , serotonin , fluorescence , transporter , chemistry , computational biology , pharmacology , biochemistry , combinatorial chemistry , medicine , biology , receptor , gene , physics , quantum mechanics

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.

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