Rhodamine-labeled 2beta-carbomethoxy-3beta-(3,4-dichlorophenyl)tropane analogues as high-affinity fluorescent probes for the dopamine transporter
Research output: Contribution to journal › Journal article › Research › peer-review
Novel fluorescent ligands were synthesized to identify a high-affinity probe that would enable visualization of the dopamine transporter (DAT) in living cells. Fluorescent tags were extended from the N- or 2-position of 2beta-carbomethoxy-3beta-(3,4-dichlorophenyl)tropane, using an ethylamino linker. The resulting 2-substituted (5) and N-substituted (9) rhodamine-labeled ligands provided the highest DAT binding affinities expressed in COS-7 cells (Ki= 27 and 18 nM, respectively) in the series. Visualization of the DAT with 5 and 9 was demonstrated by confocal fluorescence laser scanning microscopy in stably transfected HEK293 cells.
Original language | English |
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Journal | Journal of Medicinal Chemistry |
Volume | 48 |
Issue number | 24 |
Pages (from-to) | 7513-6 |
Number of pages | 4 |
ISSN | 0022-2623 |
DOIs | |
Publication status | Published - 1 Dec 2005 |
- Animals, Cell Line, Cercopithecus aethiops, Cocaine, Dopamine Plasma Membrane Transport Proteins, Fluorescent Dyes, Humans, Microscopy, Confocal, Norepinephrine Plasma Membrane Transport Proteins, Rhodamines, Serotonin Plasma Membrane Transport Proteins, Structure-Activity Relationship, Tropanes
Research areas
ID: 47293421