| Autor: |
Cha, J. H., Zou, M.-F., Adkins, E. M., Rasmussen, S. G. F., Loland, C. J., Schoenenberger, B., Gether, U., Newman, A. H. |
| Zdroj: |
Journal of Medicinal Chemistry; December 2005, Vol. 48 Issue: 24 p7513-7516, 4p |
| Abstrakt: |
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 2β-carbomethoxy-3β-(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. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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