Rhodamine-labeled 2 beta-carbomethoxy-3 beta-(3,4-dichlorophenyl)- tropane analogues as high-affinity fluorescent probes for the dopamine transporter
- Authors
- Cha, JH; Zou, MF; Adkins, EM; Rasmussen, SGF; Loland, CJ; Schoenenberger, B; Gether, U; Newman, AH
- Issue Date
- 2005-12-01
- Publisher
- AMER CHEMICAL SOC
- Citation
- JOURNAL OF MEDICINAL CHEMISTRY, v.48, no.24, pp.7513 - 7516
- Abstract
- 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 2 beta-carbomethoxy-3 beta-(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 (K-i = 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.
- Keywords
- RESONANCE ENERGY-TRANSFER; RECEPTOR; ANTAGONIST; LIGANDS; RESONANCE ENERGY-TRANSFER; RECEPTOR; ANTAGONIST; LIGANDS; Dopamin transporter; Fluorescent Probe; Rhodamine; Tropane
- ISSN
- 0022-2623
- URI
- https://pubs.kist.re.kr/handle/201004/135898
- DOI
- 10.1021/jm050431y
- Appears in Collections:
- KIST Article > 2005
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