872460-76-9Relevant articles and documents
Rhodamine-labeled 2β-carbomethoxy-3β-(3,4-dichlorophenyl)tropane analogues as high-affinity fluorescent probes for the dopamine transporter
Cha, Joo Hwan,Zou, Mu-Fa,Adkins, Erika M.,Rasmussen, S?ren G. F.,Loland, Claus Juul,Schoenenberger, Bernhard,Gether, Ulrik,Newman, Amy Hauck
, p. 7513 - 7516 (2007/10/03)
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.