Cha, JH Zou, MF Adkins, EM Rasmussen, SGF Loland, CJ Schoenenberger, B Gether, U Newman, AH 2024-01-21T04:01:52Z 2024-01-21T04:01:52Z 2021-09-01 2005-12-01 0022-2623 https://pubs.kist.re.kr/handle/201004/135898 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. English AMER CHEMICAL SOC RESONANCE ENERGY-TRANSFER RECEPTOR ANTAGONIST LIGANDS Rhodamine-labeled 2 beta-carbomethoxy-3 beta-(3,4-dichlorophenyl)- tropane analogues as high-affinity fluorescent probes for the dopamine transporter Article 10.1021/jm050431y 1 JOURNAL OF MEDICINAL CHEMISTRY, v.48, no.24, pp.7513 - 7516 JOURNAL OF MEDICINAL CHEMISTRY 48 24 7513 7516 scie scopus 000233654900002 Chemistry, Medicinal Pharmacology & Pharmacy Article RESONANCE ENERGY-TRANSFER RECEPTOR ANTAGONIST LIGANDS Dopamin transporter Fluorescent Probe Rhodamine Tropane