877467-20-4Relevant academic research and scientific papers
One-step radiosynthesis of [18F]LBT-999: A selective radioligand for the visualization of the dopamine transporter with PET
Dolle, Frederic,Helfenbein, Julie,Hinnen, Francoise,Mavel, Sylvie,Mincheva, Zoia,Saba, Wadad,Schoellhorn-Peyronneau, Marie-Anne,Valette, Heric,Garreau, Lucette,Chalon, Sylvie,Halldin, Christer,Madelmont, Jean-Claude,Deloye, Jean-Bernard,Bottlaender, Michel,Le Gailliard, Joel,Guilloteau, Denis,Emond, Patrick
, p. 716 - 723 (2007)
LBT-999 (8-((E)-4-fluoro-but-2-enyl)-3-beta-p-tolyl-8-aza-bicyclo[3.2.1] octane-2-beta-carboxylicacid methyl ester) is a recently developed cocaine derivative belonging to a new generation of highly selective dopamine transporter (DAT) ligands (KD/s
Synthesis, fluorine-18 radiolabeling, and biological evaluation of N -((E)-4-fluorobut-2-en-1-yl)-2β-carbomethoxy-3β-(4?-halophenyl) nortropanes: Candidate radioligands for in vivo imaging of the brain dopamine transporter with positron emission tomograph
Stehouwer, Jeffrey S.,Daniel, Lauryn M.,Chen, Ping,Voll, Ronald J.,Williams, Larry,Plott, Susan J.,Votaw, John R.,Owens, Michael J.,Howell, Leonard,Goodman, Mark M.
experimental part, p. 5549 - 5557 (2010/11/17)
The N-(E)-fluorobutenyl-3β-(para-halo-phenyl)nortropanes 9?12 were synthesized as ligands of the dopamine transporter (DAT) for use as 18F-labeled positron emission tomography (PET) imaging agents. In vitro competition binding assays demonstrat
Synthesis and monoamine uptake inhibition of conformationally constrained 2β-carbomethoxy-3β-phenyl tropanes
Riss, Patrick Johannes,Hummerich, Rene,Schloss, Patrick
experimental part, p. 2688 - 2698 (2009/09/07)
A series of 2β-carbomethoxy-3β-phenyl tropanes with conformationally constrained nitrogen substituents were synthesized as potential selective dopamine transporter ligands. These novel compounds were examined for their monoamine uptake inhibition potency at the human dopamine transporter (hDAT), the human serotonin transporter (hSERT) and the human noradrenalin transporter (hNET), stably expressed in human embryonic kidney cells (HEK). A SAR-study was conducted to determine the contribution of extended, 4-fluorinated, conformationally constrained C4 chains at the tropane nitrogen to human monoamine transporter affinity and selectivity. The Royal Society of Chemistry 2009.
Synthesis, radiosynthesis and in vivo preliminary evaluation of [ 11C]LBT-999, a selective radioligand for the visualisation of the dopamine transporter with PET
Dolle, Frederic,Emond, Patrick,Mavel, Sylvie,Demphel, Stephane,Hinnen, Francoise,Mincheva, Zoia,Saba, Wadad,Valette, Heric,Chalon, Sylvie,Halldin, Christer,Helfenbein, Julie,Legaillard, Joel,Madelmont, Jean-Claude,Deloye, Jean-Bernard,Bottlaender, Michel,Guilloteau, Denis
, p. 1115 - 1125 (2007/10/03)
LBT-999 (8-((E)-4-fluoro-but-2-enyl)-3β-p-tolyl-8-aza-bicyclo[3.2.1] octane-2β-carboxylic acid methyl ester), a cocaine derivative belonging to a new generation of highly selective dopamine transporter (DAT) ligands, and its corresponding carboxylic acid
