Synthesis and monoamine transporter affinity of 2beta-carbomethoxy-3beta-(2''-, 3''- or 4''-substituted) biphenyltropanes.
A series of 11 novel 3beta-substituted biphenyltropanes was synthesized and evaluated by selective radioligand binding assays for affinity to monoamine transporters. Both 5-HTT potency and selectivity for 5-HTT over DAT was greatest with electron withdrawing group at the 3''-position.
Tamagnan
G
G
Yale University, School of Medicine, VA Connecticut HCS, West Haven, CT 06516, USA. gilles.tamagnan@yale.edu
Baldwin
R M
RM
Kula
N S
NS
Baldessarini
R J
RJ
Innis
R B
RB
D000818:Animals; D002352:Carrier Proteins / Q000378:metabolism*; D003042:Cocaine / Q000737:chemistry; D004298:Dopamine; D050483:Dopamine Plasma Membrane Transport Proteins; D008562:Membrane Glycoproteins / Q000378:metabolism*; D026901:Membrane Transport Proteins; D015394:Molecular Structure; D009419:Nerve Tissue Proteins; D009638:Norepinephrine; D050484:Norepinephrine Plasma Membrane Transport Proteins; D016548:Prosencephalon / Q000187:drug effects / Q000378:metabolism; D011869:Radioligand Assay; D051381:Rats; D012701:Serotonin; D050486:Serotonin Plasma Membrane Transport Proteins; D027981:Symporters; D014326:Tropanes / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism*
D002352:Carrier Proteins; D050483:Dopamine Plasma Membrane Transport Proteins; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D050484:Norepinephrine Plasma Membrane Transport Proteins; D050486:Serotonin Plasma Membrane Transport Proteins; C493226:Slc6a2 protein, rat; C493216:Slc6a3 protein, rat; C493232:Slc6a4 protein, rat; D027981:Symporters; D014326:Tropanes; D012701:Serotonin; D003042:Cocaine; D004298:Dopamine; D009638:Norepinephrine