Synthesis and binding affinities of 2 beta-(3-iodoallyloxycarbonyl)-3 beta-(4-substituted-aryl)tropane analogues as ligands for the dopamine transporter studies.
Tropane analogues from cocaine, which is known to be one of the most reinforcing and addictive compounds, were designed, synthesized, and characterized for inhibition of presynaptic uptake of dopamine (DA) in brain. Eight new derivatives of 3 beta-aryl-2 beta-(3-iodoallyloxycarbonyl)tropanes were synthesized and tested for their potential abilities to displace [(3)H]2 beta-carbomethoxy-3 beta-(4-fluorophenyl)tropane (WIN 35,428) binding to the rat striatal membranes.
Chung
K H
KH
Department of Chemistry, Inha University, 253 Yonghyundong, Namgu, Inchon, 402-751, Republic of Korea.
Lim
C H
CH
Lee
D R
DR
Jin
C
C
Chi
D Y
DY
D000818:Animals; D001667:Binding, Competitive; D001671:Biochemistry / Q000379:methods; D002462:Cell Membrane / Q000378:metabolism; D003042:Cocaine / Q000031:analogs & derivatives* / Q000378:metabolism; D004298:Dopamine / Q000493:pharmacokinetics; D050483:Dopamine Plasma Membrane Transport Proteins; D020128:Inhibitory Concentration 50; D008024:Ligands; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins / Q000032:analysis / Q000378:metabolism*; D009419:Nerve Tissue Proteins; D051381:Rats; D013329:Structure-Activity Relationship; D014326:Tropanes / Q000737:chemistry
D050483:Dopamine Plasma Membrane Transport Proteins; D008024:Ligands; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D014326:Tropanes; C021279:(1R-(exo,exo))-3-(4-fluorophenyl)-8-methyl-8- azabicyclo(3.2.1)octane-2-carboxylic acid, methyl ester; D003042:Cocaine; D004298:Dopamine