Synthesis and binding affinities of 2β-(3-iodoallyloxycarbonyl)3β-(4-substituted-aryl)tropane analogues as ligands for the dopamine transporter studies
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作者:
Chung, KH
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机构:Inha Univ, Dept Chem, Nam Gu, Inchon 402751, South Korea
Chung, KH
Lim, CH
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机构:Inha Univ, Dept Chem, Nam Gu, Inchon 402751, South Korea
Lim, CH
Lee, DR
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机构:Inha Univ, Dept Chem, Nam Gu, Inchon 402751, South Korea
Lee, DR
Jin, CB
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机构:Inha Univ, Dept Chem, Nam Gu, Inchon 402751, South Korea
Jin, CB
Chi, DY
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机构:Inha Univ, Dept Chem, Nam Gu, Inchon 402751, South Korea
Chi, DY
机构:
[1] Inha Univ, Dept Chem, Nam Gu, Inchon 402751, South Korea
[2] Future Chem Co, Nam Gu, Inchon 402751, South Korea
[3] Korea Inst Sci & Technol, Bioanalysis & Biotransformat Res Ctr, Seoul 130650, South Korea
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 [H-3]2 beta -carbomethoxy-3 beta-(4-fluorophenyl)tropane (WIN 35,428) binding to the rat striatal membranes. (C) 2001 Elsevier Science Ltd. All rights reserved.