Title of article
Synthesis and monoamine transporter affinity of new 2β-carbomethoxy-3β-[4-(substituted thiophenyl)]phenyltropanes: discovery of a selective SERT antagonist with picomolar potency
Author/Authors
Gilles Tamagnan، نويسنده , , David Alagille، نويسنده , , Xing Fu، نويسنده , , Nora S. Kula، نويسنده , , Ross J. Baldessarini، نويسنده , , Robert B. Innis، نويسنده , , Ronald M. Baldwin، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
3
From page
1131
To page
1133
Abstract
Preparation of cocaine analogues has been aimed largely at development of stable compounds with high affinity and selectivity for the dopamine transporter (DAT). We now report the synthesis and monoamine transporter affinity of 10 new 2β-carbomethoxy-3β-[4-(substituted thiophenyl)]phenyltropanes. Among these, compound 4b exhibited very high affinity for the serotonin transporter (SERT: Ki = 17 pM) and good selectivity over dopamine (DAT: 710-fold) and norepinephrine transporters (NET: 11,100-fold).
Keywords
serotonin transporter , tropane , Affinity
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795350
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