Title of article
Synthesis and monoamine transporter affinity of new 2β-carbomethoxy-3β-[aryl or heteroaryl]phenyltropanes
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 2006
Pages
4
From page
217
To page
220
Abstract
A series of 16 new 2β-carbomethoxy-3β-[aryl or heteroaryl]phenyltropane derivatives was synthesized and evaluated for binding to monoamine transporters. Most of the compounds exhibited nanomolar affinity for the serotonin transporter (SERT). Four compounds (29, 14, 11, and 10) presented a particularly attractive pharmacological profile, with very high SERT affinity (Ki 0.15–0.5 nM) and selectivity versus the dopamine transporter of 25- to 77-fold.
Keywords
Transporter , Norepinephrine , tropane , Dopamine , Serotonin
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796348
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