Title of article
Synthesis and monoamine transporter affinity of 3-aryl substituted trop-2-enes
Author/Authors
Aleksej Krunic، نويسنده , , S.V. Santhana Mariappan، نويسنده , , Marteen E.A. Reith، نويسنده , , William J. Dunn III، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
6
From page
5488
To page
5493
Abstract
A series of new 3-aryl-tropanes have been synthesized, and their affinities and selectivities were evaluated for monoamine transporters. (1RS)-3-(Fluoren-2-yl)-8-methyl-8-azabicyclo[3.2.1]oct-2-ene exhibited the highest affinity for the human serotonin transporter (IC50 = 14.5 nM). It is also 52-fold and 230-fold selective over human dopamine and norepinephrine transporters, respectively.
Keywords
Monoamine transporters , Uptake , tropane
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796214
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