Document Report Card

Basic Information

ID: ALA1141860

Journal: Bioorg Med Chem Lett

Title: Synthesis and monoamine transporter affinity of 3-aryl substituted trop-2-enes.

Authors: Krunic A, Mariappan SV, Reith ME, Dunn WJ.

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 (IC(50)=14.5nM). It is also 52-fold and 230-fold selective over human dopamine and norepinephrine transporters, respectively.

CiteXplore: 16202585

DOI: 10.1016/j.bmcl.2005.08.082