Synthesis and evaluation of a series of tropane analogues as novel vesicular monoamine transporter-2 ligands

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4463-6. doi: 10.1016/j.bmcl.2005.07.032.

Abstract

A series of tropane derivatives has been synthesized as lobelane analogues and evaluated for their binding affinity at the vesicular monoamine transporter-2 (VMAT2), and at alpha4beta2* and alpha7* nicotinic acetylcholine receptors. The trop-2-ene analogues 4a and 4b exhibited good affinity and high selectivity for VMAT2.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Ligands
  • Protein Binding
  • Rats
  • Receptors, Nicotinic / metabolism
  • Structure-Activity Relationship
  • Tropanes / chemical synthesis*
  • Tropanes / metabolism
  • Tropanes / pharmacology*

Substances

  • Ligands
  • Receptors, Nicotinic
  • Tropanes