Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 1

Bioorg Med Chem Lett. 2000 Jul 17;10(14):1559-62. doi: 10.1016/s0960-894x(00)00290-0.

Abstract

6-Nitroquipazine has been known as one of the most potent and selective inhibitors of serotonin transporter in vitro and in vivo. Nine derivatives of 6-nitroquipazine were synthesized and tested for their potential abilities to displace [3H]citalopram binding to the rat cortical membranes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding, Competitive
  • Carrier Proteins / metabolism*
  • Cell Membrane / metabolism
  • Cerebral Cortex / metabolism
  • Citalopram / pharmacokinetics
  • Drug Design
  • Indicators and Reagents
  • Kinetics
  • Membrane Glycoproteins / metabolism*
  • Membrane Transport Proteins*
  • Models, Structural
  • Molecular Conformation
  • Nerve Tissue Proteins*
  • Quipazine / analogs & derivatives*
  • Quipazine / chemical synthesis*
  • Quipazine / chemistry
  • Quipazine / pharmacokinetics
  • Quipazine / pharmacology
  • Rats
  • Selective Serotonin Reuptake Inhibitors / chemical synthesis
  • Selective Serotonin Reuptake Inhibitors / chemistry
  • Selective Serotonin Reuptake Inhibitors / pharmacokinetics
  • Serotonin Plasma Membrane Transport Proteins
  • Structure-Activity Relationship

Substances

  • Carrier Proteins
  • Indicators and Reagents
  • Membrane Glycoproteins
  • Membrane Transport Proteins
  • Nerve Tissue Proteins
  • Serotonin Plasma Membrane Transport Proteins
  • Serotonin Uptake Inhibitors
  • Slc6a4 protein, rat
  • Citalopram
  • Quipazine
  • 6-nitroquipazine