5-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7092-6. doi: 10.1016/j.bmcl.2010.09.085. Epub 2010 Sep 27.

Abstract

5-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones have been identified with different combinations of 5-HT(1) autoreceptor antagonist and hSerT potencies and excellent rat PK profiles. The availability of tool compounds with a range of profiles at targets known to play a key role in the control of synaptic 5-HT levels will allow exploration of different pharmacological profiles in a range of animal behavioral and disease models.

MeSH terms

  • Animals
  • Autoreceptors / antagonists & inhibitors
  • Autoreceptors / drug effects
  • Quinolones / chemistry*
  • Quinolones / pharmacokinetics
  • Rats
  • Receptors, Serotonin, 5-HT1 / drug effects*
  • Selective Serotonin Reuptake Inhibitors / chemistry*
  • Selective Serotonin Reuptake Inhibitors / pharmacokinetics*
  • Selective Serotonin Reuptake Inhibitors / pharmacology
  • Synapses / chemistry

Substances

  • Autoreceptors
  • Quinolones
  • Receptors, Serotonin, 5-HT1
  • Serotonin Uptake Inhibitors