Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands--part II

Bioorg Med Chem Lett. 2009 Jan 15;19(2):428-32. doi: 10.1016/j.bmcl.2008.11.052. Epub 2008 Nov 19.

Abstract

A series of 5-(piperidinylethyloxy)quinoline 5-HT(1) receptor ligands have been studied by elaboration of the series of dual 5-HT(1)-SSRIs reported previously. These new compounds display a different in vitro pharmacological profile with potent affinity across the 5-HT(1A), 5-HT(1B) and 5-HT(1D) receptors and selectivity against the serotonin transporter. Furthermore, they have improved pharmacokinetic profiles and CNS penetration.

MeSH terms

  • Administration, Oral
  • Animals
  • Biological Availability
  • Ligands
  • Quinolines / administration & dosage
  • Quinolines / chemistry
  • Quinolines / pharmacokinetics
  • Quinolines / pharmacology*
  • Rats
  • Receptors, Serotonin, 5-HT1 / drug effects*
  • Structure-Activity Relationship

Substances

  • Ligands
  • Quinolines
  • Receptors, Serotonin, 5-HT1