Synthesis of Potent and Selective Serotonin 5-HT1B Receptor Ligands

Bioorg Med Chem Lett. 2005 Nov 1;15(21):4786-9. doi: 10.1016/j.bmcl.2005.07.024.


A series of serotonin 5-HT1B ligands were synthesized and evaluated for their potency and selectivity against other 5-HT receptor subtypes. Many of these new compounds displayed high affinity and selectivity for the 5-HT1B receptor and compound 6c was found to have the in vitro binding profile necessary for development as a PET radioligand.

Publication types

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

MeSH terms

  • Amides
  • Humans
  • Ligands
  • Piperazines
  • Protein Binding
  • Radioligand Assay
  • Receptor, Serotonin, 5-HT1B / chemistry
  • Receptor, Serotonin, 5-HT1B / metabolism*
  • Serotonin Agents / chemical synthesis*
  • Serotonin Agents / chemistry
  • Structure-Activity Relationship


  • Amides
  • Ligands
  • Piperazines
  • Receptor, Serotonin, 5-HT1B
  • Serotonin Agents
  • phenylpiperazine