Synthesis of potent and selective serotonin 5-HT1B receptor ligands

Yiyun Huang; Sung-A Bae; Bryan L Roth; Marc Laruelle

doi:10.1016/j.bmcl.2005.07.024

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.

Authors

Yiyun Huang¹, Sung-A Bae, Bryan L Roth, Marc Laruelle

Affiliation

¹ Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, NY 10032, USA. hh285@columbia.edu

PMID: 16143528
DOI: 10.1016/j.bmcl.2005.07.024

Abstract

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

Substances

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