Synthesis of potent and selective serotonin 5-HT1B receptor ligands

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 neces...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2005-11, Vol.15 (21), p.4786-4789
Main Authors: YIYUN HUANG, BAE, Sung-A, ROTH, Bryan L, LARUELLE, Marc
Format: Article
Language:English
Subjects:
Amides
Biological and medical sciences
Humans
Ligands
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Piperazines
Protein Binding
Radioligand Assay
Receptor, Serotonin, 5-HT1B - chemistry
Receptor, Serotonin, 5-HT1B - metabolism
Serotonin Agents - chemical synthesis
Serotonin Agents - chemistry
Serotoninergic system
Structure-Activity Relationship
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.07.024