Synthesis and Structure-Activity Relationships of Tool Compounds Based on WAY163909, a 5-HT2C Receptor Agonist

Ying Chu Chen, Rachel M. Hartley, Noelle C. Anastasio, Kathryn A. Cunningham, Scott R. Gilbertson

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

The development of probe molecules that can be used to investigate G protein-coupled receptor (GPCR) pharmacology, trafficking, and relationship with other GPCRs is an important and growing area of research. Here, we report the synthesis of analogues of the known selective serotonin (5-HT) 5-HT2C receptor (5-HT2CR) agonist WAY163909 which were designed to allow for the attachment of a second ligand, signaling or reporter molecules, as well as immobilization agents to the parent molecule with the maintenance of agonist activity. This goal was accomplished by the synthesis of novel molecules in which sites a-d were modified and resulting compounds were analyzed pharmacologically in vitro.

Original languageEnglish (US)
Pages (from-to)1004-1010
Number of pages7
JournalACS Chemical Neuroscience
Volume8
Issue number5
DOIs
StatePublished - May 17 2017

Fingerprint

Serotonin 5-HT2 Receptor Agonists
Receptor, Serotonin, 5-HT2C
Structure-Activity Relationship
Serotonin
Molecules
G-Protein-Coupled Receptors
Immobilization
Maintenance
Pharmacology
Ligands
Research
1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta(b)(1,4)diazepino(6,7,1hj)indole

Keywords

  • 5-HT receptor agonist
  • Serotonin
  • WAY163909 derivatives

ASJC Scopus subject areas

  • Physiology
  • Biochemistry
  • Cognitive Neuroscience
  • Cell Biology

Cite this

Synthesis and Structure-Activity Relationships of Tool Compounds Based on WAY163909, a 5-HT2C Receptor Agonist. / Chen, Ying Chu; Hartley, Rachel M.; Anastasio, Noelle C.; Cunningham, Kathryn A.; Gilbertson, Scott R.

In: ACS Chemical Neuroscience, Vol. 8, No. 5, 17.05.2017, p. 1004-1010.

Research output: Contribution to journalArticle

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