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

doi:10.1021/acschemneuro.6b00439

Synthesis and Structure-Activity Relationships of Tool Compounds Based on WAY163909, a 5-HT_2C Receptor Agonist

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

Research output: Contribution to journal › Article › peer-review

7 Scopus citations

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-HT_2C receptor (5-HT_2CR) 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 language	English (US)
Pages (from-to)	1004-1010
Number of pages	7
Journal	ACS chemical neuroscience
Volume	8
Issue number	5
DOIs	https://doi.org/10.1021/acschemneuro.6b00439
State	Published - May 17 2017

Keywords

5-HT receptor agonist
Serotonin
WAY163909 derivatives

ASJC Scopus subject areas

Biochemistry
Physiology
Cognitive Neuroscience
Cell Biology

Access to Document

10.1021/acschemneuro.6b00439

Cite this

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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.",

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