Synthesis and Structure-Activity Relationships of Tool Compounds Based on WAY163909, a 5-HT 2C Receptor Agonist.

Autor: Chen YC; Department of Chemistry, University of Houston , Houston, Texas 77204, United States., Hartley RM, Anastasio NC, Cunningham KA, Gilbertson SR; Department of Chemistry, University of Houston , Houston, Texas 77204, United States.
Jazyk: angličtina
Zdroj: ACS chemical neuroscience [ACS Chem Neurosci] 2017 May 17; Vol. 8 (5), pp. 1004-1010. Date of Electronic Publication: 2017 Apr 19.
DOI: 10.1021/acschemneuro.6b00439
Abstrakt: 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 2C R) 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.
Databáze: MEDLINE