Abstract:
:The phenethylamine backbone is a privileged substructure found in a wide variety of G protein-coupled receptor (GPCR) ligands. This includes both endogenous neurotransmitters and active pharmaceutical agents. More than 20 structurally unique heterocyclic phenethylamine derivatives were broadly evaluated for GPCR affinity. Selective ligands for the 5-HT2B, 5-HT7, and σ1 receptors were identified, each with low nanomolar binding affinities. The σ1 receptor affinity was supported in a cellular assay that provided evidence for increased cell survival under oxidative stress.
journal_name
ACS Med Chem Lettjournal_title
ACS medicinal chemistry lettersauthors
Porter MR,Xiao H,Wang J,Smith SB,Topczewski JJdoi
10.1021/acsmedchemlett.9b00225subject
Has Abstractpub_date
2019-09-23 00:00:00pages
1436-1442issue
10issn
1948-5875journal_volume
10pub_type
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