Ontology highlight
ABSTRACT:
SUBMITTER: Porter MR
PROVIDER: S-EPMC6792158 | biostudies-literature | 2019 Oct
REPOSITORIES: biostudies-literature
Porter Matthew R MR Xiao Haiyan H Wang Jing J Smith Sylvia B SB Topczewski Joseph J JJ
ACS medicinal chemistry letters 20190923 10
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-HT<sub>2B</sub>, 5-HT<sub>7</sub>, and σ<sub>1</sub> receptors were identified, each with low nanomolar binding affinities. The σ<sub>1</sub> recept ...[more]