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3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT2B, 5-HT7, or ?1 Receptor Ligands.

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 ?1 receptors were identified, each with low nanomolar binding affinities. The ?1 receptor affinity was supported in a cellular assay that provided evidence for increased cell survival under oxidative stress.

SUBMITTER: Porter MR

PROVIDER: S-EPMC6792158 | biostudies-literature | 2019 Oct

REPOSITORIES: biostudies-literature

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3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT2B, 5-HT7, or σ1 Receptor Ligands.

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-HT2B, 5-HT7, and σ1 receptors were identified, each with low nanomolar binding affinities. The σ1 recept ...[more]

PMID: 31620230

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