Synthesis and activity of functionalizable derivatives of the serotonin (5-HT) 5-HT_2A receptor (5-HT_2AR) antagonist M100907.

ABSTRACT: The approach of tethering together two known receptor ligands, to be used as molecular probes for the study of G protein-coupled receptor (GPCR) systems, has proven to be a valuable approach. Selective ligands that possess functionality that can be used to link to other ligands, are useful in the development of novel antagonists and agonists. Such molecules can also be attached to reporter molecules, such as fluorophores, for the study of GPCR dimerization and its role in signaling. The highly selective serotonin (5-HT) 5-HT_2A receptor (5-HT_2AR) antagonist M100907 (volinanserin) is of clinical interest in the treatment of neurological and mental health disorders. Here, we synthesized the most active (+)-M100907 enantiomer as well as a series of derivatives that posses

SUBMITTER: Gilbertson SR 

PROVIDER: S-EPMC6613932 | biostudies-literature | 2018 May

REPOSITORIES: biostudies-literature