89965-52-6Relevant articles and documents
Modulating the Serotonin Receptor Spectrum of Pulicatin Natural Products
Lin, Zhenjian,Smith, Misty D.,Concepcion, Gisela P.,Haygood, Margo G.,Olivera, Baldomero M.,Light, Alan,Schmidt, Eric W.
, p. 2360 - 2370 (2017/09/01)
Serotonin (5-HT) receptors are important in health and disease, but the existence of 14 subtypes necessitates selective ligands. Previously, the pulicatins were identified as ligands that specifically bound to the subtype 5-HT2B in the 500 nM to 10 μM range and that exhibited in vitro effects on cultured mouse neurons. Here, we examined the structure-activity relationship of 30 synthetic and natural pulicatin derivatives using binding, receptor functionality, and in vivo assays. The results reveal the 2-arylthiazoline scaffold as a tunable serotonin receptor-targeting pharmacophore. Tests in mice show potential antiseizure and antinociceptive activities at high doses without motor impairment.
