Ontology highlight
ABSTRACT:
SUBMITTER: Zeng F
PROVIDER: S-EPMC5846131 | biostudies-literature | 2018 Mar
REPOSITORIES: biostudies-literature
Zeng Fanxing F Nye Jonathon A JA Voll Ronald J RJ Howell Leonard L Goodman Mark M MM
ACS medicinal chemistry letters 20180205 3
Nine pyridyloxypyridyl indole carboxamides were synthesized and displayed high affinities for 5-HT<sub>2C</sub> receptors and high selectivity over 5-HT<sub>2A</sub> and 5-HT<sub>2B</sub>. Among them, 6-methyl-<i>N</i>-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]1<i>H</i>-indole-3-carboxamide (<b>8</b>) exhibits the highest 5-HT<sub>2C</sub> binding affinity (<i>K</i><sub>i</sub> = 1.3 nM) and high selectivity over 5-HT<sub>2A</sub> (∼1000 times) and 5-HT<sub>2B</sub> (∼140 times). [<sup>11</sup> ...[more]