Ontology highlight
ABSTRACT:
SUBMITTER: Gabr MT
PROVIDER: S-EPMC6072314 | biostudies-literature | 2018 Jun
REPOSITORIES: biostudies-literature
MedChemComm 20180521 6
We designed and synthesized a new biphenyl amide-tryptamine hybrid molecule <b>7</b> utilizing a pharmacophore-based approach as a 5-HT<sub>2B</sub> antagonist. The hybrid compound <b>7</b> was evaluated for its affinity to a panel of seven 5-HT receptors, demonstrating high selectivity for the 5-HT<sub>2B</sub> receptor. Functional assays revealed potent antagonism of 5-HT<sub>2B</sub> by <b>7</b> with an IC<sub>50</sub> value of 14.1 nM. Moreover, compound <b>7</b> possessed a desirable <i>in ...[more]