Ontology highlight
ABSTRACT:
SUBMITTER: Jahan R
PROVIDER: S-EPMC5253108 | biostudies-literature | 2017 Jan
REPOSITORIES: biostudies-literature
Jahan Rajwana R Stephen Michael Rajesh MR Forkuo Gloria S GS Kodali Revathi R Guthrie Margaret L ML Nieman Amanda N AN Yuan Nina Y NY Zahn Nicolas M NM Poe Michael M MM Li Guanguan G Yu Olivia B OB Yocum Gene T GT Emala Charles W CW Stafford Douglas C DC Cook James M JM Arnold Leggy A LA
European journal of medicinal chemistry 20161124
We describe the synthesis of analogs of XHE-III-74, a selective α4β3γ2 GABA<sub>A</sub>R ligand, shown to relax airway smooth muscle ex vivo and reduce airway hyperresponsiveness in a murine asthma model. To improve properties of this compound as an asthma therapeutic, a series of analogs with a deuterated methoxy group in place of methoxy group at C-8 position was evaluated for isotope effects in preclinical assays; including microsomal stability, cytotoxicity, and sensorimotor impairment. The ...[more]