Exploring the overlapping binding sites of ifenprodil and EVT-101 in GluN2B-containing NMDA receptors using novel chicken embryo forebrain cultures and molecular modeling.

ABSTRACT: N-methyl-d-aspartate receptors (NMDAR) are widely expressed in the brain. GluN2B subunit-containing NMDARs has recently attracted significant attention as potential pharmacological targets, with emphasis on the functional properties of allosteric antagonists. We used primary cultures from chicken embryo forebrain (E10), expressing native GluN2B-containing NMDA receptors as a novel model system. Comparing the inhibition of calcium influx by well-known GluN2B subunit-specific allosteric antagonists, the following rank order of potency was found: EVT-101 (EC ₅₀ 22 ± 8 nmol/L) > Ro 25-6981 (EC ₅₀ 60 ± 30 nmol/L) > ifenprodil (EC ₅₀ 100 ± 40 nmol/L) > eliprodil (EC ₅₀ 1300 ± 700 nmol/L), similar to previous observations in rat cortical cultures and ce

SUBMITTER: Fjelldal MF 

PROVIDER: S-EPMC6543015 | biostudies-literature | 2019 Jun

REPOSITORIES: biostudies-literature