Pharmacological characterization of the α_2A-adrenergic receptor inhibiting rat hippocampal CA3 epileptiform activity: comparison of ligand efficacy and potency.

ABSTRACT: The mechanism underlying the antiepileptic actions of norepinephrine (NE) is unclear with conflicting results. Our objectives are to conclusively delineate the specific adrenergic receptor (AR) involved in attenuating hippocampal CA3 epileptiform activity and assess compounds for lead drug development. We utilized the picrotoxin model of seizure generation in rat brain slices using electrophysiological recordings. Epinephrine (EPI) reduced epileptiform burst frequency in a concentration-dependent manner. To identify the specific receptor involved in this response, the equilibrium dissociation constants were determined for a panel of ligands and compared with established binding values for α₁, α₂, and other receptor subtypes. Correlation and slope of unity were found f

SUBMITTER: Biggane JP 

PROVIDER: S-EPMC10710878 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature