Mechanisms of action of currently used antiseizure drugs

GJ Sills, MA Rogawski - Neuropharmacology, 2020 - Elsevier
Antiseizure drugs (ASDs) prevent the occurrence of seizures; there is no evidence that they
have disease-modifying properties. In the more than 160 years that orally administered …

Single-target versus multi-target drugs versus combinations of drugs with multiple targets: preclinical and clinical evidence for the treatment or prevention of epilepsy

W Löscher - Frontiers in pharmacology, 2021 - frontiersin.org
Rationally designed multi-target drugs (also termed multimodal drugs, network therapeutics,
or designed multiple ligands) have emerged as an attractive drug discovery paradigm in the …

Shared structural mechanisms of general anaesthetics and benzodiazepines

JJ Kim, A Gharpure, J Teng, Y Zhuang, RJ Howard… - Nature, 2020 - nature.com
Most general anaesthetics and classical benzodiazepine drugs act through positive
modulation of γ-aminobutyric acid type A (GABAA) receptors to dampen neuronal activity in …

Direct structural insights into GABAA receptor pharmacology

JJ Kim, RE Hibbs - Trends in biochemical sciences, 2021 - cell.com
GABA A receptors are pentameric ligand-gated ion channels that mediate most fast
neuronal inhibition in the brain. In addition to their important physiological roles, they are …

The ups and downs of alkyl‐carbamates in epilepsy therapy: how does cenobamate differ?

W Löscher, GJ Sills, HS White - Epilepsia, 2021 - Wiley Online Library
Since 1955, several alkyl‐carbamates have been developed for the treatment of anxiety and
epilepsy, including meprobamate, flupirtine, felbamate, retigabine, carisbamate, and …

GABAA receptors as targets for anaesthetics and analgesics and promising candidates to help treat coronavirus infections: A mini‐review

Y Luo, T Balle - Basic & Clinical Pharmacology & Toxicology, 2022 - Wiley Online Library
GABA is a major inhibitory neurotransmitter that regulates the balance between excitatory
and inhibitory circuits in the human nervous system. The GABA receptors are divided into …

Site-specific effects of neurosteroids on GABAA receptor activation and desensitization

Y Sugasawa, WWL Cheng, JR Bracamontes, ZW Chen… - Elife, 2020 - elifesciences.org
This study examines how site-specific binding to three identified neurosteroid-binding sites
in the α1β3 GABAA receptor (GABAAR) contributes to neurosteroid allosteric modulation …

Druggable lipid binding sites in pentameric ligand-gated ion channels and transient receptor potential channels

WWL Cheng, MJ Arcario, JT Petroff - Frontiers in Physiology, 2022 - frontiersin.org
Lipids modulate the function of many ion channels, possibly through direct lipid-protein
interactions. The recent outpouring of ion channel structures by cryo-EM has revealed many …

Remimazolam tolerance in long-term benzodiazepine users: a case report of 2 cases

H Yoshikawa, M Hosokawa, Y Kashima, S Oki… - A&A …, 2021 - journals.lww.com
A 60-year-old woman with a 5-year history of anxiolytic use, a diazepam-equivalent daily
dose of 15 mg, was scheduled for esophageal stent removal. She was given remimazolam …

An Update on Stiripentol Mechanisms of Action: A Narrative Review

A Bacq, A Depaulis, V Castagné, ME Le Guern… - Advances in …, 2024 - Springer
Abstract Stiripentol (Diacomit®)(STP) is an orally active antiseizure medication (ASM)
indicated as adjunctive therapy, for the treatment of seizures associated with Dravet …