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 …

Chemical modulation of Kv7 potassium channels

M Borgini, P Mondal, R Liu, P Wipf - RSC medicinal chemistry, 2021 - pubs.rsc.org
The rising interest in Kv7 modulators originates from their ability to evoke fundamental
electrophysiological perturbations in a tissue-specific manner. A large number of therapeutic …

Structural basis for the modulation of human KCNQ4 by small-molecule drugs

T Li, K Wu, Z Yue, Y Wang, F Zhang, H Shen - Molecular Cell, 2021 - cell.com
Among the five KCNQ channels, also known as the K v 7 voltage-gated potassium (K v)
channels, KCNQ2–KCNQ5 control neuronal excitability. Dysfunctions of KCNQ2–KCNQ5 …

Discovery of HN37 as a potent and chemically stable antiepileptic drug candidate

YM Zhang, HY Xu, HN Hu, FY Tian… - Journal of Medicinal …, 2021 - ACS Publications
We previously reported that P-retigabine (P-RTG), a retigabine (RTG) analogue bearing a
propargyl group at the nitrogen atom in the linker of RTG, displayed moderate …

Pharmacological activation of neuronal voltage-gated Kv7/KCNQ/M-channels for potential therapy of epilepsy and pain

Y Liu, X Bian, KW Wang - Pharmacology of Potassium Channels, 2021 - Springer
Native M-current is a low-threshold, slowly activating potassium current that exerts an
inhibitory control over neuronal excitability. The M-channel is primarily co-assembled by …

Potassium and calcium channels in different nerve cells act as therapeutic targets in neurological disorders

Q Qiu, M Yang, D Gong, H Liang… - Neural Regeneration …, 2025 - journals.lww.com
The central nervous system, information integration center of the body, is mainly composed
of neurons and glial cells. The neuron is one of the most basic and important structural and …

Modifications of the triaminoaryl metabophore of flupirtine and retigabine aimed at avoiding quinone diimine formation

KW Wurm, FM Bartz, L Schulig, A Bodtke… - ACS …, 2022 - ACS Publications
The potassium channel opening drugs flupirtine and retigabine have been withdrawn from
the market due to occasional drug-induced liver injury (DILI) and tissue discoloration …

Synthesis and pharmacological characterization of conformationally restricted retigabine analogues as novel neuronal Kv7 channel activators

C Ostacolo, F Miceli, V Di Sarno, P Nappi… - Journal of medicinal …, 2019 - ACS Publications
Kv7 K+ channels represent attractive pharmacological targets for the treatment of different
neurological disorders, including epilepsy. In this paper, 42 conformationally restricted …

TET1 participates in complete Freund's adjuvant-induced trigeminal inflammatory pain by regulating Kv7. 2 in a mouse model

D Zhan, J Zhang, S Su, X Ren, S Zhao, W Zang… - Neuroscience …, 2024 - Springer
Trigeminal inflammatory pain is one of the most severe pain-related disorders in humans;
however, the underlying mechanisms remain largely unknown. In this study, we investigated …

Carba analogues of flupirtine and retigabine with improved oxidation resistance and reduced risk of quinoid metabolite formation

KW Wurm, FM Bartz, L Schulig, A Bodtke… - …, 2022 - Wiley Online Library
The KV7 potassium channel openers flupirtine and retigabine have been valuable options in
the therapy of pain and epilepsy. However, as a result of adverse reactions, both drugs are …