<scp>ENX</scp> ‐101, a <scp> GABA <sub>A</sub> </scp> receptor α2,3,5‐selective positive allosteric modulator, displays antiseizure effects in rodent seizure and epilepsy models
ENX-101 is an α2,α3,α5-selective GABA<sub>A</sub> receptor PAM that has high potency and partial efficacy. The drug is highly effective in rodent seizure and epilepsy models. ENX-101 is most potent in the GAERS model of absence epilepsy, and active in the 6 Hz model and amygdala kindled rats. These results demonstrate that a partial, subtype-selective GABA<sub>A</sub> receptor PAM has activity in translationally validated preclinical epilepsy screening models. Clinical evaluation of ENX-101 as a treatment for focal and generalized epilepsies is warranted.
Authors
- Vikram Sudarsan
- Michael A. Rogawski (ORCID: https://orcid.org/0000-0002-3296-8193)
- Melissa Barker‐Haliski (ORCID: https://orcid.org/0000-0002-8175-0553)
- Stephen Cunningham (ORCID: https://orcid.org/0000-0003-0373-6948)
- Eve M. Taylor
- William D. Brubaker (ORCID: https://orcid.org/0000-0002-4345-4411)
- Krishna C. Vadodaria (ORCID: https://orcid.org/0000-0002-3455-0209)
- Jordi Serrats
- Corinne Roucard
- Alexis Evrard
- H. Steve White (ORCID: https://orcid.org/0000-0003-4550-4408)
- Kimberly E. Vanover
Institutions
- University of Washington (US)
- Synerlab (France) (FR)
- University of California, Davis (US)
Publication Details
- Journal
- Epilepsia
- Published
- 2025-03-15
- DOI
- https://doi.org/10.1111/epi.18340
- Citations
- 1
- Primary Topic
- Neuroscience and Neuropharmacology Research
- Type
- article
- Field-Weighted Citation Impact
- 0.91