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D5-KRM-II-81
- Development stage
- Preclinical
- Lead developer
- RespireRx Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
D5-KRM-II-81 is a **deuterated small-molecule imidazodiazepine** developed as a backup analog of KRM-II-81 for anticonvulsant therapy. It acts as a **positive allosteric modulator of \u03b12/\u03b13-containing GABAA receptors**, with subtype-selective GABAergic activity intended to preserve anticonvulsant efficacy while reducing liabilities associated with less selective benzodiazepine-like agents. In preclinical mouse seizure models, oral D5-KRM-II-81 significantly protected against pentylenetetrazol-induced and 6 Hz electrically induced seizures and showed a somewhat longer duration of anticonvulsant action than KRM-II-81 without significant sensorimotor impairment. The compound appears to remain a **preclinical epilepsy program** associated with RespireRx and academic collaborators.
- Other names
- deuterated KRM-II-81deuterated analog of KRM-II-81
02
Targets
GABRA2 (Gamma-aminobutyric acid receptor subunit alpha 2)GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)
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