D5-KRM-II-81 / RespireRx - LARVOL DELTA

Comparative anticonvulsant activity of the GABAkine KRM-II-81 and a deuterated analog. (PubMed, Drug Dev Res) - "Oral administration of 100 mg/kg of either KRM-II-81 or D5-KRM-II-81 was significantly less disruptive of sensorimotor function in mice than diazepam (5 mg/kg, p.o.). The present report documents that D5-KRM-II-81 represents another in this series of imidazodiazepines with anticonvulsant activity at doses that do not impair sensorimotor function."

Journal • CNS Disorders • Epilepsy

RespireRx Pharmaceuticals Inc. Enters a Collaboration With National Institute for Neurological Disorders and Stroke to Advance its Lead GABAkine Toward Clinical Development (GlobeNewswire) - "RespireRx Pharmaceuticals Inc...is pleased to announce that RespireRx has been accepted into the NIH HEAL Initiative® NINDS Preclinical Screening Platform for Pain (PSPP) program. The Company’s lead GABAkine, KRM-II-81, has been shown to be effective in relieving acute, chronic, and neuropathic pain in a number of models without tolerance development or sedation."

Licensing / partnership • CNS Disorders • Neuralgia • Pain

Synthesis, metabolism, pharmacokinetics, and anticonvulsant activity of a deuterated analog of the α2/3-selective GABAkine KRM-II-81 | Poster Board #3375 (ACS-Fall 2022) - "D5-KRM-II-81, like KRM-II-81, significantly prevented seizures induced by pentylenetetrazol when given orally despite its lack of augmented exposure. These findings of this new orally active anticonvulsant GABAkine, D5-KRM-II-81 will be presented."

PK/PD data • Anesthesia • CNS Disorders • Epilepsy • Neuralgia • Pain • Vascular Neurology

RespireRx Pharmaceuticals Inc. Announces Discovery of a New GABAkine Neuromodulator that Protects Against Seizures and Lethality (GlobeNewswire) - "RespireRx Pharmaceuticals Inc...is pleased to announce that scientists associated with the Company have published a manuscript detailing the pharmacology of its newest asset, D5-KRM-II-81....Doses of D5-KRM-II-81 as low as 2 mg/kg provided enduring exposure of plasma and brain of rats after oral administration. Importantly, like KRM-II-81, D5-KRM-II-81 completely prevented clonic seizures, tonic seizures, and lethality induced by the GABA receptor antagonist chemoconvulsant pentylenetetrazol."

Preclinical • CNS Disorders • Epilepsy