RespireRx Pharmaceuticals (OTC:RSPI) Inc has announced the publication of four articles describing the pharmacological activity of novel structural analogs of KRM-II-81, the company’s lead anti-GABAkine.
Like RespireRx’s KRM-II-81, the analogs enhance GABAergic neurotransmission and function as orally bioavailable anti-seizure agents in the absence of the sedation typically associated with GABA augmentation.
KRM-II-81 has been shown to be effective across a broad array of anti-seizure models including those predicting efficacy in patients who are pharmaco-resistant and in brain tissue from epilepsy patients who are no longer treatable with drugs, the company said. KRM-II-81 is also active in relieving acute, chronic, and neuropathic pain in several models without developing tolerance or producing sedation.
“We are very excited about developing KRM-II-81 and expanding the IND enabling studies so as to begin human studies,” chief scientific officer Arnold Lippa said in a statement. “Pending clinical validation, we believe that KRM-II-81 has the potential to represent a breakthrough treatment for pain, epilepsy, and certain neuropsychiatric disorders.”
The articles document the preclinical effects and tolerability of structural analogs of KRM-II-81. The first, MP-III-024, was found to be an effective anti-tremor compound in established rat models predicting efficacy in essential tremors and tremors associated with Parkinson’s Disease.
The publications also describe three other novel structural analogs that show sufficient blood and brain levels after oral administration to produce a pharmacological response and a deuterated derivative of KRM-II-81 that produced long-lived anticonvulsant activity after being taken orally, the company said.
“The viability of the imidazodiazepine structural platform to generate drug-like molecules with broad predicted therapeutic efficacy and good tolerability has enabled the creation of compounds that can serve as backups for KRM-II-81 as it proceeds in development,” said RespireRX research fellow and University of Wisconsin-Milwaukee professor James Cook.
More information on the articles can be found here.
RespireRx Pharmaceuticals (OTC:RSPI) is a biopharmaceutical company developing innovative and revolutionary treatments for disorders caused by the disruption of neuronal signaling, including obstructive sleep apnea, attention deficit hyperactivity disorder, epilepsy, chronic pain, and spinal cord injury.
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