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Wednesday, May 15, 2024 11:31:52 AM
Yes, there is ongoing research involving KRM-II-81 in Australia.
RespireRx Pharmaceuticals Inc. has reported that as part of an ongoing collaboration, translational studies have demonstrated the ability of KRM-II-81 to dramatically reduce epileptiform electrical activity when administered in situ.
This suggests active preclinical research efforts are being conducted to further understand and develop KRM-II-81’s therapeutic potential.
For more detailed information on the specific nature of these studies or any collaborative efforts in Australia, it would be best to refer to the latest publications or announcements from RespireRx Pharmaceuticals Inc. or their research partners.
KRM-II-81 is a novel compound that acts as a positive allosteric modulator of the GABAA receptor.
It is particularly selective for the alpha2 and alpha3 subunits of this receptor.
The mechanism of action for KRM-II-81 involves enhancing the inhibitory effects of the neurotransmitter GABA (gamma-aminobutyric acid) at the GABAA receptors.
This modulation results in anxiolytic, antidepressant, and anticonvulsant effects.
Notably, KRM-II-81 has been shown to have fewer adverse effects compared to some other GABAA positive allosteric modulators (PAMs). It is associated with low to no sedation and does not lead to tolerance development, which are significant advantages over other similar compounds.
Additionally, KRM-II-81 has demonstrated effectiveness in treating seizures better than diazepam, a commonly used anticonvulsant, and has shown promise in pharmaco-resistant models of epilepsy. This makes it a potentially valuable addition to the treatment options for conditions that involve neuronal hyperexcitability, such as certain types of epilepsy.
As of the latest available information, KRM-II-81 has advanced to the next level of evaluation within the NIH HEAL Initiative®Preclinical Screening Platform for Pain (PSPP) program.
This program evaluates non-opioid assets in a battery of established preclinical pain models. The emerging data showed that KRM-II-81 blocked pain-like behaviors in rats with minimal or no detectable side effects.
While KRM-II-81 has shown promise in preclinical studies, including effectiveness in relieving acute, chronic, and neuropathic pain without tolerance development or sedation, it appears that it has not yet entered human clinical trials.
The RespireRx team is expanding the IND (Investigational New Drug) enabling studies to begin human studies.
Pending clinical validation, KRM-II-81 is believed to have the potential to be a breakthrough medication for pain, epilepsy, and other neuropsychiatric disorders.
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