Technology ID

Small Molecule MRS5474 with Anticonvulsant Activity for Treatment of Epilepsy

Lead Inventor
Jacobson, Kenneth (NIDDK)
Tosh, Dilip (NIDDK)
Research Materials
Therapeutic Areas
Development Status
  • Early-stage
  • In vitro data available
  • In vivo data available (animal)
Lead IC
Adenosine modulates many physiological processes by activating specific adenosine receptors. These adenosine receptors play a critical role in the regulation of cellular signaling and are broadly distributed throughout the body. Thus, the ability to modulate adenosine receptor-mediated signaling is an attractive therapeutic strategy for a broad range of diseases. This technology relates to a group of compounds that display high affinity and specificity for the A1 adenosine receptor subtype.

One of the compounds, MRS5474, displays anticonvulsant activity in the 6 Hz animal model of clonic seizures. In the minimal behavioral toxicity test using the rotarod, no toxicity (zero out of eight mice) was observed at all doses tested up to 30 mg/kg, the highest dose tested, which was nearly completely protective (seven out of eight animals) in the 6 Hz model. MRS 5474 also tested well in the corneal kindled mouse model to examine its effect on focal seizures.
Commercial Applications
  • Oral anticonvulsant drug.
  • Provides a means to mimic A1AR mediated signaling in vitro and in vivo.
Competitive Advantages
  • These small molecules display increased specificity for the A1 type of adenosine receptors, which may reduce unwanted side effects previously seen in A1AR agonist therapies.
  • The physical properties of these molecules are drug-like, which makes them attractive for pre-clinical development.
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