A novel TSPO ligand for preventing progression of brain damage resulting from traumatic brain injury

Researcher:

Categories:

Pharmaceuticals and Biotechnology

The Technology

The present invention relates to heterocyclic compounds based on a quinazoline scaffold, which bind effectively to the mitochondrial translocator protein (TSPO) and counteract cell death processes. These novel TSPO ligands can be used for treating or preventing neurodegeneration including microglial activation, astroglial cell death, and neuro differentiation, potentially aiding in regeneration of diseased brain tissue in animal’s model for TBI and Stroke. 2-chlorophenyl quinazolin-4-yl dimethylcarbamate (2-Cl-MGV-1) is the patent-protected lead compound.

In animal models, 2-Cl-MGV-1 stops cell death of glia and neurons, attenuates microglial activation, maintains tissue integrity, and restores normal behavior and counteracts motor and cognitive disabilities.

Advantages

  • Pre-clinical evidence
  • Mechanism-driven

Applications and Opportunities

  • Treatment of neurodegeneration
  • Treatment of traumatic brain injury
  • Pharmacotherapy of neuro-inflammatory diseases
  • Treatment of ischemic stroke
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Dr. Gal Gur
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