Preclinical (Animal)

Dihexa HGF/c-Met Mechanism - PubMed

Benoist et al./PubMed/2014

Why It Matters

This paper caught my attention because it identifies a specific mechanism for a drug that actually enhances cognition in animals — and it works orally. Most nootropic research either shows weak effects or requires injection. That said, this is preclinical only. No human data exists, and the HGF/c-Met pathway plays complex roles in cancer biology, so safety is a major unknown. Not something you can or should experiment with today, but worth tracking if clinical trials ever materialize.

Key Findings

  • Dihexa binds to hepatocyte growth factor (HGF) with high affinity and amplifies its signaling through the c-Met receptor, even at subthreshold HGF concentrations
  • Both dihexa and its parent compound Nle(1)-AngIV increased dendritic spine density and synapse formation in rat hippocampal neurons — effects blocked by HGF antagonists
  • Orally administered dihexa improved spatial learning in rats on the Morris water maze task by 62% compared to controls, and this effect was eliminated when an HGF antagonist was injected into the brain
  • The compound crosses the blood-brain barrier effectively, solving a major pharmacokinetic problem that prevented earlier angiotensin IV analogs from being developed as drugs
  • The procognitive effects require functional HGF/c-Met signaling — blocking this pathway with either antagonists or RNA interference eliminated dihexa's benefits
Read the PaperPMID: 25187433