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Azulenyl Nitrone Information Summary

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A number of compounds were identified as candidates for further study by the Committee to Identify Neuroprotective Agents in Parkinson's (CINAPS). Of these compounds, Minocycline, Creatine , CoQ10 and GPI 1485 have been selected for testing in the Neuroprotection Clinical Trial.

AZULENYL NITRONE

Azulenyl Nitrone is a free radical scavenger that forms more stable compounds with combination of free radicals. It maybe more potent and more readily cross the blood brain barrier (BBB) than Nitrones, however there are no known studies assessing pharmacokinetics, safety/tolerability, or potential drug interactions in humans to date.

Scientific Rationale

  • Free radical scavengers
  • Combine with free radicals to form more stable compounds
  • May be more potent and more readily cross the blood brain barrier (BBB) than the previously studied nitrones

Kliveny, Exp Neurol 1998; 152:163-166

Animal Model Data

RODENT:Mice were given MPTP 15 mg/kg IP q2h x 5 doses. Azulenyl spin traps were administered 1 hour before, with every MPTP dose, then 6, 12 and 24 h after the last dose of MPTP. Animals were sacrificed at 7 days. Treated animals were protected against the depletion of DA and HVA at the highest doses studied. In another series of animals, it was shown that the neuroprotection WAS NOT due to changes in the concentration of MPP+.

Pharmacokinetics (including BBB penetration)


Unknown, but reference above suggests that it penetrates, at least at high doses.

Safety/Tolerability in Humans


Unknown

Drug Interaction Potential


Unknown

Clinical Trial/Epidemiological Evidence in Human PD


NONE

Last updated February 09, 2005