Gabapentin-Lactam: A Novel Neuroprotective Agent

In glaucoma and in retinal ischemia, excessive extracellular glutamate can damage retinal ganglion cells. Glutamate receptor antagonists as well as glutamate release inhibitors can alleviate this neuronal loss. In a pilot experiment we found that the antiglutamatergic drug Gabapentin was not neuroprotective in vivo whereas its derivative Gabapentin-Lactam was neuroprotective. We also could demonstrate that inhibition of glutamate release could be blocked with Glibenclamide indicating that Gabapentin-Lactam acts as an opener of ATP-sensitive potassium channels.