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A microdialysis study on the mechanism of action of gabapentin
W Timmerman1, M Bouma, J B De Vries
1Department of Medicinal Chemistry, University Center for Pharmacy, Ant. Deusinglaan 1, 9713 AV, Groningen, The Netherlands. wia@farm.rug.nl
Abstract:
To gain insight into the mechanism of action of the anti-epileptic, gabapentin, the effects of gabapentin on the in vivo extracellular gamma-aminobutyric acid (GABA) levels in the rat substantia nigra reticulata were studied using microdialysis. In order to investigate possible interference with different GABA-ergic compartments in the substantia nigra reticulata, we studied the effects of gabapentin under basal, K(+)-, nipecotic acid- and glutamate-stimulated conditions. Intraperitoneally (i.p.) administered gabapentin, at a dose of 100 mg/kg, did not significantly affect extracellular GABA levels under any condition. Thus, our data do not support the involvement of nigral GABA release in the mechanism of action of the anti-epileptic gabapentin.