Gabapentin 

Anticonvulsant with unknown mechanism of action; crosses the blood brain barrier; increases GABA concentrations in the brain and reduces excitatory amino acid neurotransmission, perhaps through its effects on voltage-gated calcium channels; exhibits antinociceptive, anxiolytic, neuroprotective and anti-epileptic effects.

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H₂O: 10 mg/mL

human ... ADORA1(134), CACNA2D1(781)

rat ... Cacna1a(25398)

De Sarro, G., et al., Gabapentin potentiates the antiseizure activity of certain anticonvulsants in DBA/2 mice. Eur. J. Pharmacol. 349, 179-185, (1998) abstract

Gee, N., et al., The novel anticonvulsant drug gabapentin (neurontin) binds to the α₂δ subunit of a calcium channel. J. Biol. Chem. 271, 5768, (1996) abstract

Field, M.J., et al., Gabapentin (neurontin) and S-(+)-3-isobutylgaba represent a novel class of selective antihyperalgesic agents. Br. J. Pharmacol. 121, 1513-1522, (1997) abstract

Fink, K., et al., Inhibition of neuronal Ca²⁺ influx by gabapentin and subsequent reduction of neurotransmitter release from rat neocortical slices. Br. J. Pharmacol. 130, 900, (2000) abstract

Taylor, M.T., and Bonhaus, D.W., Allosteric modulation of [³H]gabapentin binding by ruthenium red. Neuropharmacology 39, 1267-1273, (2000) abstract

Shimoyama, M., et al., Gabapentin affects glutamatergic excitatory neurotransmission in the rat dorsal horn. Pain 85, 405-414, (2000) abstract

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GU6496000