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Type: Journal article
Title: Gabapentin activates presynaptic GABAB heteroreceptors in rat cortical slices
Author: Parker, D.
Ong, J.
Marino, V.
Kerr, D.
Citation: European Journal of Pharmacology, 2004; 495(2-3):137-143
Publisher: Elsevier Science BV
Issue Date: 2004
ISSN: 0014-2999
Abstract: In electrically stimulated rat neocortical brain slices preloaded with [3H]gamma-aminobutyric acid (GABA) or [3H]glutamic acid, the pharmacological actions of 1-(aminomethyl)-cyclohexaneacetic acid (gabapentin, Gp) were compared with the GABAB receptor agonists baclofen (Bac) and (3-amino-2-(S)-hydroxypropyl)-methylphosphinic acid (CGP 44532). Gabapentin, baclofen and CGP 44532 all reduced the electrically stimulated release of [3H]glutamic acid (IC50=20 microM, 0.8 microM and 2 microM, respectively). These effects were sensitive to the GABAB receptor antagonists (+)-(S)-5,5 dimethylmorpholinyl-2-acetic acid (Sch 50911) or N-3-[[1-(S)-(3,4-dichlorophenyl)ethyl]amino]-2-(S)-hydroxypropyl-P-(cyclo-hexylmethyl)-phosphinic acid (CGP 54626). By contrast, gabapentin was without effect on the release of [3H]GABA, whilst baclofen (IC50=8 microM) and CGP 44532 (IC50=1 microM) inhibited [3H]GABA release. It is concluded that gabapentin selectively activates presynaptic GABAB heteroreceptors, but not GABAB autoreceptors, and may be a useful ligand to discriminate between presynaptic GABAB receptor subtypes.
Keywords: Neocortex; Animals; Rats; Rats, Sprague-Dawley; Tritium; Amines; gamma-Aminobutyric Acid; Baclofen; Cyclohexanecarboxylic Acids; Organophosphorus Compounds; Morpholines; Glutamic Acid; Receptors, GABA-B; Receptors, Presynaptic; Excitatory Amino Acid Antagonists; GABA Agonists; Dose-Response Relationship, Drug; Male; In Vitro Techniques; Gabapentin
RMID: 0020041289
DOI: 10.1016/j.ejphar.2004.05.029
Appears in Collections:Dentistry publications

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