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https://hdl.handle.net/2440/3935
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dc.contributor.author | Parker, D. | - |
dc.contributor.author | Ong, J. | - |
dc.contributor.author | Marino, V. | - |
dc.contributor.author | Kerr, D. | - |
dc.date.issued | 2004 | - |
dc.identifier.citation | European Journal of Pharmacology, 2004; 495(2-3):137-143 | - |
dc.identifier.issn | 0014-2999 | - |
dc.identifier.issn | 1879-0712 | - |
dc.identifier.uri | http://hdl.handle.net/2440/3935 | - |
dc.description.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. | - |
dc.language.iso | en | - |
dc.publisher | Elsevier Science BV | - |
dc.source.uri | http://dx.doi.org/10.1016/j.ejphar.2004.05.029 | - |
dc.subject | Neocortex | - |
dc.subject | Animals | - |
dc.subject | Rats | - |
dc.subject | Rats, Sprague-Dawley | - |
dc.subject | Tritium | - |
dc.subject | Amines | - |
dc.subject | gamma-Aminobutyric Acid | - |
dc.subject | Baclofen | - |
dc.subject | Cyclohexanecarboxylic Acids | - |
dc.subject | Organophosphorus Compounds | - |
dc.subject | Morpholines | - |
dc.subject | Glutamic Acid | - |
dc.subject | Receptors, GABA-B | - |
dc.subject | Receptors, Presynaptic | - |
dc.subject | Excitatory Amino Acid Antagonists | - |
dc.subject | GABA Agonists | - |
dc.subject | Dose-Response Relationship, Drug | - |
dc.subject | Male | - |
dc.subject | In Vitro Techniques | - |
dc.subject | Gabapentin | - |
dc.title | Gabapentin activates presynaptic GABAB heteroreceptors in rat cortical slices | - |
dc.type | Journal article | - |
dc.identifier.doi | 10.1016/j.ejphar.2004.05.029 | - |
pubs.publication-status | Published | - |
dc.identifier.orcid | Ong, J. [0000-0002-0958-460X] | - |
Appears in Collections: | Aurora harvest 2 Dentistry publications |
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