Please use this identifier to cite or link to this item:
https://hdl.handle.net/2440/3935
Citations | ||
Scopus | Web of ScienceĀ® | Altmetric |
---|---|---|
?
|
?
|
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 1879-0712 |
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 |
DOI: | 10.1016/j.ejphar.2004.05.029 |
Published version: | http://dx.doi.org/10.1016/j.ejphar.2004.05.029 |
Appears in Collections: | Aurora harvest 2 Dentistry publications |
Files in This Item:
There are no files associated with this item.
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.