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|Title:||P2 purinoceptor blocker suramin antagonises NMDA receptors and protects against excitatory behaviour caused by NMDA receptor agonist (RS)-(tetrazol- 5-yl)-glycine in rats|
|Authors:||Ong, W.-Y. |
|Source:||Ong, W.-Y.,Motin, L.G.,Hansen, M.A.,Dias, L.S.,Ayrout, C.,Bennett, M.R.,Balcar, V.J. (1997-09-01). P2 purinoceptor blocker suramin antagonises NMDA receptors and protects against excitatory behaviour caused by NMDA receptor agonist (RS)-(tetrazol- 5-yl)-glycine in rats. Journal of Neuroscience Research 49 (5) : 627-638. ScholarBank@NUS Repository. https://doi.org/10.1002/(SICI)1097-4547(19970901)49:5<627|
|Abstract:||It has been reported that suramin, an anthelminthic, trypanocidal agent and an inhibitor of P2 receptors, may antagonise N-methyl-D-aspartate (NMDA) subtype of the excitatory amino acid receptors. Both NMDA receptors and P(2X) subclass of P2 receptors are ligand-gated Ca2+-selective channels and, since the increased influx of Ca2+ into neurons has been linked to neurotoxicity, simultaneous inhibition of P(2X) and NMDA receptors in vivo by suramin could represent an effective neuroprotective treatment. We have found that suramin inhibited the binding of [3H]CGP 39653 to NMDA receptor binding sites in vitro and reduced the frequency of NMDA channel openings in patch- clamp studies. Suramin (1 mM) had no effect on [3H]kainate binding in vitro. In vivo, intracerebroventricular (ICV) injections of suramin (70 nmol/brain) antagonised convulsive effects of the NMDA agonist (RS)-(tetrazol-5-yl)- glycine (TZG, LY 285265). Suramin, however, did not prevent neurotoxic lesions in the hippocampus caused by ICV administration of TZG. Increasing the dose of suramin resulted in death from severe respiratory depression.|
|Source Title:||Journal of Neuroscience Research|
|Appears in Collections:||Staff Publications|
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