Please use this identifier to cite or link to this item:
https://ahro.austin.org.au/austinjspui/handle/1/10198
Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | O'Shea, R D | en |
dc.contributor.author | Manallack, D T | en |
dc.contributor.author | Conway, Elizabeth L | en |
dc.contributor.author | Mercer, L D | en |
dc.contributor.author | Beart, P M | en |
dc.date.accessioned | 2015-05-15T23:34:22Z | |
dc.date.available | 2015-05-15T23:34:22Z | |
dc.date.issued | 1991-05-16 | en |
dc.identifier.citation | Experimental Brain Research; 86(3): 652-62 | en |
dc.identifier.govdoc | 1684753 | en |
dc.identifier.other | PUBMED | en |
dc.identifier.uri | https://ahro.austin.org.au/austinjspui/handle/1/10198 | en |
dc.description.abstract | The possible heterogeneity of the agonist and glycine sites of the N-methyl-D-aspartate (NMDA) receptor-complex was examined using receptor binding techniques. Binding of [3H]L-glutamate [( 3H]GLU) and [3H]glycine to synaptic membranes of cerebral and cerebellar cortices, and membranes of a granule cell preparation of rat cerebellum, was characterized. [3H]Glycine always labelled a single population of sites; densities of binding sites (Bmax) in cortical, cerebellar and "granule" membranes were 3.1, 0.87 and 3.6 pmol/mg protein, respectively. Dissociation constants (Kd) in the same three preparations were 0.13, 0.31 and 1.9 microM, respectively. In competition studies, D-cycloserine, but not D-serine and 7-chlorokynurenate, showed varying potency between the membrane preparations, and analysis of variance (ANOVA) revealed a significant interaction between ligands and membrane fractions. Binding of [3H]GLU was saturable and to a single population of sites: Kd 0.5-0.9 microM and Bmax 3.2-3.6 pmol/mg protein. In all three membrane preparations the rank order of potency of NMDA agonists as inhibitors of the binding of [3H]GLU was always L-aspartate greater than L-cysteate greater than L-cysteinesulphinate greater than L-serine-O-sulphate greater than ibotenate greater than L-homocysteate. NMDA, quinolinate and competitive NMDA antagonists were only weak inhibitors of the binding of [3H]GLU and never fully inhibited specific binding. Other subtype-selective excitatory amino acids were very weak or ineffective inhibitors of binding. Binding of NMDA agonists was better described by a two site model whereby the proportion of high affinity sites did not vary significantly across the three membrane preparations.(ABSTRACT TRUNCATED AT 250 WORDS) | en |
dc.language.iso | en | en |
dc.subject.other | Animals | en |
dc.subject.other | Autoradiography | en |
dc.subject.other | Binding, Competitive.drug effects | en |
dc.subject.other | Cerebellar Cortex.anatomy & histology.metabolism | en |
dc.subject.other | Cerebral Cortex.anatomy & histology.metabolism | en |
dc.subject.other | Cycloserine.pharmacology | en |
dc.subject.other | Glutamates.metabolism.pharmacokinetics | en |
dc.subject.other | Glutamic Acid | en |
dc.subject.other | Glycine.metabolism.pharmacokinetics | en |
dc.subject.other | In Vitro Techniques | en |
dc.subject.other | Kynurenic Acid.analogs & derivatives.pharmacology | en |
dc.subject.other | Ligands | en |
dc.subject.other | Male | en |
dc.subject.other | Rats | en |
dc.subject.other | Rats, Inbred Strains | en |
dc.subject.other | Receptors, Amino Acid | en |
dc.subject.other | Receptors, Cell Surface.metabolism | en |
dc.subject.other | Receptors, N-Methyl-D-Aspartate.antagonists & inhibitors.metabolism | en |
dc.subject.other | Serine.metabolism | en |
dc.title | Evidence for heterogenous glycine domains but conserved multiple states of the excitatory amino acid recognition site of the NMDA receptor: regional binding studies with [3H]glycine and [3H]L-glutamate. | en |
dc.type | Journal Article | en |
dc.identifier.journaltitle | Experimental Brain Research | en |
dc.identifier.affiliation | University of Melbourne, Clinical Pharmacology and Therapeutics, Austin Hospital, Heidelberg, Victoria, Australia | en |
dc.description.pages | 652-62 | en |
dc.relation.url | https://pubmed.ncbi.nlm.nih.gov/1684753 | en |
dc.type.austin | Journal Article | en |
item.openairetype | Journal Article | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.grantfulltext | none | - |
item.fulltext | No Fulltext | - |
item.cerifentitytype | Publications | - |
item.languageiso639-1 | en | - |
Appears in Collections: | Journal articles |
Items in AHRO are protected by copyright, with all rights reserved, unless otherwise indicated.