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Characterization df a $[^{3}$H]Glycine Recognition Site as a Modulatory Site of the N-Methyl-D-Aspartate Receptor Complex
| Content Provider | Scilit |
|---|---|
| Author | Monihan, Joseph B. Corpus, Valerie M. Hood, William F. Thomas, John W. Compton, Robert P. |
| Copyright Year | 1989 |
| Description | Journal: Journal of Neurochemistry A $[^{3}$H]glycine recognition site in rat brain synaptic plasma membranes (SPM) has been identified, having characteristics expected of a modulatory component of the N-methyl-D-aspartate receptor complex. Inculpation of SPM with $[^{3}$H]glycine for 10 min at 2°C results in saturable, reversible binding with a $K_{D}$ of 0.234 μMand a $B_{max}$ of 9.18 pmol/mg. A pharmacological analysis of this binding site indicates that D-serine $(K_{i}$= 0.27 μM), D-alanine $(K_{i}$= 1.02 μM), and D-cycloserine $(K_{i}$= 2.33 /μM) are patent inhibitors of binding, whereas the corresponding L isomers have significantly less activity $(K_{i}$= 25.4 μM, 15.9 μM, and > 100 μM, respectively). Inactive at concentrations of up to 100 μM were strychnine, L-valine, N,N=-dimethylglycine, ami-nomethylphosphonate, and aminomethylsulfonate. The active compounds were analyzed further for their ability to stimulate $[^{3}$H] l-[l-(2-thienyl)cyclohexyl]piperidine $([^{3}$H]TCP) binding to Triton X-100-washed SPM. Results indicate that the affinity of the compounds for the $[^{3}$H]glycine recognition site correlates with the ability of these analogues to stimulate $(^{3}$H]TCP binding. |
| Related Links | https://onlinelibrary.wiley.com/doi/pdf/10.1111/j.1471-4159.1989.tb07344.x |
| Ending Page | 375 |
| Page Count | 6 |
| Starting Page | 370 |
| e-ISSN | 14714159 |
| DOI | 10.1111/j.1471-4159.1989.tb07344.x |
| Journal | Journal of Neurochemistry |
| Issue Number | 2 |
| Volume Number | 53 |
| Language | English |
| Publisher | Wiley-Blackwell |
| Publisher Date | 1989-08-01 |
| Access Restriction | Open |
| Subject Keyword | Journal: Journal of Neurochemistry Medicinal Chemistry Glycine Receptor [3h]giycine Binding F3h] 1 -[1-(2-thienyl)cyclohexyl]-piperidine Binding N-methyl-d-aspartate Receptor Modulation Functional Correlation Excitatory Amino Acids |
| Content Type | Text |
| Resource Type | Article |
