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"Specific" Binding of $[^{3}$H]Imipramine to Protease-Sensitive and Protease-Resistant Sites
| Content Provider | Scilit |
|---|---|
| Author | Marcusson, J. Fowler, C. J. Hall, H. Ross, S. B. Winblad, B. |
| Copyright Year | 1985 |
| Description | Journal: Journal of Neurochemistry A number of 5-hydroxytryptamine (5-HT) uptake inhibitors have been shown to displace the binding of $[^{3}$H)imipramine to rat cortical membranes in a complex manner with Hill slopes less than unity. Norzimeldine displaced the binding of $[^{3}$H]imipramine in a biphasic manner with $IC_{50}$ values for the two components of about 30 nM and 30 μM. This latter site alone was found in tissues that had been treated with a protease. Binding to both of these sites was displaced by 10μM desipramine. The protease-sensitive $[^{3}$H]imipramine binding sites were found to be saturable, high-affinity binding sites with a $K_{D}$ of 8 nM. The number of these sites varied between brain regions and was positively correlated with the regional distribution of $[^{14}$C]5-HT but not $[^{3}$H]noradrenaline uptake. This was not the case however for the protease resistant but desipramine-displaceable binding sites. Since most previous $[^{3}$H]imipramine binding studies have been performed with high concentrations of desipramine (10 μ. M) to define “specific binding,” these data would suggest that either protease-sensitivity or displaceability by 1 μM norzimeldine would give more reliable estimates of the specific binding. |
| Related Links | https://onlinelibrary.wiley.com/doi/pdf/10.1111/j.1471-4159.1985.tb12872.x |
| Ending Page | 711 |
| Page Count | 7 |
| Starting Page | 705 |
| e-ISSN | 14714159 |
| DOI | 10.1111/j.1471-4159.1985.tb12872.x |
| Journal | Journal of Neurochemistry |
| Issue Number | 3 |
| Volume Number | 44 |
| Language | English |
| Publisher | Wiley-Blackwell |
| Publisher Date | 1985-03-01 |
| Access Restriction | Open |
| Subject Keyword | Journal: Journal of Neurochemistry [3h]imipramine Binding 5-hydroxytryptamine Uptake |
| Content Type | Text |
| Resource Type | Article |
