High affinity binding of3H-paroxetine and3H-imipramine to rat neuronal membranes
- Erling T. MellerupAffiliated withPsychochemistry Institute, University of Copenhagen
- , Per PlengeAffiliated withPsychochemistry Institute, University of Copenhagen
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Paroxetine is the most potent and one of the most specific serotonin uptake inhibitors. High-affinity3H-paroxetine and3H-imipramine binding was compared in rat neuronal membranes.
TheK d value for3H-paroxetine binding to neuronal membranes was 0.08 nM, which is exactly the same value as with platelet membranes. TheK d value for3H-imipramine binding to neuronal membranes was about 4 nM, which is higher than theK d value for3H-imipramine binding to platelet membranes (0.5 nM).
The results indicated that the3H-paroxetine binding site is identical in neuronal membranes and in platelet membranes; this binding site is probably located on the serotonin transport mechanism. In addition, part of the highaffinity3H-imipramine binding to neuronal membranes is probably located on the serotonin transport mechanism, but another part is located elsewhere. Furthermore the polypeptides containing the3H-imipramine binding sites may not be identical in neuronal and platelet membranes.
Key words3H-paroxetine 3H-imipramine Binding sites Rat neuronal membranes
- High affinity binding of3H-paroxetine and3H-imipramine to rat neuronal membranes
Volume 89, Issue 4 , pp 436-439
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