High affinity binding of3H-paroxetine and3H-imipramine to rat neuronal membranes

@article{Mellerup2006HighAB,
  title={High affinity binding of3H-paroxetine and3H-imipramine to rat neuronal membranes},
  author={Erling Mellerup and Per Plenge},
  journal={Psychopharmacology},
  year={2006},
  volume={89},
  pages={436-439}
}
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.TheKd value for3H-paroxetine binding to neuronal membranes was 0.08 nM, which is exactly the same value as with platelet membranes. TheKd value for3H-imipramine binding to neuronal membranes was about 4 nM, which is higher than theKd value for3H-imipramine binding to platelet membranes (0.5 nM).The results indicated… 
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25 Citations
Background Citations
3
Methods Citations
2

25 Citations

[3H] sertraline binding to rat brain membranes
TLDR
A marked decrease in ex vivo [3H] sertraline binding in the brain of rats 7 days after treatment withp-chloroamphetamine was consistent with the loss of serotonin uptake sites induced by this agent.
Binding of some antidepressants to the 5-hydroxytryptamine transporter in brain and platelets
TLDR
Antidepressant agents with properties to inhibit 5-hydroxytryptamine uptake in brain tissue and platelets bind with high affinities to neuronal and platelet membranes and appear to be better ligands than [3H]imipramine.
Regional distribution of specific high affinity binding sites for 3H-imipramine and 3H-paroxetine in human brain
TLDR
The higher affinity of 3H-paroxetine confirms that this compound is a better radioligand for the 5HT uptake site, and suggests that both ligands are good markers of the5HT transporter.
High-affinity [3H]6-nitroquipazine binding sites in rat brain.
Regional distribution of serotonergic pre‐ and postsynaptic markers in human brain
TLDR
The binding characteristics of [3Hl-paroxetine in human brain is investigated to determine its use as a specific 5-HT presynaptic marker.
Changes in the serotonin transporter in the hippocampus of subjects with schizophrenia identified using [3H]paroxetine
TLDR
It would seem that the changes in the affinity of [3H]paroxetine binding to the hippocampus of schizophrenic subjects are not likely to be due to neuroleptic drug treatment but may be involved in the pathology of the illness.
Repeated electroconvulsive shock does not change [3H]-paroxetine binding to the 5-HT uptake site in rat cortical membranes
TLDR
The effects of repeated electroconvulsive shock on the 5-HT uptake site were studied in rat cortex using [3H]-paroxetine binding, and a parallel investigation of β-adrenoceptor binding showed the expected decrease in receptor number.
Regional studies of serotonin and dopamine metabolism and quantification of serotonin uptake sites in human cerebral cortex
TLDR
Results obtaining using [3H]-Paroxetine suggest that 5-HT uptake sites in the human cortex are distributed rather uniformally and are not correlated with 5- HT levels.
The regeneration of d,l-fenfluramine-destroyed serotonergic nerve terminals.
Drug inhibition indicates a single-site model of the 5-HT uptake site/antidepressant binding site in rat and human brain
TLDR
There is no heterogeneity of specific [3H]paroxetine binding, supporting a single site model of the 5-HT uptake site and antidepressant binding site, and changes in apparent binding affinity without changes in the number of binding sites are suggested.
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