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… Expand
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27 Citations
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Methods Citations
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27 Citations

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Citation Type

[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. Expand
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. Expand
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. Expand
High-affinity [3H]6-nitroquipazine binding sites in rat brain.
TLDR
The results indicate that the binding site specifically labelled by [3H]6-nitroquipazine is associated with the neuronal 5-HT transporter complex, an excellent radioligand for the study of the5-HT uptake system. Expand
Inhibitory and regulatory binding sites on the rat brain serotonin transporter: molecular weight of the [3H]paroxetine and [3H]citalopram binding proteins.
TLDR
The results support a hypothesis that the binding area for citalopram is located deeper in the transport channel than the [3H]paroxetine binding area, and suggest that the two high-affinity binding sites probably cover different, but overlapping, parts of the protein molecule. Expand
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. Expand
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. Expand
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. Expand
Distribution of indoleamines and [3H]paroxetine binding in rat brain regions following acute or perinatal Δ9-tetrahydrocannabinol treatments
TLDR
The present results show that acute and maternal exposure to Δ9-THC produced different effects on the central 5-HT system of the offspring, with a clear regional especifity, but with no changes in the densities of 5- HT uptake sites. Expand
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. Expand
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