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

  title={High affinity binding of3H-paroxetine and3H-imipramine to rat neuronal membranes},
  author={Erling Mellerup and Per Plenge},
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… 
[3H] sertraline binding to rat brain membranes
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
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
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
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
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
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
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.
Drug inhibition indicates a single-site model of the 5-HT uptake site/antidepressant binding site in rat and human brain
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.


Imipramine binding site. Temperature dependence of the binding of 3H-labeled imipramine and 3H-labeled paroxetine to human platelet membrane.
High affinity binding of [3H]paroxetine and [3H]imipramine to human platelet membranes.
Size determination of binding polymers for [3H]imipramine and [3H]paroxetine in human platelet membranes.
High-affinity [3H]imipramine binding in rat hypothalamus: association with uptake of serotonin but not of norepinephrine.
The results suggest that high-affinity [3H]imipramine binding might be associated with the mechanism of serotonin uptake in the brain.
Quantitative autoradiographic localization of [3H]imipramine binding sites in the brain of the rat: relationship to ascending 5-hydroxytryptamine neuron systems.
The present results underline the possibility that the 5-HT and dopamine hypotheses for the mechanism of action of antidepressant drugs are not mutually exclusive, because both 5- HT and dopamine neurons can be regulated by large numbers of [3H]imipramine binding sites.
Citalopram — Pharmacological profile of a specific serotonin uptake inhibitor with antidepressant activity
  • J. Hyttel
  • Chemistry, Psychology
    Progress in Neuro-Psychopharmacology and Biological Psychiatry
  • 1982
High‐ and Low‐Affinity Binding of [3H]Imipramine in Mouse Cerebral Cortex
Binding of [3H]imipramine in mouse cerebral cortex was found to be nonhomogeneous and low‐affinity binding could be eliminated by the use of low concentrations of imipramines as the competing ligand.
Localisation of Tricyclic Antidepressant Binding Sites on Serotonin Nerve Terminals
Results suggest that [3H]imipramine binding sites are located on serotonin nerve terminals, which are similar to those demonstrated in the brain and platelets of various species including man.
Central and peripheral 5-HT uptake in rats treated chronically with femoxetine, paroxetine, and chlorimipramine
In rats, it appears difficult under chronic conditions to keep the plasma concentrations of chlorimipramine high enough to inhibit neuronal 5-HT uptake without simultaneous high toxic concentrations of DCIP which is a weak 5- HT uptake inhibitor.
Tricyclic antidepressants: therapeutic properties and affinity for alpha-noradrenergic receptor binding sites in the brain.
Affinities of tricyclic drugs for alpha-noradrenergic receptor sites in the brain correlate well with the capacity of these agents to relieve psychomotor agitation and to induce sedation and hypotension; these affinities also correlate inversely with tendencies to elicit psychom motor activation.