Citalopram — Pharmacological profile of a specific serotonin uptake inhibitor with antidepressant activity

  title={Citalopram — Pharmacological profile of a specific serotonin uptake inhibitor with antidepressant activity},
  author={John Hyttel},
  journal={Progress in Neuro-Psychopharmacology and Biological Psychiatry},
  • J. Hyttel
  • Published 31 December 1982
  • Chemistry, Psychology, Biology
  • Progress in Neuro-Psychopharmacology and Biological Psychiatry

Comparative pharmacology of selective serotonin re-uptake inhibitors (SSRIs)

Selective serotonin re-uptake inhibitors (SSRIs) are those which have a high potency ratio of 5-HT-uptakes inhibition as compared to NA-uptaking inhibition, together with slight or no effect on other uptake mechanisms, neurotransmitter receptors, enzymes, etc.

Biochemical effects of the antidepressant paroxetine, a specific 5-hydroxytryptamine uptake inhibitor

Paroxetine provides a useful pharmacological tool for investigating 5-HT systems and furthermore should be an antidepressant with reduced tricyclic-like side-effects.

Development of antidepressant drugs. Fluoxetine (Prozac) and other selective serotonin uptake inhibitors.

Some of the background which attracted the attention, and some studies on the chemical series of phenoxyphenylpropylamines and the enantiomers of fluoxetine and its major metabolite norfluoxetines as inhibitors of 5-HT and NE uptake in vitro are presented.

Alaproclate, a new selective 5-HT uptake inhibitor with therapeutic potential in depression and senile dementia

Alaproclate was found to display a regional selectivity in blocking 5-HT uptake in vivo (measured with the H 75/12-method) and was most potent in the hippocampus and hypothalamus followed by striatum and cerebral cortex with a low potency in the spinal cord.

Serotonin uptake inhibitors

In contrast to tricyclic antidepressants most of which inhibit receptors for acetylcholine, histamine, NA, 5-HT or DA, most selective 5- HT-uptake inhibitors neither bind to nor inhibit these receptors.

Serotonin autoreceptor subsensitivity and antidepressant activity.

Escitalopram, the S-(+)-enantiomer of citalopram, is a selective serotonin reuptake inhibitor with potent effects in animal models predictive of antidepressant and anxiolytic activities

Escitalopram is a very selective 5-HT reuptake inhibitor which is effective in animal models predictive of antidepressant and anxiolytic activities and had very potent anti-aggressive effects when co-administered with l-5-HTP.

Effects of citalopram, a synthetic serotonin uptake inhibitor, on indoleamine and catecholamine concentrations in the cerebrospinal fluid of freely moving rats

  • H. TohgiT. Abe Y. Ikeda
  • Biology, Chemistry
    Journal of neural transmission. Parkinson's disease and dementia section
  • 1995
CSF results appear to reflect selective inhibition of 5-HT uptake in brain tissues by citalopram that is not associated with changes in catecholamines, indicating that there is coordination of the serotonin and kynurenine pathways in normal rats.



Serotonin--dopamine interactions in the nigrostriatal system.


The most commonly used classical antidepressants and some prominent representatives of the newer classes of uptake inhibitors in the same standardised test procedures in vivo and in vitro are compared.

Effect of a specific 5HT uptake inhibitor (citalopram) on drug accumulation by rat lung slices.

It is concluded that at low concentrations, citalopram is a specific and potent inhibitor of 5HT uptake by rat lung slices.

Effect of antidepressants, lithium and electroconvulsive treatment on rat serum prolactin levels

The ability of bupropion and mazindol to inhibit alpha‐methylparatyrosine‐ induced prolactin secretion, and of nomifensine to inhibit reserpine‐induced prolact in secretion, is consistent with other evidence that these agents are indirect dopamine (DA) agonists.

Inhibitory effect of two newer antidepressants, Lu 5-003 and Lu 3-010, on serotonin uptake in human blood platelets in vitro.

The inhibitory effect of Lu 5-003 was found to be of the competitive type and the possible correlation between inhibitory effects on the “serotonin pump” and the antidepressant effect is discussed briefly.

Antidepressants and serotonin neurons of the raphe.

The 'capillary effect' differentiates antidepressant drugs acting specifically on 5-HT or NA neurons, and may be considered together with other parameters which also indicate asymmetries on the modes of action of antidepressant drugs, such as effects on monoamine turnover and on receptor sensitivity.

Effects of antidepressant drugs on different receptors in the brain.

Effect of antidepressant drugs on accumulation and disappearance of monoamines formed in vivo from labelled precursors in mouse brain

The effect of some tricyclic antidepressants on the accumulation and disappearance of labelled 5-HT (3H-5-HT), dopamine and noradrenaline formed in mouse brain in vivo after the administration of [3H]tryptophan or [14C]tyrosine intravenously is reported.