Literature DB >> 7888147

[3H]paroxetine and [3H]citalopram as markers of the human brain 5-HT uptake site: a comparison study.

B Arranz1, J Marcusson.   

Abstract

The binding of [3H]paroxetine and [3H]citalopram to the human brain serotonin (5-HT) uptake site has been characterized and compared. Our results reveal that the binding exclusively involved with the 5-HT uptake site is identical for both [3H]ligands. The selective 5-HT uptake inhibitor citalopram displays the highest affinity for this uptake site, as compared with the affinities obtained for desipramine and norzimeldine, which is in accordance with their respective blockage of 5-HT uptake. Similar Bmax values were obtained for both radioligands in the brain regions studied, indicating their binding to the same presynaptic membrane protein. Together these findings suggest that both [3H]paroxetine and [3H]citalopram are good markers of the 5-HT transporter as both bind selectively and with high affinity to the serotonin uptake sites. However, the higher affinity of [3H]paroxetine confirms that this compound is the best radioligand for the 5-HT uptake site available today.

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Year:  1994        PMID： 7888147     DOI： 10.1007/bf01277960

Source DB:  PubMed          Journal:  J Neural Transm Gen Sect


  35 in total

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4.  Regional distribution of the serotonin transport complex in human brain, identified with 3H-paroxetine, 3H-citalopram and 3H-imipramine.

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Journal:  Prog Neuropsychopharmacol Biol Psychiatry       Date:  1990       Impact factor: 5.067

Review 5.  Binding of some antidepressants to the 5-hydroxytryptamine transporter in brain and platelets.

Authors:  J O Marcusson; S B Ross
Journal:  Psychopharmacology (Berl)       Date:  1990       Impact factor: 4.530

6.  Inhibitory and regulatory binding sites on the rat brain serotonin transporter: molecular weight of the [3H]paroxetine and [3H]citalopram binding proteins.

Authors:  P Plenge; E T Mellerup; M Nielsen
Journal:  Eur J Pharmacol       Date:  1990-09-18       Impact factor: 4.432

7.  Studies on the serotonin uptake binding site in major depressive disorder and control post-mortem brain: neurochemical and clinical correlates.

Authors:  A Leake; A F Fairbairn; I G McKeith; I N Ferrier
Journal:  Psychiatry Res       Date:  1991-11       Impact factor: 3.222

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Authors:  J Hyttel
Journal:  Psychopharmacology (Berl)       Date:  1977-03-16       Impact factor: 4.530

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Authors:  D Graham; H Esnaud; S Z Langer
Journal:  Biochem J       Date:  1992-09-15       Impact factor: 3.857

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Authors:  C J Humphreys; J Levin; G Rudnick
Journal:  Mol Pharmacol       Date:  1988-06       Impact factor: 4.436
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  6 in total

1.  In vitro and in vivo characterisation of nor-beta-CIT: a potential radioligand for visualisation of the serotonin transporter in the brain.

Authors:  K A Bergström; C Halldin; H Hall; C Lundkvist; N Ginovart; C G Swahn; L Farde
Journal:  Eur J Nucl Med       Date:  1997-06

2.  The effects of hypothyroidism on 5-HT1A and 5-HT2A receptors and the serotonin transporter protein in the rat brain.

Authors:  A V Kulikov; R Jeanningro
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3.  High affinity [3H]imipramine and [3H]paroxetine binding sites in suicide brains.

Authors:  P Rosel; B Arranz; J Vallejo; M Oros; J M Menchón; P Alvarez; M A Navarro
Journal:  J Neural Transm (Vienna)       Date:  1997       Impact factor: 3.575

4.  Regional distribution of specific high affinity binding sites for 3H-imipramine and 3H-paroxetine in human brain.

Authors:  P Rosel; J M Menchon; M Oros; J Vallejo; T Cortadellas; B Arranz; P Alvarez; M A Navarro
Journal:  J Neural Transm (Vienna)       Date:  1997       Impact factor: 3.575

Review 5.  Citalopram--a review of pharmacological and clinical effects.

Authors:  K Bezchlibnyk-Butler; I Aleksic; S H Kennedy
Journal:  J Psychiatry Neurosci       Date:  2000-05       Impact factor: 6.186

6.  Altered levels of dopamine transporter in the frontal pole and dorsal striatum in schizophrenia.

Authors:  Hirotaka Sekiguchi; Geoff Pavey; Brian Dean
Journal:  NPJ Schizophr       Date:  2019-12-02
  6 in total

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