Characterization of [3H]paroxetine binding to rat cortical membranes

Habert, Estelle; Graham, David Y.; Tahroui, Lila; Claustre, Y.; Langer, Salomón Z.

doi:10.1016/0014-2999(85)90668-5

Cited by 264 publications

(93 citation statements)

References 32 publications

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“…A single binding site, however, has already been determined in rat cortical membrane with different ligands of the serotonin transporter such as [ 3 H]paroxetine (Habert et al, 1985), et al, 1987), and [ 125 I]␤-CIT (Boja et al, 1992). The affinity of [ 3 H]MADAM for the serotonin transporter was at least 2 times greater than described for the most commonly used in vitro radioactive probes such as [ 3 H]paroxetine (Habert et al, 1985) 3 H]M-ADAM showed no inhibitory effect of desipramine (norepinephrine transporter) or GBR 12935 (dopamine transporter), a poor inhibitory effect of nisoxetine (norepinephrine transporter) and PE2I (dopamine transporter), and a strong effect of serotonin transporter ligands such as citalopram, paroxetine, and ADAM. This showed that MADAM had around 1000-fold selectivity for the serotonin transporter over the norepinephrine transporter and dopamine transporter, comparable to that of ADAM and DASB (Wilson et al, 2000).…”

Section: Discussionmentioning

confidence: 99%

Pharmacological Characterization ofN,N-Dimethyl-2-(2-amino-4-methylphenyl thio)benzylamine as a Ligand of the Serotonin Transporter with High Affinity and Selectivity

Chalon

Tarkiainen²,

Garreau³

et al. 2003

J Pharmacol Exp Ther

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Serotonin transporter has a key-role in regulation of serotoninergic function, and is involved in numerous neurodegenerative and psychiatric disorders. To obtain an efficient radioactive ligand allowing the study of this transporter in vitro and in vivo, we synthesized a new diphenyl sulfide derivative, N,N-dimethyl-2-(2-amino-4-methylphenylthio)benzylamine or MADAM. We present here extensive pharmacological characterization of this compound.[3 H]MADAM bound to serotonin transporters with a very high affinity in vitro on rat cortical membranes, at least 2 times better than the most commonly used radioactive probes (K d , 60 pM; B max , 543 fmol/mg of protein). Competition studies showed few inhibitory effect of nisoxetine (K i ϭ 270 nM), no inhibitory effect of desipramine or 1-[2-(diphenylmethoxy) ethyl]-4-(3-phenylpropyl)piperazine (GBR 12935) (K i Ͼ1000 nM), and strong effect of paroxetine (K i ϭ 0.32 nM) and citalopram (K i ϭ 1.57 nM). Therefore, MADAM has around 1000-fold better selectivity for the serotonin transporter than for other transporters. Autoradiographic studies both on rat and postmortem human brain slices demonstrated that the distribution of

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Section: Discussionmentioning

confidence: 99%

Pharmacological Characterization ofN,N-Dimethyl-2-(2-amino-4-methylphenyl thio)benzylamine as a Ligand of the Serotonin Transporter with High Affinity and Selectivity

Chalon

Tarkiainen²,

Garreau³

et al. 2003

J Pharmacol Exp Ther

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“…Blood platelets are able to take up, store, and release 5-HT via mechanisms that are very similar to those of central 5-HT neurons (Sneddon 1973;Stahl 1977). [ 3 H]-paroxetine binds with high affinity to a specific population of binding sites located on platelets and neuronal membranes associated with 5-HT uptake mechanisms (Mellerup et al 1983;Habert et al 1985;Cheetham et al 1993).…”

Section: Discussionmentioning

confidence: 99%

Peripheral Markers of Serotonergic and Noradrenergic Function in Post-Pubertal, Caucasian Males with Autistic Disorder

Croonenberghs

Delmeire²,

Verkerk³

et al. 2000

Neuropsychopharmacology

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Some studies have suggested that disorders in the peripheral and central metabolism of serotonin (5-HT) and noradrenaline may play a role in the pathophysiology of autistic disorder. This study examines serotonergic and noradrenergic markers in a study(5-15 per 10.000) and is four times more common in boys than in girls. Research on the biological pathophysiology of autism has found some evidence for a role of the turnover of serotonin (5-HT) and catecholamines.

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“…Blood platelets are able to take up, store, and release 5-HT via mechanisms that are very similar to those of central 5-HT neurons (Sneddon 1969;1973;Stahl 1977). [ 3 H]-paroxetine binds with high affinity to a specific population of binding sites located on platelets and neuronal membranes associated with 5-HT uptake mechanisms (Mellerup et al 1983;Habert et al 1985;Cheetham et al 1993). It has been found that the cloned 5-HT transporter on human platelets is identical to the 5-HT transporter in human brain (Lesch et al 1993).…”

Section: Discussionmentioning

confidence: 99%

Serotonergic and Noradrenergic Markers of Post-Traumatic Stress Disorder with and without Major Depression

Maes

1999

Neuropsychopharmacology

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Characterization of [3H]paroxetine binding to rat cortical membranes

Cited by 264 publications

References 32 publications

Pharmacological Characterization ofN,N-Dimethyl-2-(2-amino-4-methylphenyl thio)benzylamine as a Ligand of the Serotonin Transporter with High Affinity and Selectivity

Pharmacological Characterization ofN,N-Dimethyl-2-(2-amino-4-methylphenyl thio)benzylamine as a Ligand of the Serotonin Transporter with High Affinity and Selectivity

Peripheral Markers of Serotonergic and Noradrenergic Function in Post-Pubertal, Caucasian Males with Autistic Disorder

Serotonergic and Noradrenergic Markers of Post-Traumatic Stress Disorder with and without Major Depression

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