Although evidence exists of the presence of serotonin (5-HT) reuptake system in lymphocytes, no information is available on the pharmacological characterization of this structure. Our study aimed to investigate this matter, therefore, by means of the binding of [H-3]-paroxetine ([H-3]PAR), a selective 5-HT reuptake inhibitor (SSRI), which is considered the ligand of choice for binding studies. Lymphocytes were obtained from a pool of 20 healthy subjects who volunteered for the study. The results showed the presence of a specific and saturable [H-3]PAR binding to lymphocyte membranes, with a Hill number close to unity indicative of the presence of one site only. The most potent drugs inhibiting [H-3]PAR binding were SSRIs (paroxetine, fluoxetine, citalopram) followed by clomipramine, imipramine, and 5-HT, whereas haloperidol, mazindol, and nomifensine had a negligible effect. These findings suggest that [H-3]-PAR in human resting lymphocytes specifically labels the 5-HT transporter. (C) 1998 American College of Neuropsychopharmacology. Published by Elsevier Science Inc.
Presence and characterization of the serotonin transporter in human resting lymphocytes
ROSSI, ALESSANDRA;GIANNACCINI, GINO;LUCACCHINI, ANTONIO;
1998-01-01
Abstract
Although evidence exists of the presence of serotonin (5-HT) reuptake system in lymphocytes, no information is available on the pharmacological characterization of this structure. Our study aimed to investigate this matter, therefore, by means of the binding of [H-3]-paroxetine ([H-3]PAR), a selective 5-HT reuptake inhibitor (SSRI), which is considered the ligand of choice for binding studies. Lymphocytes were obtained from a pool of 20 healthy subjects who volunteered for the study. The results showed the presence of a specific and saturable [H-3]PAR binding to lymphocyte membranes, with a Hill number close to unity indicative of the presence of one site only. The most potent drugs inhibiting [H-3]PAR binding were SSRIs (paroxetine, fluoxetine, citalopram) followed by clomipramine, imipramine, and 5-HT, whereas haloperidol, mazindol, and nomifensine had a negligible effect. These findings suggest that [H-3]-PAR in human resting lymphocytes specifically labels the 5-HT transporter. (C) 1998 American College of Neuropsychopharmacology. Published by Elsevier Science Inc.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
