2007
DOI: 10.1016/j.ejphar.2007.08.017
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Pharmacological properties of the active metabolites of the antidepressants desipramine and citalopram

Abstract: Although major metabolites of some antidepressant drugs are know to be active, their pharmacological effects are poorly characterized. Two of the most selective antidepressants, desipramine (selectively inhibits norepinephrine reuptake) and citalopram (selectively inhibits serotonin reuptake) are frequently used in animal studies of antidepressant action, as well as being useful therapeutically. The primary aim of this study was to determine the affinity of desmethyldesipramine, an active metabolite of desipra… Show more

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Cited by 24 publications
(18 citation statements)
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“…1A), consistent with a previous report (10). Although the binding of DMI to NET occurs with a much higher affinity (nanomolar), a low micromolar value is nevertheless within the reported physiological therapeutic range of the drug (see Table 1).…”
Section: Discussionsupporting
confidence: 80%
“…1A), consistent with a previous report (10). Although the binding of DMI to NET occurs with a much higher affinity (nanomolar), a low micromolar value is nevertheless within the reported physiological therapeutic range of the drug (see Table 1).…”
Section: Discussionsupporting
confidence: 80%
“…Nisoxetine, a NET-selective inhibitor, also appeared to have some inhibitory effect, but like escitalopram, it had no inhibitory effect in the cerebellum. Escitalopram and nisoxetine are known to be highly selective for SERT (100,000-fold over NET) and NET (1,000-fold over SERT), respectively (25,26). If the inhibition seen with nisoxetine pretreatment was attributable to a NET-binding component, then incomplete inhibition by escitalopram in those 4 regions would be expected.…”
Section: Discussionmentioning
confidence: 99%
“…67). The metabolites have lower affinity for the reuptake transporter than the parent (6-to 8-fold) (Owens et al, 1997;Deupree et al, 2007) and circulate at lower steadystate concentrations than the parent (Sidhu et al, 1997). Thus, the metabolites contribute very little to the antidepressant effect of citalopram.…”
Section: Drugs With Metabolites That Possess Target Potency But Comentioning
confidence: 99%