Decrease of the platelet 5‐HT_2A receptor function by long‐term imipramine treatment in endogenous depression

Abstract

The results showed a decrease in a platelet functional response mediated by 5-HT2A receptors following effective imipramine treatment, suggesting that desensitization or down-regulation of the 5-HT2A receptor function could be linked to the therapeutic effect of some antidepressants. The data also support the use of platelet aggregometry as a surrogate measurement of antidepressant action, particularly in intra-subject designs.

Synergistic antidepressant- and anxiolytic-like effects of harmaline along with cinanserin in acute restraint stress-treated mice

“…+++p < 0.001 in comparison with the cinanserin group. ###p < 0.001 and #p < 0.05 in comparison with the ARS group inhibition as well as enhancement of BDNF levels could induce antidepressant-and anxiolytic-like responses (Dos Santos et al 2016a;Gomez-Gil et al 2004). Moreover, the obtained results revealed that there was an interaction between the harmaline and 5-HT2 receptor on the modulation of depression-and anxiety-like behaviors in the ARS mice.…”

“…Since anxiety is a symptom commonly observed in depressed patients after the acute application of SSRIs, the beneficial effects of 5-HT2 receptor antagonists on the antidepressant response could involve anxiolytic behaviors (Dekeyne et al 2008). Researches revealed that the desensitization or downregulation of 5-HT2 receptors could be related to the therapeutic properties of some antidepressants (Gomez-Gil et al 2004). Imaging studies supported this hypothesis because the downregulation of the 5-HT2 receptor was identified in the brain of depressed patients in response to SSRI treatment (Meyer et al 2001).…”

Rapid and sustained symptom reduction following psilocybin treatment for anxiety and depression in patients with life-threatening cancer: a randomized controlled trial

“…In considering changes at the 5HT2A receptor as a potential mechanism of action: cortical 5HT2A receptor expression is increased in postmortem samples of patients with depression who display suicidality (Mendelson, 2000; Pandey et al, 2002; Shelton et al, 2009); depressed patients with elevated pessimism display increased PFC 5HT2A receptor binding compared to control participants (Bhagwagar et al, 2006; Meyer, 2012; Meyer et al, 2003); and sustained treatment with various anti-depressants (e.g. selective serotonin reuptake inhibitors, tricyclic anti-depressants) have been associated with a reduction of 5HT2A receptor density (Gomez-Gil et al, 2004; Yamauchi et al, 2006). …”

Effects of Imipramine and Bupropion on the Duration of Immobility of ACTH-Treated Rats in the Forced Swim Test: Involvement of the Expression of 5-HT_2A Receptor mRNA

“…[18][19][20][21] Using drugs with significant antagonistic properties toward the 5-HT 2A receptor (mianserin and mirtazapine), in addition to selective serotonin reuptake inhibitor (SSRI)s enhanced therapeutic responses in patients with major depression. 22,23) In an animal study, a reduction in the number of 5-HT 2A receptors caused by the administration of an antisense oligonucleotide decreased the duration of immobility in the forced swim test in mice.…”