Multimodal antidepressant vortioxetine increases frontal cortical oscillations unlike escitalopram and duloxetine – a quantitative EEG study in rats was written by Leiser, S. C.;Pehrson, A. L.;Robichaud, P. J.;Sanchez, C.. And the article was included in British Journal of Pharmacology in 2014.Name: (R)-3-((2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)phenol hydrochloride This article mentions the following:
Background and Purpose : EEG studies show that 5-HT is involved in regulation of sleep-wake state and modulates cortical oscillations. Vortioxetine is a 5-HT3, 5-HT7, and 5-HT1D receptor antagonist, 5-HT1B partial agonist, 5-HT1A agonist, and 5-HT transporter inhibitor. Preclin. (animal) and clin. studies with vortioxetine show pos. impact on cognitive metrics involving cortical function. Here we assess vortioxetine’s effect on cortical neuronal oscillations in actively awake rats. Exptl. Approach : Telemetric EEG recordings were obtained with the following treatments (mg·kg-1, s.c.): vehicle, vortioxetine (0.1, 1.0, 3.0, 10), 5-HT1A agonist flesinoxan (2.5), 5-HT3 antagonist ondansetron (0.30), 5-HT7 antagonist SB-269970-A (10), escitalopram (2.0), duloxetine (10) and vortioxetine plus flesinoxan. Target occupancies were determined by ex vivo autoradiog. Key Results : Vortioxetine dose-dependently increased wakefulness. Flesinoxan, duloxetine, ondansetron, but not escitalopram or SB-269970-A increased wakefulness. Quant. spectral analyses showed vortioxetine alone and with flesinoxan increased θ (4-8 Hz), α (8-12 Hz) and γ (30-50 Hz) power. Duloxetine had no effect on θ and γ, but decreased α power, while escitalopram produced no changes. Ondansetron and SB-269970 (≈31-35% occupancy) increased θ power. Flesinoxan (≈41% occupancy) increased θ and γ power. Conclusions and Implications : Vortioxetine increased wakefulness and increased frontal cortical activity, most likely because of its 5-HT7 and 5-HT3 antagonism and 5-HT1A agonism. Vortioxetine differs from escitalopram and duloxetine by increasing cortical θ, α and γ oscillations. These preclin. findings suggest a role of vortioxetine in modulating cortical circuits known to be recruited during cognitive behaviors and warrant further investigation as to their clin. impact. In the experiment, the researchers used many compounds, for example, (R)-3-((2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)phenol hydrochloride (cas: 261901-57-9Name: (R)-3-((2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)phenol hydrochloride).
(R)-3-((2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)phenol hydrochloride (cas: 261901-57-9) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Name: (R)-3-((2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)phenol hydrochloride
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics