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   Articles with "rel 1017" as a keyword



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Effect of REL-1017 (Esmethadone) on Cholesterol, Triglycerides, PCSK9, and hs-CRP in a Phase 2a Double-Blind Randomized Trial in Patients with MDD

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recommendations! Published in 2022 at "CNS Spectrums"

DOI: 10.1017/s1092852922000578

Abstract: Abstract Background Atherosclerotic cardiovascular disease (ASCVD) is the leading cause of morbidity and mortality. Hyperlipidemia and vascular subinflammation play critical roles in the pathogenesis of atherosclerosis. Patients with Major Depressive Disorder (MDD) are at higher… read more here.

Keywords: pcsk9 crp; rel 1017; rel; day ... See more keywords
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REL-1017 (Esmethadone), A Novel NMDAR Blocker for the Treatment of MDD is Not Neurotoxic in Sprague-Dawley Rats

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recommendations! Published in 2022 at "Frontiers in Pharmacology"

DOI: 10.3389/fphar.2022.863959

Abstract: REL-1017 (esmethadone; dextromethadone; (S)-methadone) is the opioid-inactive dextro-isomer of the racemic mixture, (R, S)-methadone. REL-1017 acts as a low affinity, low potency N-methyl-D-aspartate receptor (NMDAR) channel blocker with rapid, robust, and sustained therapeutic effects in… read more here.

Keywords: sprague dawley; rel 1017; 1017 esmethadone; rel ... See more keywords
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Esmethadone (REL-1017) and Other Uncompetitive NMDAR Channel Blockers May Improve Mood Disorders via Modulation of Synaptic Kinase-Mediated Signaling

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recommendations! Published in 2022 at "International Journal of Molecular Sciences"

DOI: 10.3390/ijms232012196

Abstract: This article presents a mechanism of action hypothesis to explain the rapid antidepressant effects of esmethadone (REL-1017) and other uncompetitive N-methyl-D-aspartate receptor (NMDAR) antagonists and presents a corresponding mechanism of disease hypothesis for major depressive… read more here.

Keywords: esmethadone rel; rel 1017; nmdar; glun2d subtypes ... See more keywords
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The N-Methyl-D-Aspartate Receptor Blocker REL-1017 (Esmethadone) Reduces Calcium Influx Induced by Glutamate, Quinolinic Acid, and Gentamicin

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recommendations! Published in 2022 at "Pharmaceuticals"

DOI: 10.3390/ph15070882

Abstract: REL-1017 (esmethadone) is a novel N-methyl-D-aspartate receptor (NMDAR) antagonist and promising rapid antidepressant candidate. Using fluorometric imaging plate reader (FLIPR) assays, we studied the effects of quinolinic acid (QA) and gentamicin, with or without L-glutamate… read more here.

Keywords: gentamicin; rel 1017; induced glutamate; glun1 ... See more keywords
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Pharmacological Comparative Characterization of REL-1017 (Esmethadone-HCl) and Other NMDAR Channel Blockers in Human Heterodimeric N-Methyl-D-Aspartate Receptors

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recommendations! Published in 2022 at "Pharmaceuticals"

DOI: 10.3390/ph15080997

Abstract: Excessive Ca2+ currents via N-methyl-D-aspartate receptors (NMDARs) have been implicated in many disorders. Uncompetitive NMDAR channel blockers are an emerging class of drugs in clinical use for major depressive disorder (MDD) and other neuropsychiatric diseases.… read more here.

Keywords: nmdar channel; rel 1017; nmdar; methyl aspartate ... See more keywords