- Published articles
- Congress presentations
-
Efficacy and safety of esmethadone (REL-1017) in patients with major depressive disorder and inadequate response to standard antidepressants: a Phase 3 randomized controlled trial
-
The novel uncompetitive NMDA receptor antagonist esmethadone has no meaningful abuse potential in recreational drug users
-
REL-1017 (esmethadone) as adjunctive treatment in patients with major depressive disorder: a Phase 2a randomized double-blind trial
-
Pharmacokinetics, tolerability, and safety of esmethadone in subjects with chronic kidney disease or hepatic impairment
-
Subanalysis of subjective cognitive measures from a Phase 2, double-blind, randomized trial of REL-1017 in patients with major depressive disorder
-
Sex-dependent effects of the uncompetitive N-methyl-D-aspartate receptor antagonist REL-1017 in G93A-SOD1 amyotrophic lateral sclerosis mice
-
Esmethadone‐HCl (REL‐1017): a promising rapid antidepressant
-
REL-1017 (esmethadone) may rapidly reduce dissociative symptoms in adults with major depressive disorder unresponsive to standard antidepressants: a report of 2 cases
-
REL-1017 (esmethadone) increases circulating BDNF levels in healthy subjects of a Phase 1 clinical study
-
Characterization of the safety and pharmacokinetic profile of d-methadone, a novel N-methyl-D-aspartate receptor antagonist in healthy, opioid-naive subjects: results of two Phase 1 studies
-
Drug–drug interaction studies of esmethadone (REL‐1017) involving CYP3A4‐ and CYP2D6‐mediated metabolism
-
Pharmacological comparative characterization of REL-1017 (esmethadone-HC1) and other NMDAR channel blockers in human heterodimeric N-Methyl-D-Aspartate receptors
-
The N-methyl-D-aspartate receptor blocker REL-1017 (esmethadone) reduces calcium influx induced by glutamate, quinolinic acid and gentamicin
-
REL-1017 (esmethadone, d-methadone) does not cause reinforcing effect, physical dependence and withdrawal signs in Sprague Dawley rats
-
REL-1017 (esmethadone), a novel NMDAR blocker for the treatment of MDD is not neurotoxic in Sprague-Dawley rats
-
The N-methyl-D-aspartate receptor antagonist d-methadone acutely improves depressive-like behavior in the forced swim test performance of rats
-
N-methyl-D-aspartate receptor antagonist d-methadone produces rapid, mTORC1-dependent antidepressant effects
-
Esmethadone (REL-1017) and other uncompetitive NMDAR channel blockers may improve mood disorders via modulation of synaptic kinase-mediated signaling
-
Letter to the Editor regarding ‘Unique pharmacodynamic properties and low abuse liability of the µ-opioid receptor ligand (S)-methadone’
-
Effect of time from onset of major depressive disorder on the therapeutic response to esmethadone (REL-1017)
-
Chronic non-psychedelic psilocybin therapy promotes visual rehabilitation in mice post-occipital stroke
-
Long-term safety and efficacy of esmethadone in patients with major depressive disorder: findings from a 12-Month open-label study
-
N-Methyl-D-Aspartate receptor uncompetitive antagonists and depression, from psychopharmacology and pathology to physiology: a unifying hypothesis for the epigenetic code of neural plasticity
-
No indication of abuse or withdrawal potential with esmethadone (REL-1017): results from two Phase 3 randomized placebo-controlled trials in patients with major depressive disorder
-
Efficacy and safety of esmethadone (REL-1017) in patients with major depressive disorder and inadequate response to standard antidepressants: a phase 3 randomized placebo-controlled trial
-
The serotonin receptor agonist psilocybin as a novel therapeutic approach for NAFLD: preclinical studies
-
Behavioral effects of a 14-day repeated treatment with psilocybin at a low non-psychedelic dose: a preliminary study in C57BL/6J mice
-
Efficacy of esmethadone (REL-1017) in patients with major depressive disorder and antidepressant tolerance (antidepressant tachyphylaxis)
-
No indication of abuse potential and absence of withdrawal from esmethadone (REL-1017) in patients with major depressive disorder
-
Efficacy and safety of esmethadone (REL-1017) in patients with major depressive disorder and inadequate response to standard antidepressants: a phase 3 randomized controlled trial
-
No indication of abuse potential and absence of withdrawal signs and symptoms from esmethadone (REL-1017): results from a phase 3 randomized controlled trial in patients with major depressive disorder
-
No meaningful abuse potential in recreational opioid users of REL-1017 (esmethadone hydrochloride), a new NMDAR antagonist and potential rapid-acting antidepressant
-
REL-1017 (esmethadone hydrochloride) a novel uncompetitive NMDAR antagonist with a preference for NR1-NR2D subtypes shows rapid, robust and sustained rapid antidepressant effects as adjunctive treatment for Major Depressive Disorder
-
No meaningful abuse potential in recreational opioid users of REL-1017 (esmethadone hydrochloride), a new NMDAR antagonist and potential rapid-acting antidepressant
-
No meaningful abuse potential in recreational ketamine users of REL-1017 (esmethadone hydrochloride), a new NMDAR antagonist and potential rapid-acting antidepressant
-
REL-1017 (esmethadone hydrochloride), a potential rapid-acting antidepressant has no meaningful opioid abuse potential in non-clinical and clinical abuse potential studies
-
No meaningful abuse potential in recreational ketamine users of REL-1017 (esmethadone hydrochloride), a new NMDAR antagonist and potential rapid-acting antidepressant
-
REL-1017 (esmethadone hydrochloride) demonstrates neither toxic effects on maternal health nor teratogenic effects in pregnant rats
-
No meaningful opioid abuse liability of REL-1017 (esmethadone; d-methadone), a rapid-acting antidepressant in clinical development: a human abuse potential study
-
REL-1017 (esmethadone) showed no reinforcing properties compared to oxycodone in a rat self-administration study
-
REL-1017 (esmethadone) demonstrates no physical dependence and no withdrawal effects in a rat study
-
Case report: REL-1017 reduces abnormal Clinician Administered Dissociative States Scale scores in patients with major depressive disorder
-
A Phase 2a double-blind randomized trial of REL-1017 (esmethadone) in patients with major depressive disorder: analysis of subscales from the symptoms of depression questionnaire
-
Effect of REL-1017 (esmethadone) on cholesterol, triglycerides, PCSK9 and hs-CRP in patients with major depressive disorder
-
Effect of percentage of life-years from the start of major depressive disorder on the therapeutic response to REL-1017
-
Esmethadone (REL-1017) compares with NMDA receptor antagonists in FLIPR-calcium assay
-
Esmethadone (REL-1017) blocks NMDA receptors and reduces Ca2+ entry in presence of quinolinic acid and gentamicin
-
Esmethadone (REL-1017) reduces glutamate-induced currents in NMDA receptors with the GluN2D subunit
-
Esmethadone (REL-1017) reduces NMDA receptor currents in a concentration dependent manner
-
Esmethadone (REL-1017) shows slower onset kinetics compared to ketamine in manual patch clamp studies
-
Esmethadone (REL-1017) restores NMDA receptor 1 subunit expression in an in vitro model of glutamatergic excitotoxicity
Published articles
Efficacy and safety of esmethadone (REL-1017) in patients with major depressive disorder and inadequate response to standard antidepressants: a Phase 3 randomized controlled trial
J Clin Psychiatry. 2024;85(3):24m15265.
Published articles
The novel uncompetitive NMDA receptor antagonist esmethadone has no meaningful abuse potential in recreational drug users
Transl Psychiatry. 2023 Jun 7;13(1):192.
Published articles
REL-1017 (esmethadone) as adjunctive treatment in patients with major depressive disorder: a Phase 2a randomized double-blind trial
Am J Psychiatry. 2022 Feb;179(2):122-131.
Published articles
Pharmacokinetics, tolerability, and safety of esmethadone in subjects with chronic kidney disease or hepatic impairment
Drugs R D. 2024 Jun;24(2):341-352.
Published articles
Subanalysis of subjective cognitive measures from a Phase 2, double-blind, randomized trial of REL-1017 in patients with major depressive disorder
Prim Care Companion CNS Disord. 2023 Feb 14;25(1):22m03267.
Published articles
Sex-dependent effects of the uncompetitive N-methyl-D-aspartate receptor antagonist REL-1017 in G93A-SOD1 amyotrophic lateral sclerosis mice
Front Neurol. 2024 May 3:15:1384829.
Published articles
Esmethadone‐HCl (REL‐1017): a promising rapid antidepressant
Eur Arch Psychiatry Clin Neurosci. 2023 Oct;273(7):1463-1476.
Published articles
REL-1017 (esmethadone) may rapidly reduce dissociative symptoms in adults with major depressive disorder unresponsive to standard antidepressants: a report of 2 cases
J Clin Psychopharmacol. 2022 Sep-Oct;42(5):503-506.
Published articles
REL-1017 (esmethadone) increases circulating BDNF levels in healthy subjects of a Phase 1 clinical study
Front Pharmacol. 2021 Apr 28:12:671859.
Published articles
Characterization of the safety and pharmacokinetic profile of d-methadone, a novel N-methyl-D-aspartate receptor antagonist in healthy, opioid-naive subjects: results of two Phase 1 studies
J Clin Psychopharmacol. 2019 May/Jun;39(3):226-237.
Published articles
Drug–drug interaction studies of esmethadone (REL‐1017) involving CYP3A4‐ and CYP2D6‐mediated metabolism
Drugs R D. 2024 Mar;24(1):51-68.
Published articles
Pharmacological comparative characterization of REL-1017 (esmethadone-HC1) and other NMDAR channel blockers in human heterodimeric N-Methyl-D-Aspartate receptors
Pharmaceuticals (Basel). 2022 Aug 13;15(8):997.
Published articles
The N-methyl-D-aspartate receptor blocker REL-1017 (esmethadone) reduces calcium influx induced by glutamate, quinolinic acid and gentamicin
Pharmaceuticals (Basel). 2022 Jul 17;15(7):882.
Published articles
REL-1017 (esmethadone, d-methadone) does not cause reinforcing effect, physical dependence and withdrawal signs in Sprague Dawley rats
Sci Rep. 2022 Jul 6;12(1):11389.
Published articles
REL-1017 (esmethadone), a novel NMDAR blocker for the treatment of MDD is not neurotoxic in Sprague-Dawley rats
Front Pharmacol. 2022 Apr 25:13:863959.
Published articles
The N-methyl-D-aspartate receptor antagonist d-methadone acutely improves depressive-like behavior in the forced swim test performance of rats
Exp Clin Psychopharmacol. 2020;28(2):196-201.
Published articles
N-methyl-D-aspartate receptor antagonist d-methadone produces rapid, mTORC1-dependent antidepressant effects
Neuropsychopharmacology. 2019 Dec;44(13):2230-2238.
Published articles
Esmethadone (REL-1017) and other uncompetitive NMDAR channel blockers may improve mood disorders via modulation of synaptic kinase-mediated signaling
Int J Mol Sci. 2022 Oct 13;23(20):12196.
Published articles
Letter to the Editor regarding ‘Unique pharmacodynamic properties and low abuse liability of the µ-opioid receptor ligand (S)-methadone’
Mol Psychiatry. 2024 May 28.
Published articles
Effect of time from onset of major depressive disorder on the therapeutic response to esmethadone (REL-1017)
J Clin Psychiatry 2024;85(2):22m14735
Congress presentations
Chronic non-psychedelic psilocybin therapy promotes visual rehabilitation in mice post-occipital stroke
Society for Neuroscience (SfN) 2024
Congress presentations
Long-term safety and efficacy of esmethadone in patients with major depressive disorder: findings from a 12-Month open-label study
American Society of Clinical Psychopharmacology (ASCP) 2024
Congress presentations
N-Methyl-D-Aspartate receptor uncompetitive antagonists and depression, from psychopharmacology and pathology to physiology: a unifying hypothesis for the epigenetic code of neural plasticity
American Society of Clinical Psychopharmacology (ASCP) 2024
Congress presentations
No indication of abuse or withdrawal potential with esmethadone (REL-1017): results from two Phase 3 randomized placebo-controlled trials in patients with major depressive disorder
American College of Neuropsychopharmacology (ACNP) 2023
Congress presentations
Efficacy and safety of esmethadone (REL-1017) in patients with major depressive disorder and inadequate response to standard antidepressants: a phase 3 randomized placebo-controlled trial
American College of Neuropsychopharmacology (ACNP) 2023
Congress presentations
The serotonin receptor agonist psilocybin as a novel therapeutic approach for NAFLD: preclinical studies
American Association For The Study Of Liver Diseases (AASLD) 2023
Congress presentations
Behavioral effects of a 14-day repeated treatment with psilocybin at a low non-psychedelic dose: a preliminary study in C57BL/6J mice
European College of Neuropsychopharmacology (ECNP) 2023
Congress presentations
Efficacy of esmethadone (REL-1017) in patients with major depressive disorder and antidepressant tolerance (antidepressant tachyphylaxis)
European College of Neuropsychopharmacology (ECNP) 2023
Congress presentations
No indication of abuse potential and absence of withdrawal from esmethadone (REL-1017) in patients with major depressive disorder
European College of Neuropsychopharmacology (ECNP) 2023
Congress presentations
Efficacy and safety of esmethadone (REL-1017) in patients with major depressive disorder and inadequate response to standard antidepressants: a phase 3 randomized controlled trial
American Society of Clinical Psychopharmacology (ASCP) 2023
Congress presentations
No indication of abuse potential and absence of withdrawal signs and symptoms from esmethadone (REL-1017): results from a phase 3 randomized controlled trial in patients with major depressive disorder
American Society of Clinical Psychopharmacology (ASCP) 2023
Congress presentations
No meaningful abuse potential in recreational opioid users of REL-1017 (esmethadone hydrochloride), a new NMDAR antagonist and potential rapid-acting antidepressant
American Society of Clinical Psychopharmacology (ASCP) 2022
Congress presentations
REL-1017 (esmethadone hydrochloride) a novel uncompetitive NMDAR antagonist with a preference for NR1-NR2D subtypes shows rapid, robust and sustained rapid antidepressant effects as adjunctive treatment for Major Depressive Disorder
Ketamine 2022
Congress presentations
No meaningful abuse potential in recreational opioid users of REL-1017 (esmethadone hydrochloride), a new NMDAR antagonist and potential rapid-acting antidepressant
Ketamine 2022
Congress presentations
No meaningful abuse potential in recreational ketamine users of REL-1017 (esmethadone hydrochloride), a new NMDAR antagonist and potential rapid-acting antidepressant
Ketamine 2022
Congress presentations
REL-1017 (esmethadone hydrochloride), a potential rapid-acting antidepressant has no meaningful opioid abuse potential in non-clinical and clinical abuse potential studies
The College of Problems of Drug Dependence (CPDD) 2022
Congress presentations
No meaningful abuse potential in recreational ketamine users of REL-1017 (esmethadone hydrochloride), a new NMDAR antagonist and potential rapid-acting antidepressant
American Society of Clinical Psychopharmacology (ASCP) 2022
Congress presentations
REL-1017 (esmethadone hydrochloride) demonstrates neither toxic effects on maternal health nor teratogenic effects in pregnant rats
Society of Biological Psychiatry (SOBP) 2022
Congress presentations
No meaningful opioid abuse liability of REL-1017 (esmethadone; d-methadone), a rapid-acting antidepressant in clinical development: a human abuse potential study
American College of Neuropsychopharmacology (ACNP) 2021
Congress presentations
REL-1017 (esmethadone) showed no reinforcing properties compared to oxycodone in a rat self-administration study
The College on Problems of Drug Dependence (CPDD) 2021
Congress presentations
REL-1017 (esmethadone) demonstrates no physical dependence and no withdrawal effects in a rat study
The College on Problems of Drug Dependence (CPDD) 2021
Congress presentations
Case report: REL-1017 reduces abnormal Clinician Administered Dissociative States Scale scores in patients with major depressive disorder
Neuroscience Education Institute (NEI) 2021
Congress presentations
A Phase 2a double-blind randomized trial of REL-1017 (esmethadone) in patients with major depressive disorder: analysis of subscales from the symptoms of depression questionnaire
Neuroscience Education Institute (NEI) 2021
Congress presentations
Effect of REL-1017 (esmethadone) on cholesterol, triglycerides, PCSK9 and hs-CRP in patients with major depressive disorder
Neuroscience Education Institute (NEI) 2021
Congress presentations
Effect of percentage of life-years from the start of major depressive disorder on the therapeutic response to REL-1017
American Psychiatric Association (APA) 2021
Congress presentations
Esmethadone (REL-1017) compares with NMDA receptor antagonists in FLIPR-calcium assay
Society of Biological Psychiatry (SOBP) 2021
Congress presentations
Esmethadone (REL-1017) blocks NMDA receptors and reduces Ca2+ entry in presence of quinolinic acid and gentamicin
Society of Biological Psychiatry (SOBP) 2021
Congress presentations
Esmethadone (REL-1017) reduces glutamate-induced currents in NMDA receptors with the GluN2D subunit
Society of Biological Psychiatry (SOBP) 2021
Congress presentations
Esmethadone (REL-1017) reduces NMDA receptor currents in a concentration dependent manner
Society of Biological Psychiatry (SOBP) 2021
Congress presentations
Esmethadone (REL-1017) shows slower onset kinetics compared to ketamine in manual patch clamp studies
Society of Biological Psychiatry (SOBP) 2021
Congress presentations
Esmethadone (REL-1017) restores NMDA receptor 1 subunit expression in an in vitro model of glutamatergic excitotoxicity
Society of Biological Psychiatry (SOBP) 2021
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