- Published articles
- Congress presentations
-
Long-term safety and efficacy of esmethadone in patients with major depressive disorder: findings from a 12-Month open-label study
-
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
-
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
-
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
-
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
-
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
-
Esmethadone (REL-1017) compares with NMDA receptor antagonists in FLIPR-calcium assay
-
REL-1017 (esmethadone hydrochloride), a potential rapid-acting antidepressant has no meaningful opioid abuse potential in non-clinical and clinical abuse potential studies
-
REL-1017 (esmethadone) may rapidly reduce dissociative symptoms in adults with major depressive disorder unresponsive to standard antidepressants: a report of 2 cases
-
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
-
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
-
No meaningful abuse potential in recreational opioid users of REL-1017 (esmethadone hydrochloride), a new NMDAR antagonist and potential rapid-acting antidepressant
-
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 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 opioid abuse liability of REL-1017 (esmethadone; d-methadone), a rapid-acting antidepressant in clinical development: a human abuse potential study
-
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
-
Esmethadone (REL-1017) blocks NMDA receptors and reduces Ca2+ entry in presence of quinolinic acid and gentamicin
-
REL-1017 (esmethadone) showed no reinforcing properties compared to oxycodone in a rat self-administration study
-
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
-
REL-1017 (esmethadone) demonstrates no physical dependence and no withdrawal effects in a rat study
-
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
-
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) 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
-
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)
Congress presentations
Long-term safety and efficacy of esmethadone in patients with major depressive disorder: findings from a 12-Month open-label study
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
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
ACNP 2023
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
ASCP 2024
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
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.
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)
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
Esmethadone (REL-1017) compares with NMDA receptor antagonists in FLIPR-calcium assay
Society of Biological Psychiatry (SOBP) Annual Meeting 2021
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
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.
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) Annual Meeting 2022
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.
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
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.
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 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) 60th Annual Meeting 2021
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.
Congress presentations
Esmethadone (REL-1017) blocks NMDA receptors and reduces Ca2+ entry in presence of quinolinic acid and gentamicin
Society of Biological Psychiatry (SOBP) Annual Meeting 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) Annual Meeting 2021
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.
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) Annual Meeting 2021
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
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
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) Annual Meeting 2021
Congress presentations
Esmethadone (REL-1017) reduces glutamate-induced currents in NMDA receptors with the GluN2D subunit
Society of Biological Psychiatry (SOBP) Annual Meeting 2021
Congress presentations
Esmethadone (REL-1017) reduces NMDA receptor currents in a concentration dependent manner
Society of Biological Psychiatry (SOBP) Annual Meeting 2021
Congress presentations
Esmethadone (REL-1017) shows slower onset kinetics compared to ketamine in manual patch clamp studies
Society of Biological Psychiatry (SOBP) Annual Meeting 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) Annual Meeting 2021
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
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