Search Results - "Inturrisi, Charles"
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Cav1.3 L-type Ca2+ channel-activated CaMKII/ERK2 pathway in the ventral tegmental area is required for cocaine conditioned place preference
Published in Neuropharmacology (15-02-2023)“…We have previously demonstrated that pharmacological blockade of ventral tegmental area (VTA) Cav1.3 L-type calcium channels (LTCCs) using Cav1.2…”
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Esmethadone-HCl (REL-1017): a promising rapid antidepressant
Published in European archives of psychiatry and clinical neuroscience (01-10-2023)“…This review article presents select recent studies that form the basis for the development of esmethadone into a potential new drug. Esmethadone is a promising…”
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REL-1017 (Esmethadone) as Adjunctive Treatment in Patients With Major Depressive Disorder: A Phase 2a Randomized Double-Blind Trial
Published in The American journal of psychiatry (01-02-2022)“…The purpose of this study was to examine the effects of REL-1017 (esmethadone), a novel -methyl-d-aspartate receptor (NMDAR) channel blocker, in patients with…”
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4
Comment on “Novel Glutamatergic Modulators for the Treatment of Mood Disorders: Current Status
Published in CNS drugs (01-02-2022)Get full text
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The N-Methyl-D-Aspartate Receptor Antagonist d-Methadone Acutely Improves Depressive-Like Behavior in the Forced Swim Test Performance of Rats
Published in Experimental and clinical psychopharmacology (01-04-2020)“…d-Methadone (dextromethadone) is a noncompetitive N-methyl-D-aspartate receptor (NMDAR) antagonist that binds to the dizocilpine (MK-801)-binding site of the…”
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Esmethadone (REL-1017) and Other Uncompetitive NMDAR Channel Blockers May Improve Mood Disorders via Modulation of Synaptic Kinase-Mediated Signaling
Published in International journal of molecular sciences (13-10-2022)“…This article presents a mechanism of action hypothesis to explain the rapid antidepressant effects of esmethadone (REL-1017) and other uncompetitive…”
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The novel uncompetitive NMDA receptor antagonist esmethadone (REL-1017) has no meaningful abuse potential in recreational drug users
Published in Translational psychiatry (07-06-2023)“…Esmethadone (REL-1017) is the opioid-inactive dextro-isomer of methadone and a low-affinity, low-potency uncompetitive NMDA receptor antagonist. In a Phase 2,…”
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Letter to the Editor regarding 'Unique pharmacodynamic properties and low abuse liability of the µ-opioid receptor ligand (S)-methadone'
Published in Molecular psychiatry (28-05-2024)Get full text
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REL-1017 (Esmethadone) Increases Circulating BDNF Levels in Healthy Subjects of a Phase 1 Clinical Study
Published in Frontiers in pharmacology (28-04-2021)“…Brain-derived neurotrophic factor (BDNF), a neurotrophin widely expressed in the central nervous system, exhibits important effects on neural plasticity. BDNF…”
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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
Published in The journal of clinical psychiatry (17-06-2024)“…To test esmethadone (REL-1017) as adjunctive treatment in patients with major depressive disorder (MDD) and inadequate response to standard antidepressants. In…”
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Drug–Drug Interaction Studies of Esmethadone (REL-1017) Involving CYP3A4- and CYP2D6-Mediated Metabolism
Published in Drugs in R&D (01-03-2024)“…Background and Objective Esmethadone (dextromethadone; d-methadone; S-methadone (+)-methadone; REL-1017) is the opioid inactive dextro-isomer of racemic…”
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REL-1017 (esmethadone; d-methadone) does not cause reinforcing effect, physical dependence and withdrawal signs in Sprague Dawley rats
Published in Scientific reports (06-07-2022)“…REL-1017 (esmethadone, d -methadone) is the opioid-inactive d-isomer of racemic d,l -methadone. REL-1017 may exert antidepressant effects via uncompetitive N…”
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Pharmacokinetics, Tolerability, and Safety of Esmethadone in Subjects with Chronic Kidney Disease or Hepatic Impairment
Published in Drugs in R&D (01-06-2024)“…Background and Objectives Esmethadone (dextromethadone; d-methadone; S-methadone (+)-methadone; REL-1017) is a low potency N -methyl- D -aspartate (NMDA)…”
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The N-Methyl-D-Aspartate Receptor Blocker REL-1017 (Esmethadone) Reduces Calcium Influx Induced by Glutamate, Quinolinic Acid, and Gentamicin
Published in Pharmaceuticals (Basel, Switzerland) (17-07-2022)“…REL-1017 (esmethadone) is a novel N-methyl-D-aspartate receptor (NMDAR) antagonist and promising rapid antidepressant candidate. Using fluorometric imaging…”
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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
Published in Pharmaceuticals (Basel, Switzerland) (01-08-2022)“…Excessive Ca2+ currents via N-methyl-D-aspartate receptors (NMDARs) have been implicated in many disorders. Uncompetitive NMDAR channel blockers are an…”
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Clinical Pharmacology of Opioids for Pain
Published in The Clinical journal of pain (01-07-2002)“…The pharmacological effects of the opioid analgesics are derived from their complex interactions with three opioid receptor types (μ, δ, and κ; morphine is an…”
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Understanding Opioid Actions, Pain and Analgesia: A Tribute to Dr. Gavril Pasternak
Published in Cellular and molecular neurobiology (01-07-2021)“…This special issue is a tribute to our mentor, colleague and friend, Gavril W. Pasternak, MD, PhD. Homage to the breadth and depth of his work (~ 450…”
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Stabilization of the μ-Opioid Receptor by Truncated Single Transmembrane Splice Variants through a Chaperone-like Action
Published in The Journal of biological chemistry (19-07-2013)“…The μ-opioid receptor gene, OPRM1, undergoes extensive alternative pre-mRNA splicing, as illustrated by the identification of an array of splice variants…”
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N-Methyl- d-aspartate receptor (NMDAR) independent maintenance of inflammatory pain
Published in Pain (Amsterdam) (01-02-2010)“…Following peripheral inflammation, NMDA receptor (NMDAR) activation in spinal cord dorsal horn neurons facilitates the generation of pain in response to low…”
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Pain assessment, management, and control among patients 65 years or older receiving hospice care in the U.S
Published in Journal of pain and symptom management (01-11-2016)“…Abstract Context Knowledge is limited regarding pain assessment and management practices, as well as pain-related outcomes in hospice care. Objectives To…”
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