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20 Results Found

  • Perspective
  • Open Access
20 Citations
4,129 Views
12 Pages

Esmethadone (REL-1017) and Other Uncompetitive NMDAR Channel Blockers May Improve Mood Disorders via Modulation of Synaptic Kinase-Mediated Signaling

  • Stephen M. Stahl,
  • Sara De Martin,
  • Andrea Mattarei,
  • Ezio Bettini,
  • Luca Pani,
  • Clotilde Guidetti,
  • Franco Folli,
  • Marc de Somer,
  • Sergio Traversa and
  • Paolo L. Manfredi
  • + 5 authors

13 October 2022

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 h...

  • Article
  • Open Access
27 Citations
4,844 Views
22 Pages

Pharmacological Comparative Characterization of REL-1017 (Esmethadone-HCl) and Other NMDAR Channel Blockers in Human Heterodimeric N-Methyl-D-Aspartate Receptors

  • Ezio Bettini,
  • Stephen M. Stahl,
  • Sara De Martin,
  • Andrea Mattarei,
  • Jacopo Sgrignani,
  • Corrado Carignani,
  • Selena Nola,
  • Patrizia Locatelli,
  • Marco Pappagallo and
  • Paolo L. Manfredi
  • + 8 authors

13 August 2022

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 neuropsychia...

  • Article
  • Open Access
12 Citations
7,429 Views
14 Pages

Preparation, Characterization and Dermal Delivery of Methadone

  • Chin-Ping Kung,
  • Bruno C. Sil,
  • Jonathan Hadgraft,
  • Majella E. Lane,
  • Bhumik Patel and
  • Renée McCulloch

The use of methadone for the management of pain has received great interest in recent years. Currently, oral and intravenous formulations are available for clinical use. Dermal delivery represents an attractive alternative route of administration for...

  • Systematic Review
  • Open Access
2 Citations
3,137 Views
20 Pages

The Relevance of Pharmacokinetic Biomarkers in Response to Methadone Treatment: A Systematic Review

  • Sheila Recarey-Rama,
  • Jesús Gómez-Trigo,
  • Almudena Gil-Rodriguez,
  • Eduardo Dominguez,
  • Inés Sánchez-Martínez,
  • Ángela Riveiro-Recimil,
  • Alba Barral-Raña,
  • Jose de Leon,
  • Ana Rodriguez-Viyuela and
  • Olalla Maroñas
  • + 2 authors

25 April 2025

Background/Objectives: Methadone maintenance treatment (MMT) is widely used in opioid use disorder (OUD). Its efficacy is influenced by its metabolism, primarily mediated by Cytochrome P450 (CYP450) enzymes in the liver. Genetic polymorphisms in CYP4...

  • Review
  • Open Access
654 Views
18 Pages

Personalized Perioperative Opioid Strategies in Children: Focus on Methadone, Pharmacogenomics and Prevention of Persistent Postoperative Opioid Use

  • Hamsa Priya Bhuchakra,
  • Sennaraj Balasubramanian,
  • Alivia G. Nair,
  • Isabella Marcos,
  • Victoria Chen Falconett,
  • Dominic Falcon,
  • Ayesha Abdul Bari and
  • Senthilkumar Sadhasivam

7 December 2025

Persistent postoperative opioid use (PPOU) is an emerging challenge in pediatric perioperative care, with rates as high as 4.7% in opioid-naive adolescents. Despite advances in multimodal analgesia, current protocols often fail to prevent long-term o...

  • Article
  • Open Access
6 Citations
3,500 Views
25 Pages

Effects of a Two-Month Exercise Training Program on Concurrent Non-Opiate Substance Use in Opioid-Dependent Patients during Substitution Treatment

  • Alexandros Psarianos,
  • Costas Chryssanthopoulos,
  • Athanasios Theocharis,
  • Thomas Paparrigopoulos and
  • Anastassios Philippou

6 February 2024

Background: This randomized controlled trial aimed to evaluate the effects of a two-month exercise intervention on the concurrent non-opiate substance use (alcohol, cocaine, cannabis, and benzodiazepines) in opioid users during their medication treat...

  • Review
  • Open Access
1,299 Views
34 Pages

Crosstalk Between Glycinergic and N-Methyl-D-Aspartate Receptor-Mediated Glutamatergic Transmission in Behaviours Associated with Opioid Use Disorder

  • Nariman Essmat,
  • Imre Boldizsár,
  • Yashar Chalabiani,
  • Bence Tamás Varga,
  • Sarah Kadhim Abbood,
  • Judit Mária Kirchlechner-Farkas,
  • Kornél Király,
  • Ildikó Miklya,
  • István Gyertyán and
  • Mahmoud Al-Khrasani
  • + 4 authors

29 October 2025

The current pharmacological approach for the treatment of opioid use disorder (OUD), as a result of prescription misuse or illicit opioids, utilises opioid ligands that have either an agonist or antagonist profile. In this context, methadone and bupr...

  • Article
  • Open Access
3 Citations
5,762 Views
14 Pages

Cortisol and β-Endorphin Responses During a Two-Month Exercise Training Program in Patients with an Opioid Use Disorder and on a Substitution Treatment

  • Alexandros E. Psarianos,
  • Anastassios Philippou,
  • Argyro Papadopetraki,
  • Eirini Chatzinikita,
  • Costas Chryssanthopoulos,
  • Apostolos Theos,
  • Athanasios Theocharis,
  • Chara Tzavara and
  • Thomas Paparrigopoulos

Physical exercise may affect drug use by balancing neurohormonal system mechanisms. Cortisol and β-endorphin, associated with stress, mood, and pleasure feelings, can be affected by exercise and act as regulators of withdrawal symptoms associate...

  • Article
  • Open Access
3 Citations
2,628 Views
11 Pages

The Discrimination Against, Health Status and Wellness of People Who Use Drugs in Italian Services: A Survey

  • Concetta Paola Pelullo,
  • Fabio Curcio,
  • Francesco Auriemma,
  • Giuseppe Cefalo,
  • Antonio Fabozzi,
  • Riccardo Rossiello,
  • Laura Spagnoli and
  • Francesco Attena

30 September 2019

Background and Objectives: The aims of this study are to: describe the sociodemographic characteristics and typology of drug addiction among people who use drugs that attend the Servizio per le Dipendenze (SerD), and evaluate the competence and abili...

  • Review
  • Open Access
14 Citations
4,899 Views
35 Pages

Exploring the Therapeutic Potential of N-Methyl-D-Aspartate Receptor Antagonists in Neuropathic Pain Management

  • Ciprian Pușcașu,
  • Cornel Chiriță,
  • Simona Negreș and
  • Nicoleta Mirela Blebea

16 October 2024

Neuropathic pain (NeP) is a complex and debilitating condition that impacts millions of people globally. Although various treatment options exist, their effectiveness is often limited, and they can be accompanied by significant side effects. In recen...

  • Article
  • Open Access
31 Citations
6,029 Views
21 Pages

The use of the new psychoactive substances is continuously growing and the implementation of accurate and sensible analysis in biological matrices of users is relevant and fundamental for clinical and forensic purposes. Two different analytical techn...

  • Article
  • Open Access
1 Citations
960 Views
14 Pages

28 August 2025

This paper introduces a novel Lateral Extraction Enhanced Desorption Electrospray Ionization (LEE-DESI) source. This source is specifically designed to tackle the crucial issue of electric field interference in dual-channel ambient ionization mass sp...

  • Perspective
  • Open Access
32 Citations
9,511 Views
26 Pages

Mental Disorders and Heroin Use Disorder (HUD) often co-occur and constitute correlated risk factors that the authors believe are best considered from a unitary perspective. In this article we review and discuss data collected by the V.P. Dole Resear...

  • Article
  • Open Access
5 Citations
4,511 Views
20 Pages

Pharmacogenetics of Lethal Opioid Overdose: Review of Current Evidence and Preliminary Results from a Pilot Study

  • Leen Magarbeh,
  • Ilona Gorbovskaya,
  • Richard Wells,
  • Reuven Jhirad,
  • Bernard Le Foll and
  • Daniel J. Müller

There has been a worldwide substantial increase in accidental opioid-overdose deaths. The aim of this review, along with preliminary results from our pilot study, is to highlight the use of pharmacogenetics as a tool to predict causes of accidental o...

  • Article
  • Open Access
5 Citations
8,419 Views
14 Pages

2 September 2016

A qualitative study was undertaken with five people on methadone maintenance treatment (MMT) to better understand their experiences and daily routines. Through an in-depth exploration of their everyday occupations, we sought to reveal the ongoing cha...

  • Article
  • Open Access
4 Citations
2,207 Views
13 Pages

20 November 2024

Background/Objectives: This study evaluates the applicability of a comprehensive two-dimensional gas chromatography−flame ionisation detection (GC×GC−FID) approach for the simultaneous determination of 12 underivatised psychoactive...

  • Article
  • Open Access
16 Citations
4,117 Views
14 Pages

Heteromerization of Endogenous Mu and Delta Opioid Receptors Induces Ligand-Selective Co-Targeting to Lysosomes

  • Lyes Derouiche,
  • Florian Pierre,
  • Stéphane Doridot,
  • Stéphane Ory and
  • Dominique Massotte

30 September 2020

Increasing evidence indicates that native mu and delta opioid receptors can associate to form heteromers in discrete brain neuronal circuits. However, little is known about their signaling and trafficking. Using double-fluorescent knock-in mice, we i...

  • Article
  • Open Access
1,513 Views
18 Pages

Monitoring Opioid-Use-Disorder Treatment Adherence Using Smartwatch Gesture Recognition

  • Andrew Smith,
  • Kuba Jerzmanowski,
  • Phyllis Raynor,
  • Cynthia F. Corbett and
  • Homayoun Valafar

12 April 2025

The opioid epidemic in the United States has significantly impacted pregnant women with opioid use disorder (OUD), leading to increased health and social complications. This study explores the feasibility of using machine learning algorithms with con...

  • Article
  • Open Access
10 Citations
7,809 Views
22 Pages

28 August 2020

Opioids and their antagonists alter vitamin C metabolism. Morphine binds to glutathione (l-γ-glutamyl-l-cysteinyl-glycine), an intracellular ascorbic acid recycling molecule with a wide range of additional activities. The morphine metabolite mo...

  • Article
  • Open Access
16 Citations
7,412 Views
11 Pages

Assessment of Unsuspected Exposure to Drugs of Abuse in Children from a Mediterranean City by Hair Testing

  • Simona Pichini,
  • Oscar Garcia-Algar,
  • Airam Alvarez,
  • Massimo Gottardi,
  • Emilia Marchei,
  • Fiorenza Svaizer,
  • Manuela Pellegrini,
  • Maria Concetta Rotolo and
  • Roberta Pacifici

Hair testing was used to investigate the prevalence of unsuspected exposure to drugs of abuse in a group of children presenting to an urban paediatric emergency department without suggestive signs or symptoms. Hair samples were obtained from 114 chil...