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Pharmaceuticals

ISSN 1424-8247

33 papers in the library · 380 citations · publishing 2011-2026

Papers

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Alkyl-Chain Extension and Terminal Amine Substitution Shape Cardiotoxic Profiles of Methylenedioxy Cathinones in Zebrafish Embryos

Pharmaceuticals August 7, 2026 Ouwais Aljabasini, Niki Tagkalidou, Martalu D. Pazos et al.

Background/Objectives: Synthetic cathinones are a rapidly evolving class of new psychoactive substances whose structural diversity complicates toxicological risk assessment. Methylenedioxy cathinones occupy a pharmacological space between MDMA-like entactogens and more dopaminergic stimulant cathinones, but their direct cardiac liabilities remain poorly characterized. This study aimed to...

Evaluation of Neurotoxicity of NBOH Derivatives

Pharmaceuticals July 8, 2026 Rodrigo Foss da Silva, Lennon Machado Alves, Fernanda Conte et al.

Background/Objectives: The study sought to investigate the neurotoxicity of NBOHs, which are a class of new psychoactive substances (NPSs) that act as agonists of serotonin 5-HT2A and 5-HT2C receptors, resulting in hallucinogenic effects similar to those of LSD, often found in paper blotters. Methods: Differentiated SH-SY5Y cells were incubated for 24 h with 0.5, 1.0, 3.5, 5 and 10 nM of the...

Indole Alkaloids as Biased Opioid Receptor Modulators

Pharmaceuticals February 28, 2026 Oliver Grundmann, Allison Henderson

Background: Opioid receptors are a commonly used target for treatment of pain conditions. Most opioids used in therapy are linked to adverse effects such as tolerance, dependence, and respiratory depression. Indole alkaloids acting on opioid receptors may provide a novel molecular mechanism to confer analgesic effects. Results: Indole alkaloids such as ibogaine and mitragynine act on μ-opioid...

Ischemia-Induced Neurodegeneration in Glaucoma: Mechanistic Insights and Translational Opportunities for Psychoplastogen-Based Therapies

Pharmaceuticals February 14, 2026 Petra Dolenec, Goran Pelčić, Kristina Pilipović et al.

Glaucoma is increasingly recognized as an ischemic neurodegenerative disorder that extends beyond elevated intraocular pressure (IOP) to involve complex vascular, metabolic, and inflammatory mechanisms. Retinal ganglion cells are particularly vulnerable to ischemia-reperfusion injury, oxidative stress, and chronic neuroinflammation, leading to progressive disconnection from central visual...

Overlap and Divergence in Ketamine and Lithium Response in Bipolar Disorder: A Scoping Review

Pharmaceuticals November 3, 2025 Jay Toulany, Jasmyn E. A. Cunningham, Abraham Nunes

Background/Objectives: Lithium remains the first choice for long-term prophylaxis of mood episodes in bipolar disorder (BD), but only 30% of patients will respond, and there is no reliable method by which to predict treatment response. Ketamine is a rapid antidepressant therapy which ostensibly yields greater results in patients with clinical phenotypes that are classically associated with...

Review of Selected 2-Phenylethylamine Derivatives and Opioids, Systematic Review of Their Effects on Psychomotor Abilities and Driving Performance: Psychopharmacology in the Context of Road Safety

Pharmaceuticals October 28, 2025 Kacper Żełabowski, Kamil Biedka, Wojciech Pichowicz et al.

Background: Driving is a coordinated psychomotor activity that involves reaction time, attention, and decision-making. Psychoactive substances such as 2-phenylethylamine (PEA) derivatives and opioids may affect these functions and contribute to traffic safety. This systematic review revealed the effects of the selected PEA derivatives and opioids on psychomotor performance among drivers and...

Effects of Psilocin and Psilocybin on Human 5-HT4 Serotonin and H2 Histamine Receptors in Perfused Hearts of Transgenic Mice

Pharmaceuticals July 6, 2025 Pauline Braekow, Joachim Neumann, Uwe Kirchhefer et al.

Background/Objectives: Hallucinogenic substances such as psilocybin, psilocin, ergometrine, ergotamine, and lysergic acid diethylamide (LSD) have been demonstrated to enhance the force of contraction (FOC), in part due to the phosphorylation of phospholamban in human atrial preparations via 5-HT4 serotonin receptors and/or H2 histamine receptors. However, whether psilocybin or psilocin acts at...

Chemical Composition and Biological Activities of Psilocybe Mushrooms: Gaps and Perspectives

Pharmaceuticals July 1, 2025 Mateus Araújo Da Luz, H. Guedes, Antônio B. M. Bisneto et al. 5 citations

The Psilocybe genus is known for producing tryptamine alkaloids, specifically the compounds psilocybin and psilocin, which have shown antidepressant and anxiolytic potential. The presence of these alkaloids makes Psilocybe mushrooms promising sources of molecules with potential applications in the treatment of mental disorders. To explore this, a bibliographic study was conducted with the aim...

The Emergence of Psilocybin in Psychiatry and Neuroscience

Pharmaceuticals April 9, 2025 Hossein Omidian, Alborz Omidian 11 citations

Psilocybin, a naturally occurring psychedelic compound, has garnered renewed scientific interest for its potential in treating psychiatric and neurological disorders. This review systematically examines the latest research on psilocybin’s pharmacokinetics, pharmacodynamics, clinical efficacy, and safety profile. Emerging evidence supports its efficacy in conditions such as major depressive...

LPS-Induced Liver Inflammation Is Inhibited by Psilocybin and Eugenol in Mice

Pharmaceuticals March 23, 2025 Gregory Ian Robinson, Marta Gerasymchuk, Timur Zanikov et al. 4 citations

Background/Objectives: Liver inflammatory diseases are a major global health burden and are often exacerbated by inflammation driven by lipopolysaccharides (LPS) through toll-like receptor 4 signaling. This study evaluates the anti-inflammatory effects of psilocybin and eugenol in an LPS-induced liver inflammation model in C57BL/6J mice. Methods: Mice were treated with psilocybin (0.88 mg/kg)...

Extraction Yields of Psilocybin and Psilocin: A Short Review of Current Methods and Their Implications

Pharmaceuticals March 7, 2025 Taynah P Galdino, Lucas C Oliveira, Mateus A Luz et al. 11 citations

The growing body of evidence supporting the therapeutic efficacy of psychoactive substances, like psilocybin, has driven significant interest in recent decades due to their low toxicity and potential applications in treating various mental health disorders. However, producing pharmaceutical-grade psilocybin remains challenging, with three primary approaches: chemical synthesis, biosynthesis,...

Uncovering Psychedelics: From Neural Circuits to Therapeutic Applications

Pharmaceuticals January 19, 2025 Marco Bonaso, Letizia Biso, Benedetta Zucchini et al. 13 citations

Psychedelics, historically celebrated for their cultural and spiritual significance, have emerged as potential breakthrough therapeutic agents due to their profound effects on consciousness, emotional processing, mood, and neural plasticity. This review explores the mechanisms underlying psychedelics’ effects, focusing on their ability to modulate brain connectivity and neural circuit activity,...

Ketamine, an Old–New Drug: Uses and Abuses

Pharmaceuticals December 21, 2023 Katarina Savić Vujović, Ana Jotić, Branislava Medić et al. 32 citations

Ketamine as an old-new drug has a variety of clinical implications. In the last 30 years, ketamine has become popular for acute use in humans. Ketamine in standard doses is principally utilized for the induction and maintenance of surgical procedures. Besides its use in anesthesia and analgesia, recent studies have shown that ketamine has found a place in the treatment of asthma, epilepsy,...

Unraveling the In Vitro Toxicity Profile of Psychedelic 2C Phenethylamines and Their N-Benzylphenethylamine (NBOMe) Analogues

Pharmaceuticals August 15, 2023 Daniel Martins, Eva Gil-Martins, Fernando Cagide et al. 13 citations

Mescaline derivative (2C phenethylamines) drugs have been modified by the introduction of a N-2-methoxybenzyl group to originate a new series of compounds with recognized and potent psychedelic effects, the NBOMe-drugs. Although they are prevalent in unregulated drug markets, their toxicity profile is still poorly understood, despite several reports highlighting cases of acute intoxication,...

Efficacy of Ketamine with and without Lamotrigine in Treatment-Resistant Depression: A Preliminary Report

Pharmaceuticals August 1, 2023 Boney Joseph, Nicolas A. Nunez, Simon Kung et al. 14 citations

Intravenous (IV) ketamine and FDA-approved intranasal (IN) esketamine are increasingly used for treatment-resistant depression (TRD). Preliminary studies have suggested a synergistic effect of ketamine and lamotrigine, although the data are inconclusive. Herein, we report the response to serial ketamine/esketamine treatment among patients with TRD with or without lamotrigine therapy. In this...

Exploring the Molecular Targets for the Antidepressant and Antisuicidal Effects of Ketamine Enantiomers by Using Network Pharmacology and Molecular Docking

Pharmaceuticals July 17, 2023 Glorister A. Altê, Ana Lúcia S. Rodrigues 17 citations

Ketamine, a racemic mixture of esketamine (S-ketamine) and arketamine (R-ketamine), has received particular attention for its rapid antidepressant and antisuicidal effects. NMDA receptor inhibition has been indicated as one of the main mechanisms of action of the racemic mixture, but other pharmacological targets have also been proposed. This study aimed to explore the possible multiple targets...

Effect of Ketamine on Sleep in Treatment-Resistant Depression: A Systematic Review

Pharmaceuticals April 1, 2023 Aleksander Kwaśny, A. Włodarczyk, Damian Ogonowski et al. 27 citations

Background: Depression is a debilitating disease with a high socioeconomic burden. Regular antidepressants usually require several weeks to ameliorate symptoms; however, numerous patients do not achieve remission. What is more, sleep disturbances are one of the most common residual symptoms. Ketamine is a novel antidepressant with rapid onset of action with a proven antisuicidal effect. Little...

The Antidepressant-like Activity and Cognitive Enhancing Effects of the Combined Administration of (R)-Ketamine and LY341495 in the CUMS Model of Depression in Mice Are Related to the Modulation of Excitatory Synaptic Transmission and LTP in the PFC

Pharmaceuticals February 1, 2023 Agnieszka Pałucha-Poniewiera, B. Bobula, Anna Rafało-Ulińska

(S)-Ketamine is the first rapid-acting antidepressant drug (RAAD) introduced for the treatment of depression. However, research is still being carried out on the search for further RAADs that will be not only effective but also safe to use. Recent data have indicated that the combined administration of (R)-ketamine and the mGlu2/3 receptor antagonist LY341495 (mixRL) induces rapid and sustained...

Safety and Tolerability of the Acute Ketamine Treatment in Treatment-Resistant Depression: Focus on Comorbidities Interplay with Dissociation and Psychomimetic Symptoms

Pharmaceuticals January 24, 2023 Adam Włodarczyk, Alicja Dywel, Wiesław Jerzy Cubała 10 citations

There is evidence for ketamine use in treatment-resistant depression (TRD). Several safety concerns arise regarding adverse drug reactions in specific subpopulations. The aim of this study was to investigate the safety of intravenous ketamine treatment in relation to dissociative and psychotic measures in TRD inpatients with Major Depressive Disorder (MDD) and Bipolar depression (BP) with...

Psilocybin for Depression: From Credibility to Feasibility, What’s Missing?

Pharmaceuticals December 31, 2022 Antonio Munafò, Davide Arillotta, Guido Mannaioni et al. 15 citations

Psilocybin has been suggested as a promising transdiagnostic treatment strategy for a wide range of psychiatric disorders. Recent findings showed that psychedelic-assisted/”psycholitic” psychotherapy should provide significant and sustained alleviation of depressive symptoms. However, to date, there have been several study limitations (e.g., small sample sizes, blinding, limited follow-up,...

4-Isobutylmethcathinone—A Novel Synthetic Cathinone with High In Vitro Cytotoxicity and Strong Receptor Binding Preference of Enantiomers

Pharmaceuticals November 30, 2022 Martin Paškan, Silvie Rimpelová, Vladimíra Svobodová Pavlíčková et al. 9 citations

New psychoactive substances and among them synthetic cathinones represent a significant threat to human health globally. However, within such a large pool of substances derived from a natural compound ((S)-cathinone), substances with important pharmaceutical uses can be identified, as already documented by bupropione. Therefore, this work aimed to find a synthetic pathway for a novel synthetic...

New Paradigms of Old Psychedelics in Schizophrenia

Pharmaceuticals May 23, 2022 Danish Mahmood, Sattam Khulaif Alenezi, Md Jamir Anwar et al. 29 citations

Psychedelics such as lysergic acid diethylamide (LSD), psilocybin (magic mushrooms), and mescaline exhibit intense effects on the human brain and behaviour. In recent years, there has been a surge in studies investigating these drugs because clinical studies have shown that these once banned drugs are well tolerated and efficacious in medically supervised low doses called microdosing....

Combined Administration of (R)-Ketamine and the mGlu2/3 Receptor Antagonist LY341495 Induces Rapid and Sustained Effects in the CUMS Model of Depression via a TrkB/BDNF-Dependent Mechanism

Pharmaceuticals January 21, 2022 A. Rafało-Ulińska, P. Brański, A. Pałucha-Poniewiera

Ketamine is an effective, rapid-acting antidepressant drug (RAAD), but it induces side effects. To overcome these challenges, attempts have been made to use safer enantiomer ((R)-ketamine) or mGlu2/3 receptor antagonists, which induce ketamine-like effects and enhance its action. Here, we propose combining these two strategies to investigate the antidepressant-like effects of low doses of two...

Psilocybin, a Naturally Occurring Indoleamine Compound, Could Be Useful to Prevent Suicidal Behaviors

Pharmaceuticals November 24, 2021 Robertas Strumila, Bénédicte Nobile, Laura Korsakova et al. 35 citations

The available interventions for people who are at risk of suicide have limited efficacy. Recently, research on new mental health treatments has started to consider psychedelic compounds, particularly psilocybin, a molecule with a few thousand years of history of use in human societies. The possible effects of psilocybin on suicidal ideation and behaviors have not been specifically studied yet;...

Rediscovering Psilocybin as an Antidepressive Treatment Strategy

Pharmaceuticals September 28, 2021 René Zeiss, Maximilian Gahr, Heiko Graf 17 citations

There has recently been a renewal of interest in psychedelic research on the use of psilocybin in psychiatric treatment and, in particular, for the treatment of major depressive disorder (MDD). Several state-of-the-art studies have provided new insight into the mechanisms of action of psilocybin and its therapeutic potential. Nevertheless, many questions remain unanswered. With this review, we...