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Frontiers in Pharmacology

ISSN 1663-9812

134 papers in the library · 5,329 citations · publishing 2013-2026

Papers

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Unveiling behavioral and molecular neuroadaptations related to the antidepressant action of cannabidiol in the unpredictable chronic mild stress model

Frontiers in Pharmacology April 18, 2023 María Salud García-Gutiérrez, Daniela Navarro, Amaya Austrich-Olivares et al.

Introduction: This study aims to further characterize cannabidiol’s pharmacological and molecular profile as an antidepressant.Methods: Effects of cannabidiol (CBD), alone or combined with sertraline (STR), were evaluated in male CD1 mice (n = 48) exposed to an unpredictable chronic mild stress (UCMS) procedure. Once the model was established (4 weeks), mice received CBD (20 mg·kg-1, i.p.), STR...

Deletion of Cryab increases the vulnerability of mice to the addiction-like effects of the cannabinoid JWH-018 via upregulation of striatal NF-κB expression

Frontiers in Pharmacology March 16, 2023 Leandro Val Sayson, Darlene Mae Ortiz, Hyun Jun Lee et al. 4 citations

Synthetic cannabinoids have exhibited unpredictable abuse liabilities, especially self-administration (SA) responses in normal rodent models, despite seemingly inducing addiction-like effects in humans. Thus, an efficient pre-clinical model must be developed to determine cannabinoid abuse potential in animals and describe the mechanism that may mediate cannabinoid sensitivity. The Cryab...

Pharmacological effects of methylone and MDMA in humans

Frontiers in Pharmacology February 17, 2023 Lourdes Poyatos, Clara Pérez‐mañá, Olga Hladun et al. 26 citations

Methylone is one of the most common synthetic cathinones popularized as a substitute for 3,4-methylenedioxymethamphetamine (MDMA, midomafetamine) owing to its similar effects among users. Both psychostimulants exhibit similar chemistry (i.e., methylone is a β-keto analog of MDMA) and mechanisms of action. Currently, the pharmacology of methylone remains scarcely explored in humans. Herein, we...

Rearing behaviour in the mouse behavioural pattern monitor distinguishes the effects of psychedelics from those of lisuride and TBG

Frontiers in Pharmacology February 16, 2023 Yahong Chen, Junhong Liu, Yishan Yao et al. 19 citations

Psychedelics alter consciousness and may have potential for drug development. As psychedelics are likely therapeutically active, it is important to study their effects and mechanisms using preclinical models. Here, we examined the effects of phenylalkylamine and indoleamine psychedelics on locomotor activity and exploratory behaviour using the mouse Behavioural Pattern Monitor (BPM). DOM,...

Psilocybin sex-dependently reduces alcohol consumption in C57BL/6J mice

Frontiers in Pharmacology January 4, 2023 Kenneth Alper, Janelle Cange, Ria Sah et al. 39 citations

The classical psychedelic psilocybin is of interest as a treatment for alcohol use disorder (AUD). This study investigated the effects of psilocybin on voluntary ethanol consumption in adult male and female C57BL/6J mice administered saline or psilocybin intraperitoneally as a single dose of 0.1, 0.5, 1.0 or 2.0 mg/kg and provided 20% ethanol utilizing a two-bottle choice alcohol drinking...

Overcoming the clinical challenges of traditional ayahuasca: a first-in-human trial exploring novel routes of administration of N,N-Dimethyltryptamine and harmine.

Frontiers in Pharmacology 2023 Dario Dornbierer, Laurenz Marten, Jovin Mueller et al. 32 citations

Recently, the Amazonian plant medicine "ayahuasca"-containing the psychedelic compound N,N-dimethyltryptamine (DMT) and numerous β-carboline alkaloids, such as harmine-has been suggested to exhibit beneficial effects in patients with affective and other mental health disorders. Although ayahuasca ingestion is considered safe, its pharmacokinetics/pharmacodynamics and tolerability profile pose...

A pilot study of cerebral metabolism and serotonin 5-HT2A receptor occupancy in rats treated with the psychedelic tryptamine DMT in conjunction with the MAO inhibitor harmine.

Frontiers in Pharmacology 2023 Klemens Egger, Frederik Gudmundsen, Naja Støckel Jessen et al. 17 citations

Rationale: The psychedelic effects of the traditional Amazonian botanical decoction known as ayahuasca are often attributed to agonism at brain serotonin 5-HT2A receptors by N,N-dimethyltryptamine (DMT). To reduce first pass metabolism of oral DMT, ayahuasca preparations additionally contain reversible monoamine oxidase A (MAO-A) inhibitors, namely β-carboline alkaloids such as harmine....

μ-opioid receptor agonists and psychedelics: pharmacological opportunities and challenges.

Frontiers in Pharmacology 2023 Leah M Salinsky, Christina R Merritt, Joshua C Zamora et al. 14 citations

Opioid misuse and opioid-involved overdose deaths are a massive public health problem involving the intertwined misuse of prescription opioids for pain management with the emergence of extremely potent fentanyl derivatives, sold as standalone products or adulterants in counterfeit prescription opioids or heroin. The incidence of repeated opioid overdose events indicates a problematic use...

Binding and functional structure-activity similarities of 4-substituted 2,5-dimethoxyphenyl isopropylamine analogues at 5-HT2A and 5-HT2B serotonin receptors.

Frontiers in Pharmacology 2023 Prithvi Hemanth, Pallavi Nistala, Vy T Nguyen et al. 4 citations

Certain 4-substituted analogs of 1-(2,5-dimethoxyphenyl)isopropylamine (2,5-DMA) are psychoactive classical hallucinogens or serotonergic psychedelic agents that function as human 5-HT2A (h5-HT2A) serotonin receptor agonists. Activation of a related receptor population, h5-HT2B receptors, has been demonstrated to result in adverse effects including cardiac valvulopathy. We previously published...

Acute pharmacological profile of 2C-B-Fly-NBOMe in male Wistar rats-pharmacokinetics, effects on behaviour and thermoregulation.

Frontiers in Pharmacology 2023 Kateřina Syrová, Klára Šíchová, Hynek Danda et al. 4 citations

Introduction: N-2-methoxy-benzylated ("NBOMe") analogues of phenethylamine are a group of new psychoactive substances (NPS) with reported strong psychedelic effects in sub-milligram doses linked to a number of severe intoxications, including fatal ones. In our present work, we provide a detailed investigation of pharmacokinetics and acute behavioural effects of 2C-B-Fly-NBOMe...

Corrigendum: Three naturally-occurring psychedelics and their significance in the treatment of mental health disorders.

Frontiers in Pharmacology 2023 Nataliya S. Vorobyeva, Alena A. Kozlova 1 citation correction

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The treatment of depression — searching for new ideas

Frontiers in Pharmacology October 7, 2022 Katarzyna Stachowicz, Magdalena Sowa-Kućma 48 citations

Depression is a severe mental health problem that affects people regardless of social status or education, is associated with changes in mood and behavior, and can result in a suicide attempt. Therapy of depressive disorders is based mainly on drugs discovered in the 1960s and early 1970s. Selective serotonin reuptake inhibitors (SSRIs) and serotonin-norepinephrine reuptake inhibitors (SNRIs)...

Editorial: Psychedelic sociality: Pharmacological and extrapharmacological perspectives

Frontiers in Pharmacology July 22, 2022 Leor Roseman, Katrin H. Preller, Evgenia Fotiou et al. 15 citations

The heralded psychedelic renaissance is currently at a new level where psychedelics are being accepted by the scientific community and the public. Medicalization and the ongoing introduction of market forces are imposing a trend in which psychedelic treatments are reduced to focus into strictly pharmacological and psychological effects on the self, rather than interactions with broader social...

Effects of 3,4-Methylenedioxymethamphetamine on Conditioned Fear Extinction and Retention in a Crossover Study in Healthy Subjects

Frontiers in Pharmacology July 13, 2022 Patrick Vizeli, Isabelle Straumann, Urs Duthaler et al. 43 citations

Background: 3,4-Methylenedioxymethamphetamine (MDMA) has shown initial promise as an adjunct in psychotherapy to treat posttraumatic stress disorder (PTSD). Its efficacy and safety have been demonstrated across phase I–III studies. However, the mechanism underlying the potential utility of MDMA to treat PTSD in humans has not yet been thoroughly investigated. Preliminary evidence suggests that...

Uncovering the Underlying Mechanisms of Ketamine as a Novel Antidepressant

Frontiers in Pharmacology July 7, 2022 Songbai Xu, Xiaoxiao Yao, Bingjin Li et al. 50 citations

Major depressive disorder (MDD) is a devastating psychiatric disorder which exacts enormous personal and social-economic burdens. Ketamine, an N-methyl-D-aspartate receptor (NMDAR) antagonist, has been discovered to exert rapid and sustained antidepressant-like actions on MDD patients and animal models. However, the dissociation and psychotomimetic propensities of ketamine have limited its use...

Three Naturally-Occurring Psychedelics and Their Significance in the Treatment of Mental Health Disorders

Frontiers in Pharmacology June 28, 2022 Nataliya S. Vorobyeva, Alena A. Kozlova 16 citations

Classical psychedelics represent a family of psychoactive substances with structural similarities to serotonin and affinity for serotonin receptors. A growing number of studies have found that psychedelics can be effective in treating various psychiatric conditions, including post-traumatic stress disorder, major depressive disorder, anxiety, and substance use disorders. Mental health disorders...

Psychedelic Therapies at the Crossroads of Trauma and Substance Use: Historical Perspectives and Future Directions, Taking a Lead From New Mexico

Frontiers in Pharmacology June 27, 2022 Snehal Bhatt, Maya Armstrong, Tassy Parker et al. 4 citations

Post-traumatic stress disorder (PTSD), a common condition with potentially devastating individual, family, and societal consequences, is highly associated with substance use disorders (SUDs). The association between PTSD and SUD is complex and may involve adverse childhood experiences (ACEs), historical and multi-generational traumas, and social determinants of health as well as cultural and...

Monoamine Oxidase Inhibition by Plant-Derived β-Carbolines; Implications for the Psychopharmacology of Tobacco and Ayahuasca

Frontiers in Pharmacology May 2, 2022 Ilana Berlowitz, Klemens Egger, Paul Cumming 32 citations

The monoamine oxidases (MAOs) are flavin-containing amine oxidoreductases responsible for metabolism of many biogenic amine molecules in the brain and peripheral tissues. Whereas serotonin is the preferred substrate of MAO-A, phenylethylamine is metabolized by MAO-B, and dopamine and tyramine are nearly ambivalent with respect to the two isozymes. β-Carboline alkaloids such as harmine,...

Therapeutic Alliance and Rapport Modulate Responses to Psilocybin Assisted Therapy for Depression

Frontiers in Pharmacology March 31, 2022 Roberta Murphy, Roberta Murphy, Hannes Kettner et al. 229 citations

Background: Across psychotherapeutic frameworks, the strength of the therapeutic alliance has been found to correlate with treatment outcomes; however, its role has never been formally assessed in a trial of psychedelic-assisted therapy. We aimed to investigate the relationships between therapeutic alliance and rapport, the quality of the acute psychedelic experience and treatment outcomes....

Language as a Window Into the Altered State of Consciousness Elicited by Psychedelic Drugs

Frontiers in Pharmacology March 22, 2022 Enzo Tagliazucchi 20 citations

Psychedelics are drugs capable of eliciting profound alterations in the subjective experience of the users, sometimes with long-lasting consequences. Because of this, psychedelic research tends to focus on human subjects, given their capacity to construct detailed narratives about the contents of their consciousness experiences. In spite of its relevance, the interaction between serotonergic...

Psilocybin-Induced Mystical-Type Experiences are Related to Persisting Positive Effects: A Quantitative and Qualitative Report

Frontiers in Pharmacology March 9, 2022 Drummond E-Wen Mcculloch, Maria Zofia Grzywacz, Martin Bruun Madsen et al. 91 citations

Psychedelic drugs such as psilocybin have shown substantial promise for the treatment of several psychiatric conditions including mood and addictive disorders. They also have the remarkable property of producing persisting positive psychological changes in healthy volunteers for at least several months. In this study (NCT03289949), 35 medium-high doses of psilocybin were administered to 28...

Receptor Interaction Profiles of 4-Alkoxy-3,5-Dimethoxy-Phenethylamines (Mescaline Derivatives) and Related Amphetamines

Frontiers in Pharmacology February 9, 2022 Karolina E. Kolaczynska, Dino Luethi, Dino Luethi et al. 16 citations

3,4,5-Trimethoxyphenethylamine (mescaline) is a psychedelic alkaloid found in peyote cactus. Related 4-alkoxy-3,5-dimethoxy-substituted phenethylamines (scalines) and amphetamines (3C-scalines) are reported to induce similarly potent psychedelic effects and are therefore potential novel therapeutics for psychedelic-assisted therapy. Herein, several pharmacologically uninvestigated scalines and...

Evaluating the Potential Use of Serotonergic Psychedelics in Autism Spectrum Disorder

Frontiers in Pharmacology January 27, 2022 Athanasios Markopoulos, Antonio Inserra, Danilo de Gregorio et al. 44 citations

Recent clinical and preclinical evidence points towards empathogenic and prosocial effects elicited by psychedelic compounds, notably the serotonin 5-HT 2A agonists lysergic acid diethylamide (LSD), psilocybin, N,N-Dimethyltryptamine (DMT), and their derivatives. These findings suggest a therapeutic potential of psychedelic compounds for some of the behavioural traits associated with autism...

Changes in mental health, wellbeing and personality following ayahuasca consumption: Results of a naturalistic longitudinal study.

Frontiers in Pharmacology 2022 Daniel Perkins, Broc A. Pagni, Jerome Sarris et al. 53 citations

Background: Naturalistic and placebo-controlled studies suggest ayahuasca, a potent psychedelic beverage originating from Indigenous Amazonian tradition, may improve mental health, alter personality structure, and reduce alcohol and drug intake. To better understand ayahuasca's therapeutic potential and to identify factors that influence therapeutic efficacy, we conducted a naturalistic,...

Drug Transporters ABCB1 (P-gp) and OATP, but not Drug-Metabolizing Enzyme CYP3A4, Affect the Pharmacokinetics of the Psychoactive Alkaloid Ibogaine and its Metabolites.

Frontiers in Pharmacology 2022 Margarida L F Martins, Paniz Heydari, Wenlong Li et al. 9 citations

The psychedelic alkaloid ibogaine is increasingly used as an oral treatment for substance use disorders, despite being unlicensed in most countries and having reported adverse events. Using wild-type and genetically modified mice, we investigated the impact of mouse (m)Abcb1a/1b and Abcg2 drug efflux transporters, human and mouse OATP drug uptake transporters, and the CYP3A drug-metabolizing...