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The International Journal of Neuropsychopharmacology

ISSN 1461-1457

86 papers in the library · 4,809 citations · publishing 2003-2026

Papers

Differential long-term effects of MDMA on the serotoninergic system and hippocampal cell proliferation in 5-HTT knock-out vs. wild-type mice

The International Journal of Neuropsychopharmacology July 9, 2008 Thibault Renoir, Eleni Païzanis, Malika El Yacoubi et al. 58 citations

A single sentence summary is not possible because the abstract contains multiple distinct findings. Four weeks after administering MDMA to mice, the potency of a 5-HT1A receptor agonist to inhibit serotonin neuron firing in the dorsal raphe nucleus doubled, and the hypothermic response to 8-OH-DPAT increased, indicating supersensitivity of 5-HT1A autoreceptors. Brain serotonin levels decreased without changes in citalopram binding. MDMA treatment also reduced hippocampal cell proliferation by 30% and increased immobility in the forced swim test, suggesting depressive-like behavior. These effects were absent in mice lacking the serotonin transporter, indicating the transporter is required for these delayed, antidepressant-opposite effects that may contribute to MDMA-induced mood disorders.

Psychedelics and Consciousness: Distinctions, Demarcations, and Opportunities

The International Journal of Neuropsychopharmacology May 10, 2021 Natalie Gukasyan, David B. Yaden, Matthew W. Johnson et al. 56 citations

Psychedelic substances produce unusual changes in conscious experience, leading some to propose they offer unique insights into consciousness. However, psychedelics are unlikely to provide information relevant to the "hard problem of consciousness," which involves explaining how first-person experience emerges. Instead, they bear on multiple "easy problems of consciousness," involving relations between subjectivity, brain function, and behavior. This review discusses common meanings of "consciousness" regarding psychedelics and considers models of their effects on the brain linked to explanatory claims about consciousness. It calls for epistemic humility about psychedelic research's potential to explain the hard problem while noting ways psychedelics may advance study of specific aspects of consciousness.

(R)-Ketamine Rapidly Ameliorates the Decreased Spine Density in the Medial Prefrontal Cortex and Hippocampus of Susceptible Mice After Chronic Social Defeat Stress

The International Journal of Neuropsychopharmacology August 28, 2019 Jiancheng Zhang, Youge Qu, Lijia Chang et al. 56 citations

A single injection of (R)-ketamine (10 mg/kg) rapidly reversed the loss of dendritic spines in the medial prefrontal cortex and hippocampus of mice that had become susceptible after chronic social defeat stress. Spine density was measured three hours after treatment and was significantly increased in the prelimbic area of the medial prefrontal cortex, the Cornu Ammonis3 region, and the dentate gyrus of the hippocampus. The findings suggest that (R)-ketamine's rapid restoration of spine density in these brain regions may underlie its fast-acting antidepressant effects.

Ketamine’s Antidepressant Efficacy is Extended for at Least Four Weeks in Subjects with a Family History of an Alcohol Use Disorder

The International Journal of Neuropsychopharmacology December 19, 2014 Mark J. Niciu, David A. Luckenbaugh, Dawn F. Ionescu et al. 55 citations

A single low-dose infusion of the anesthetic ketamine produces rapid antidepressant effects in people with treatment-resistant major depressive disorder. In this trial, depressed individuals with a family history of alcohol use disorder showed a longer-lasting antidepressant response to ketamine compared to those without such a family history. Adding the drug riluzole did not extend or enhance ketamine's antidepressant durability. The findings suggest that family history of alcohol use disorder may predict a more durable ketamine response, which should be accounted for in future ketamine depression studies.

Drug seeking in response to a priming injection of MDMA in rats: relationship to initial sensitivity to self-administered MDMA and dorsal striatal dopamine

The International Journal of Neuropsychopharmacology March 25, 2010 Joyce Colussi‐mas, Richard J. Wise, Alex Howard et al. 51 citations

In rats that learned to self-administer MDMA, a later injection of the drug triggered renewed drug-seeking behavior. The strength of this drug seeking was greater in rats that had acquired self-administration more quickly and in those that showed larger MDMA-induced increases in dopamine in the dorsal striatum. Rats that never learned to self-administer MDMA or that received the drug passively did not show this effect. The findings suggest that individual differences in initial sensitivity to MDMA's reinforcing effects and in the drug's ability to elevate striatal dopamine influence the propensity to seek the drug after a period of abstinence.

Cannabinoid Modulation of Amygdala Subregion Functional Connectivity to Social Signals of Threat

The International Journal of Neuropsychopharmacology December 28, 2014 Stephanie M. Gorka, Daniel A. Fitzgerald, Harriet de Wit et al. 43 citations

Δ(9)-Tetrahydrocannabinol (THC) enhances functional connectivity between specific amygdala subregions (basolateral and superficial) and the rostral anterior cingulate/medial prefrontal cortex during social threat processing in healthy adults. This effect may help reduce threat perception or improve socio-emotional regulation, shedding light on the neurocircuitry underlying affective processes. The findings come from a double-blind, placebo-controlled, within-subjects study with 16 participants using functional magnetic resonance imaging.

Comparative Effects of Methylphenidate, Modafinil, and MDMA on Response Inhibition Neural Networks in Healthy Subjects

The International Journal of Neuropsychopharmacology May 16, 2017 André Schmidt, Felix Müller, Patrick C. Dolder et al. 41 citations

Methylphenidate and modafinil, but not MDMA (ecstasy), improved the ability to stop a motor response in healthy adults. Using brain imaging, methylphenidate broadly activated frontal, temporal, and parietal regions, including the anterior cingulate cortex and presupplementary motor area, more than modafinil did. Modafinil increased activation in the right middle frontal gyrus and parietal lobule, while MDMA activated the right middle/inferior frontal gyrus and superior parietal lobule without improving performance. The findings suggest that methylphenidate may be superior to modafinil and MDMA for enhancing cognitive performance related to response inhibition in healthy people.

Effects of Chronic Exposure to Low-Dose delta-9-Tetrahydrocannabinol in Adolescence and Adulthood on Serotonin/Norepinephrine Neurotransmission and Emotional Behavior

The International Journal of Neuropsychopharmacology July 23, 2020 Danilo de Gregorio, Joshua Dean Conway, Martha-Lopez Canul et al. 39 citations

Chronic exposure to a low dose of THC (1 mg/kg) during adolescence in rats leads to depressive-like behaviors (increased immobility in the forced swim test and anhedonia in the sucrose preference test) and anxiety-like behavior (fewer open-arm entries in the elevated plus maze). Adult exposure also produces anxiety but not depressive-like behaviors. Both adolescent and adult THC exposure reduce the activity of serotonin neurons in the dorsal raphe, while noradrenergic neurons in the locus coeruleus remain unaffected. These findings suggest that the serotonin system is vulnerable to chronic low-dose THC, and that adolescents are particularly susceptible to THC-induced depressive effects.

Involvement of 5-HT2A receptors in MDMA reinforcement and cue-induced reinstatement of MDMA-seeking behaviour

The International Journal of Neuropsychopharmacology October 14, 2010 María Juliana Orejarena, Laurence Lanfumey, Rafaël Maldonado et al. 38 citations

The serotonin 5-HT2A receptor plays a crucial role in the reinforcing and addictive properties of MDMA. In experiments with mice, those lacking the 5-HT2A receptor showed reduced self-administration of MDMA at both 0.125 and 0.25 mg/kg per infusion compared to normal mice. MDMA increased horizontal locomotion more in the knockout mice than in normal mice. Dopamine release in the nucleus accumbens was lower in knockout mice both at baseline and after MDMA challenge. Cue-induced reinstatement of MDMA-seeking behavior was blocked by a selective 5-HT2A receptor antagonist at 0.5 mg/kg. These findings suggest that 5-HT2A receptors are essential for MDMA's reinforcing effects and for relapse triggered by drug-associated cues, likely through modulation of dopamine activity in the brain's reward pathway.

Naltrexone but Not Ketanserin Antagonizes the Subjective, Cardiovascular, and Neuroendocrine Effects of Salvinorin-A in Humans

The International Journal of Neuropsychopharmacology February 12, 2016 Marta Valle, Montserrat Puntes, Jimena Coimbra et al. 31 citations

Salvinorin-A, a terpene from the plant Salvia divinorum, induces an intense but short-lasting altered state of awareness similar to classical psychedelics, but it acts on kappa-opioid receptors rather than serotonin-2A receptors. In a double-blind, placebo-controlled study with 24 healthy volunteers experienced with psychedelics, inhalation of 1 mg of vaporized salvinorin-A severely reduced external sensory perception, caused intense visual and auditory modifications, and increased systolic blood pressure, cortisol, and prolactin. These effects were effectively blocked by the opioid antagonist naltrexone (50 mg orally) but not by the serotonin-2A antagonist ketanserin (40 mg orally), confirming that salvinorin-A's mechanism involves kappa-opioid receptor agonism and not serotonin-2A agonism.

Long-lasting alterations in 5-HT2A receptor after a binge regimen of methamphetamine in mice

The International Journal of Neuropsychopharmacology April 24, 2014 Hong‐yi Chiu, Ming‐huan Chan, Mei-Yi Lee et al. 31 citations

A single-day 'binge' dosing regimen of methamphetamine in male mice impaired recognition memory, reduced social behaviors, and increased sensitivity to a hallucinogenic drug that activates serotonin 5-HT2A receptors. The heightened behavioral, molecular, and electrophysiological responses to the hallucinogen were linked to an up-regulation of 5-HT2A receptors in the medial prefrontal cortex, while 5-HT2C and 5-HT1A receptors remained unchanged. These findings suggest that methamphetamine-induced changes in 5-HT2A receptor expression may contribute to psychosis-like behaviors and could inform therapies for methamphetamine-related psychiatric disorders.

Preclinical models of antipsychotic drug action

The International Journal of Neuropsychopharmacology June 10, 2013 José L. Moreno, Javier González‐maeso 30 citations

Psychedelic drugs like LSD and dissociative drugs like PCP produce psychotic and cognitive symptoms in healthy people that resemble aspects of schizophrenia. Serotonin 5-HT2A and metabotropic glutamate 2 receptors are involved in how these drugs work. This review examines recent studies using LSD-like and PCP-like drugs in rodents that link these receptors to the biology of schizophrenia and its treatment.

A Complex Impact of Systemically Administered 5-HT2A Receptor Ligands on Conditioned Fear

The International Journal of Neuropsychopharmacology July 5, 2021 Sven Melker Hagsäter, Robert Pettersson, Christopher Pettersson et al. 29 citations

Activating the 5-HT2A serotonin receptor with drugs such as psilocybin reduces conditioned fear in male rats, an effect blocked by a 5-HT2A inverse agonist. Inverse agonists alone did not change fear behavior, but they unmasked a fear-reducing effect of the SSRI escitalopram, which by itself had no effect. These results suggest that 5-HT2A receptor activation is not required for normal conditioned freezing but can dampen fear when over-activated. In the presence of an SSRI, the 5-HT2A receptor appears to oppose the anti-freezing effect of increased serotonin levels.

Ethanol increases the distribution of MDMA to the rat brain: possible implications in the ethanol-induced potentiation of the psychostimulant effects of MDMA

The International Journal of Neuropsychopharmacology December 2, 2008 Sami Ben Hamida, A. Tracqui, Anne Pereira de Vasconcelos et al. 27 citations

Taking the club drug ecstasy (MDMA) together with alcohol (ethanol) increases the drug's levels in the blood and brain, which may explain why alcohol amplifies MDMA's stimulant effects. In rats, alcohol raised MDMA concentrations in the blood, hippocampus, frontal cortex, and striatum within 15 to 60 minutes after injection, without changing the proportion converted to its active metabolite MDA. MDMA and MDA accumulated more in the striatum and cortex than in the hippocampus. These higher brain and blood levels suggest that combining alcohol with MDMA could increase the risk of neurotoxicity and potential for abuse.

Acute and long-term effects of a single dose of MDMA on aggression in Dark Agouti rats

The International Journal of Neuropsychopharmacology August 1, 2005 Eszter Kirilly, Anita Benkő, Linda Ferrington et al. 26 citations

A single dose of MDMA (15 mg/kg) in male Dark Agouti rats caused lasting damage to the serotonin system, shown by 30–60% reductions in paroxetine binding in the forebrain and decreased brain glucose metabolism in aggression-related areas. Despite this neurotoxicity, aggressive behaviors (biting, boxing, wrestling) were not significantly different from controls three weeks later, and the acute anti-aggressive effects of MDMA and two 5-HT1B receptor agonists remained intact. The findings suggest that aggressive behavior and the acute anti-aggressive action of MDMA are preserved even with substantial serotonergic damage, at least under the social isolation conditions of the resident-intruder test.

Acute Effects of Methylphenidate, Modafinil, and MDMA on Negative Emotion Processing

The International Journal of Neuropsychopharmacology November 22, 2017 André Schmidt, Felix Müller, Patrick C. Dolder et al. 25 citations

Modafinil, but not methylphenidate or MDMA, increased brain activity in a limbic-cortical-striatal-pallidal-thalamic circuit and the amygdala when healthy subjects viewed fearful faces. Activation in frontal brain regions correlated with increased feelings of fearfulness and depressiveness after modafinil. Despite modafinil's cognitive enhancement effects, potential adverse effects on emotion processing should be considered.

Cognitive impairments from developmental exposure to serotonergic drugs: citalopram and MDMA

The International Journal of Neuropsychopharmacology January 11, 2013 Tori L. Schaefer, Curtis E. Grace, A Braun et al. 24 citations

In rats, treatment with the recreational drug MDMA during a developmental period equivalent to the human third trimester causes long-term spatial and egocentric learning and memory deficits, along with serotonin reductions. Pretreatment with the antidepressant citalopram, a selective serotonin reuptake inhibitor, did not prevent these cognitive deficits. Unexpectedly, citalopram alone produced learning deficits as severe as those caused by MDMA. These are the first findings showing cognitive impairments from developmental exposure to a selective serotonin reuptake inhibitor, suggesting the need for further research on the long-term safety of antidepressants during pregnancy.

Predicting Antidepressant Effects of Ketamine: the Role of the Pregenual Anterior Cingulate Cortex as a Multimodal Neuroimaging Biomarker

The International Journal of Neuropsychopharmacology August 10, 2022 Anne Weigand, Matti Gärtner, Milan Scheidegger et al. 22 citations

Activity in the pregenual anterior cingulate cortex (pgACC) during emotional stimulation can predict how well a single intravenous infusion of ketamine will relieve depression symptoms in people with major depressive disorder. In 24 patients, pgACC activity was linked to an increase in glutamate in the same brain region 24 hours after the infusion, and this glutamate increase was associated with greater symptom improvement. The findings suggest pgACC activity may serve as a neuroimaging biomarker for early treatment response to ketamine.

5-HT2A Agonists: A Novel Therapy for Functional Neurological Disorders?

The International Journal of Neuropsychopharmacology February 8, 2017 Alexander Bryson, Olivia Carter, Trevor R. Norman et al. 19 citations

Functional neurological disorders are common, have poor outcomes, and few treatments exist. Their cause is unknown, but leading theories suggest a disturbance in how the mind represents the body, with abnormal top-down cognitive influences on sensorimotor function despite intact neural pathways. Recent studies indicate that 5-HT2A agonists, such as psychedelics, alter brain activity in ways that disrupt hierarchical dynamics and modulate networks involved in self-processing. Converging evidence suggests these agents may hold unique therapeutic potential for these disorders. Given the personal and societal burden, the authors argue a clinical trial to test this hypothesis is warranted.

In abstinent MDMA users the cortisol awakening response is off-set but associated with prefrontal serotonin transporter binding as in non-users

The International Journal of Neuropsychopharmacology February 14, 2014 Vibe G. Frøkjær, David Erritzøe, Klaus K. Holst et al. 19 citations

Prefrontal serotonin transporter binding is positively associated with the cortisol awakening response, a measure of hypothalamic-pituitary-adrenal-axis output, in both MDMA users and non-users. MDMA users showed a significantly higher cortisol awakening response than non-users. The findings suggest that the inhibitory control on HPA-axis output is less efficient after recent MDMA use, likely through mechanisms beyond those compensated by reduced serotonin transporter levels.

Psychedelics for the Treatment of Obsessive–Compulsive Disorder: Efficacy and Proposed Mechanisms

The International Journal of Neuropsychopharmacology November 29, 2024 Helen M Collins 18 citations

Psychedelics are being investigated as treatments for several mental health conditions, including obsessive–compulsive disorder (OCD). Since the 1960s, case studies have reported improvements in obsessive and compulsive behaviors after recreational psychedelic use. A small 2006 open-label trial found that psilocybin significantly reduced OCD symptoms, and rodent models show reduced compulsive behaviors after psilocybin. However, the mechanisms remain unclear, with hypotheses involving acute pharmacological effects, neuroplasticity changes, and altered resting state neural networks. This review evaluates evidence for psychedelics in OCD treatment, discusses mechanisms, and notes ongoing trials addressing current knowledge gaps.

Enhancing action of LSD on neuronal responsiveness to serotonin in a brain structure involved in obsessive–compulsive disorder

The International Journal of Neuropsychopharmacology March 1, 2003 Tarek Zghoul, Pierre Blier 13 citations

LSD enhances the inhibitory effect of serotonin on neurons in the orbitofrontal cortex, a brain region linked to obsessive-compulsive disorder (OCD), while reducing serotonin's inhibitory effect in the hippocampus, a region linked to depression. In rats under anesthesia, LSD applied directly to neurons decreased their firing rate and boosted serotonin's inhibitory action in the orbitofrontal cortex, but weakened it in the hippocampus. After four daily injections of LSD, the same pattern persisted 24 hours after the last dose, suggesting a lasting change in serotonin responsiveness. This enhancement in the orbitofrontal cortex may explain why some hallucinogens have anti-OCD effects that outlast their psychotomimetic action.

Psilocybin Therapy of Psychiatric Disorders Is Not Hampered by hERG Potassium Channel–Mediated Cardiotoxicity

The International Journal of Neuropsychopharmacology December 3, 2021 Benjamin Hackl, Hannes Todt, Helmut Kubista et al. 11 citations

Psilocybin, the hallucinogen in magic mushrooms, is being studied for psychiatric disorders, but safety concerns arose after reports of cardiac events and QT interval prolongation linked to its metabolite psilocin. Clinical concentrations of psilocin do not significantly inhibit the hERG potassium channel, a key risk factor for adverse cardiac effects. Therefore, hERG channel blockage by psilocin is not responsible for psilocybin-associated cardiotoxicity.

PM506. Psilocybin Clinical Trial: Acute Effects and its relationship to the brain activity as measured by quantitative EEG

The International Journal of Neuropsychopharmacology May 27, 2016 Filip Tylš, Michaela Viktorinová, Dominika Prokopcova et al. 10 citations

Among first-episode, drug-naive Han Chinese patients with schizophrenia, 24.5% had impaired glucose tolerance, compared to none of the healthy controls. Patients also had higher fasting and two-hour glucose levels, greater insulin resistance, and higher waist circumference, BMI, and triglycerides. Those with impaired glucose tolerance were older, had later schizophrenia onset, and scored higher on total and negative symptom scales, but showed no greater cognitive impairment except on an emotional intelligence measure. Abnormal glucose metabolism may be linked to clinical symptoms but not cognitive impairment in early schizophrenia.

Role of endogenous serotonin in psychedelic-like effects of psilocybin in mice

The International Journal of Neuropsychopharmacology May 25, 2025 Ines Erkizia-Santamaría, Nerea Martínez-Álvarez, Leyre Salinas-Novoa et al. 7 citations

The intensity of acute psychedelic effects from psilocybin is inversely related to cortical serotonin levels. In mice, the head-twitch response—a behavioral measure of psychedelic-like effects—was lower in animals lacking the serotonin 2A receptor and was dose-dependently reduced by the antidepressant citalopram, which increases synaptic serotonin. Conversely, depleting serotonin with p-chlorophenylalanine potentiated the response. A serotonin 1A receptor agonist also decreased the response, indicating functional interaction between receptor types. These findings suggest that prior antidepressant treatment may influence individual variability in acute responses to psilocybin, with implications for optimizing psychedelic-based therapies.