Pharmacological reports : PR - The Consciousness Library

The Sigma1 receptor antagonist CM304 potentiates the antinociceptive effects of the cannabinoid receptor agonist delta9-tetrahydrocannabinol in rats and mice.

Pharmacological reports : PR April 1, 2026 Elmira Zolali, Mallory Burns, Sebastiano Intagliata et al.

BACKGROUND: Mu opioid receptor (MOR) agonists are the primary medication class used to treat moderate to severe pain; however, the ongoing opioid overdose crisis underscores the need for alternatives to MOR agonists for pain treatment. Delta9-tetrahydrocannabinol (THC), a cannabinoid CB1 receptor (CB1R) agonist, and sigma1 receptor (σ1R) antagonists elicit antinociceptive effects albeit less...

DOI: 10.1007/s43440-026-00834-w Full text Antinociception Cm304 Cannabinoid Drug discrimination +1

The effect of psilocin on neurotransmitters release in the claustrum and on rat behavior.

Pharmacological reports : PR February 1, 2026 Zuzanna Kościuk, Izabela Szpręgiel, Agnieszka Bysiek et al. 2 citations

The claustrum, a subcortical structure densely expressing 5-hydroxytryptamine 2 A (5-HT2A) receptors, has been implicated in sensory integration, emotional regulation, salience, and attention. Despite its hypothesized involvement in the effects of serotonergic psychedelics, the neurochemical impact of these substances on claustral neurotransmission remains unexplored. This study aimed to...

DOI: 10.1007/s43440-025-00817-3 Full text Psilocin 25i-nbome Claustrum Microdialysis +1

A preliminary proof-of-concept trial on the effects of ketamine on fatigue: a randomized crossover trial.

Pharmacological reports : PR January 22, 2026 Taichi Goto, Joy D Kreskow, Alexander L R Ross et al.

Fatigue, a prevalent symptom of chronic illness, impacts quality of life. This proof-of-concept, randomized, double-blind, crossover trial assessed the anti-fatigue effects of ketamine (0.5 mg/kg) versus midazolam (0.045 mg/kg), the active comparator. Ten participants, who were cancer survivors, with fibromyalgia, myalgic encephalomyelitis/chronic fatigue syndrome, or systemic lupus...

DOI: 10.1007/s43440-025-00808-4 Full text Active placebo Chronic illness Glutamate receptor Midazolam +1

The phenomenology of psilocybin's experience mediates subsequent persistent psychological effects independently of sex, previous experience, or setting.

Pharmacological reports : PR June 16, 2025 Tereza Klučková, Marek Nikolič, Filip Tylš et al. 4 citations

Recent studies intensively explore psilocybin's antidepressant potential, but variables like previous experience, repeated use, setting, and sex remain underexplored. This study examines acute and long-term effects of psilocybin in healthy individuals. A double-blind, placebo-controlled, cross-over study included 40 healthy participants (20 females, mean age 38). Each received two doses of...

DOI: 10.1007/s43440-025-00742-5 Full text Healthy population Previous experience Repeated administration Sex +7

Non-response to short-term ketamine use for treatment-resistant depression.

Pharmacological reports : PR April 30, 2025 Michał Walaszek, Wiesław Jerzy Cubała, Zofia Kachlik et al. 3 citations

Ketamine is currently gaining attention as a rapid-acting antidepressant for treatment-resistant depression (TRD). However, many patients fail to respond, and limited data exist on predictors of non-response. This study aims to characterize the sociodemographic and clinical features associated with non-response to ketamine among TRD patients. This is a post-hoc analysis of a naturalistic...

DOI: 10.1007/s43440-025-00730-9 Full text Treatment-resistant depression Mood disorders Psychopharmacology Treatment non-response +2

Psilocybin and the glutamatergic pathway: implications for the treatment of neuropsychiatric diseases.

Pharmacological reports : PR December 1, 2024 Izabela Szpręgiel, Agnieszka Bysiek 18 citations

In recent decades, psilocybin has gained attention as a potential drug for several mental disorders. Clinical and preclinical studies have provided evidence that psilocybin can be used as a fast-acting antidepressant. However, the exact mechanisms of action of psilocybin have not been clearly defined. Data show that psilocybin as an agonist of 5-HT2A receptors located in cortical pyramidal...

DOI: 10.1007/s43440-024-00660-y Full text 5-ht2a receptor Psilocybin Psychedelic medicine Neurotransmitters brain chemicals +4

Drugs with glutamate-based mechanisms of action in psychiatry.

Pharmacological reports : PR December 1, 2024 Adrian Andrzej Chrobak, Marcin Siwek 11 citations

Psychopharmacotherapy of major psychiatric disorders is mostly based on drugs that modulate serotonergic, dopaminergic, or noradrenergic neurotransmission, either by inhibiting their reuptake or by acting as agonists or antagonists on specific monoamine receptors. The effectiveness of this approach is limited by a significant delay in the therapeutic mechanism and self-perpetuating growth of...

DOI: 10.1007/s43440-024-00656-8 Full text Serotonin Antidepressant drugs Antipsychotic drugs Excitotoxicity +7

The quest for optimal ketamine dosing formula in treatment-resistant major depressive disorder.

Pharmacological reports : PR December 1, 2024 Julia Kwaśna, Wiesław Jerzy Cubała, Aleksander Kwaśny et al. 4 citations

Emerging evidence indicates that intravenous ketamine is effective in managing treatment-resistant unipolar and bipolar depression. Clinical studies highlight its favorable efficacy, safety, and tolerability profile within a dosage range of 0.5-1.0 mg/kg based on actual body weight. However, data on alternative dosage calculation methods, particularly in relation to body mass index (BMI) and...

DOI: 10.1007/s43440-024-00637-x Full text Major depressive disorder Body surface area Dose calculation Ideal body weight +6

Sleep alterations in treatment-resistant depression patients undergoing ketamine treatment.

Pharmacological reports : PR December 1, 2024 Aleksander Kwaśny, Wiesław Jerzy Cubała, Adam Włodarczyk et al. 2 citations

This study examines self-reported sleep alterations in treatment-resistant depression (TRD) inpatients following intravenous ketamine administration. This is a post-hoc analysis of a naturalistic observational study, which enrolled 28 inpatients with treatment-resistant major depressive disorder and analyzed self-reported sleep changes (items 1-4; 'insomnia', 'nighttime restlessness', 'early...

DOI: 10.1007/s43440-024-00641-1 Full text Major depressive disorder Treatment-resistant depression Ketamine therapy Sleep disorders +2

Fast-acting antidepressant-like effects of ketamine in aged male rats.

Pharmacological reports : PR October 1, 2024 Elena Hernández-Hernández, Sandra Ledesma-Corvi, Jordi Jornet-Plaza et al. 8 citations

The aging process causes anatomical and physiological changes that predispose to the development of late-life depression while reduces the efficacy of classical antidepressants. Novel fast-acting antidepressants such as ketamine might be good candidates to be explored in the context of aging, especially given the lack of previous research on its efficacy for this age period. Thus, the aim of...

DOI: 10.1007/s43440-024-00636-y Full text Aging Bdnf Fast-acting antidepressant Ketamine therapy +4

Partial mGlu5 receptor NAM, M-5MPEP, induces rapid and sustained antidepressant-like effects in the BDNF-dependent mechanism and enhances (R)-ketamine action in mice.

Pharmacological reports : PR June 1, 2024 Agnieszka Pałucha-Poniewiera, Anna Rafało-Ulińska, Michal Santocki et al. 8 citations

Partial negative allosteric modulators (NAM) of the metabotropic glutamate 5 (mGlu5) receptor are an excellent alternative to full antagonists and NAMs because they retain therapeutic effects and have a much broader therapeutic window. Here, we investigated whether partial mGlu5 NAM, 2-(2-(3-methoxyphenyl)ethynyl)-5-methylpyridine (M-5MPEP), induced a fast and sustained antidepressant-like...

DOI: 10.1007/s43440-024-00588-3 Full text R-ketamine Bdnf M-5mpep Raad +7

MDPV (3,4-methylenedioxypyrovalerone) administered to mice during development of the central nervous system produces persistent learning and memory impairments.

Pharmacological reports : PR June 1, 2024 Katarzyna Kuczyńska, Katarzyna Bartkowska, Ruzanna Djavadian et al. 3 citations

Synthetic cathinones (SC) constitute the second most frequently abused class of new psychoactive substances. They serve as an alternative to classic psychostimulatory drugs of abuse, such as methamphetamine, cocaine, or 3,4-methylenedioxymethamphetamine (MDMA). Despite the worldwide prevalence of SC, little is known about their long-term impact on the central nervous system. Here, we examined...

DOI: 10.1007/s43440-024-00599-0 Full text Neurogenesis Hippocampus Mdpv Object recognition +6

Preclinical models of treatment-resistant depression: challenges and perspectives.

Pharmacological reports : PR December 1, 2023 Magdalena Kolasa, Agata Faron-Górecka 18 citations

Treatment-resistant depression (TRD) is a subgroup of major depressive disorder in which the use of classical antidepressant treatments fails to achieve satisfactory treatment results. Although there are various definitions and grading models for TRD, common criteria for assessing TRD have still not been established. However, a common feature of any TRD model is the lack of response to at least...

DOI: 10.1007/s43440-023-00542-9 Full text Psilocybin Animal models Chronic mild stress Dbs +8

The possible place for psychedelics in pharmacotherapy of mental disorders.

Pharmacological reports : PR December 1, 2023 Adam Wojtas 10 citations

Since its emergence in the 1960s, the serotonergic theory of depression bore fruit in the discovery of a plethora of antidepressant drugs affecting the lives of millions of patients. While crucial in the history of drug development, recent studies undermine the effectiveness of currently used antidepressant drugs in comparison to placebo, emphasizing the long time it takes to initiate the...

DOI: 10.1007/s43440-023-00550-9 Full text 5-MEO-DMT Ketamine LSD Psilocybin +7

Can research on entactogens contribute to a deeper understanding of human sexuality?

Pharmacological reports : PR December 1, 2023 Justyna Holka-Pokorska 5 citations

In recent years, scientific research into the therapeutic potential of psychedelic compounds has experienced a resurgence of interest. New studies have shown promising results, supporting the use of psychedelic drugs in treating various psychiatric disorders, including treatment-resistant depression, post-traumatic stress disorder, and even alcohol addiction. The FDA has recognized...

DOI: 10.1007/s43440-023-00552-7 Full text Psychedelic-assisted psychotherapy 3,4-methylenedioxymethamphetamine Entactogens Sexuality

Interaction of hallucinogenic rapid-acting antidepressants with mGlu2/3 receptor ligands as a window for more effective therapies.

Pharmacological reports : PR December 1, 2023 Barbara Chruścicka-Smaga, Agata Machaczka, Bernadeta Szewczyk et al. 2 citations

The desire to find a gold-standard therapy for depression is still ongoing. Developing one universal and effective pharmacotherapy remains troublesome due to the high complexity and variety of symptoms. Over the last decades, the understanding of the mechanism of pathophysiology of depression and its key consequences for brain functioning have undergone significant changes, referring to the...

DOI: 10.1007/s43440-023-00547-4 Full text Mdd Co-treatment Glutamatergic system Rapid-acting antidepressants +8

Pharmacologic hyperreactivity of kappa opioid receptors in periaqueductal gray matter during alcohol withdrawal syndrome in rats.

Pharmacological reports : PR October 1, 2023 Priscila Vázquez-león, Abraham Miranda-Páez, Hugo Sánchez-Castillo et al.

Periaqueductal gray matter (PAG) is a brain region rich in kappa-opioid receptors (KOR). KOR in PAG mediates behavioral responses related to pain integration, and panic response, among others. Its participation in the addiction phenomena has been poorly studied. Hence, this preliminary study explored the pharmacological effects of KOR stimulation/blockade in dorsal-PAG (D-PAG) during alcohol...

DOI: 10.1007/s43440-023-00522-z Full text Anxiety Salvinorin a Alcohol withdrawal Kappa-opioid +1

Contribution of serotonin receptor subtypes to hallucinogenic activity of 25I-NBOMe and to its effect on neurotransmission.

Pharmacological reports : PR December 1, 2020 Monika Herian, Adam Wojtas, Małgorzata Katarzyna Sobocińska et al. 19 citations

4-Iodo-2,5-dimethoxy-N-(2-methoxybenzyl)phenethylamine (25I-NBOMe) is a potent serotonin (5-HT) receptor agonist with hallucinogenic properties. The aim of our research was to examine the role of the 5-HT2A, 5-HT2C and 5-HT1A serotonin receptor subtypes in 25I-NBOMe hallucinogenic activity and its effect on dopamine (DA), 5-HT and glutamate release in the rat frontal cortex. Hallucinogenic...

DOI: 10.1007/s43440-020-00181-4 Full text 25i-nbome 5-ht2a/2c/1a receptor antagonists Hallucinogenic activity Neurotransmission

The effect of repeated-intermittent exposure to 5-methoxy-N,N-diisopropyltryptamine (5-MeO-DIPT) during adolescence on learning and memory in adult rats.

Pharmacological reports : PR October 1, 2018 Karolina Noworyta-Sokołowska, Anna Maria Górska, Krystyna Gołembiowska 5 citations

According to the European Drug Report, the use of novel psychoactive substances (NPS) is constantly growing. NPS are widely abused by human adolescent subjects. 5-Methoxy-N,N-diisopropyltryptamine (5-MeO-DIPT) is one of the most frequently used hallucinogenic NPS. 5-MeO-DIPT intoxication results in hallucinations, vomiting, and tachycardia. Long-term exposure to 5-MeO-DIPT was reported to lead...

DOI: 10.1016/j.pharep.2018.04.001 Full text 5-Methoxy-N,N-Diisopropyltryptamine Adolescence Open field test

Modification of 5-methoxy-N,N-dimethyltryptamine-induced hyperactivity by monoamine oxidase A inhibitor harmaline in mice and the underlying serotonergic mechanisms.

Pharmacological reports : PR June 1, 2016 Xi-Ling Jiang, Hong-Wu Shen, Ai-Ming Yu 13 citations

5-Methoxy-N,N-dimethyltryptamine (5-MeO-DMT) and harmaline are indolealkylamine (IAA) drugs often abused together. Our recent studies have revealed the significant effects of co-administered harmaline, a monoamine oxidase inhibitor (MAOI), on 5-MeO-DMT pharmacokinetics and thermoregulation. This study was to delineate the impact of harmaline and 5-MeO-DMT on home-cage activity in mouse models,...

DOI: 10.1016/j.pharep.2016.01.008 Full text 5-HT Receptor Harmaline Maoi 5-MEO-DMT Combination +14

Pharmacological activity of salvinorin A, the major component of Salvia divinorum.

Pharmacological reports : PR 2011 Joanna Listos, Alicja Merska, Sylwia Fidecka 52 citations

The hallucinogenic plant Salvia divinorum (i.e., "magic mint") is a member of the Sage family that has been historically used for divination and shamanism by the Mazatecs. Today, S. divinorum has become increasingly popular as a recreational drug for its hallucinogenic effects. The non-nitrogenous diterpene, salvinorin A, the major active component of S. divinorum, is responsible for the...

DOI: 10.1016/s1734-1140(11)70694-6 Full text Salvinorin a Salvia divinorum Active compound Magic mint compound +13

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