Lysergic acid diethylamide stimulates cardiac human H2 histamine and cardiac human 5-HT4-serotonin receptors

Article Pharmacology & Pharmacy

Levosimendan increases the phosphorylation state of phospholamban in the isolated human atrium

Lina Maria Rayo Abella et al.

Summary: Our study demonstrates that levosimendan acts via inhibition of phosphodiesterase III in the human atrium, leading to phosphorylation of phospholamban and explaining its positive inotropic effects.

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY (2023)

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Review Biochemistry & Molecular Biology

Cardiac Roles of Serotonin (5-HT) and 5-HT-Receptors in Health and Disease

Joachim Neumann et al.

Summary: Serotonin controls human cardiac contractile function solely through 5-HT4-receptors, leading to positive inotropic and chronotropic effects, as well as arrhythmias. This review focuses on the potential effects of 5-HT4-receptors in sepsis, ischemia, and reperfusion. The formation and inactivation of serotonin in the heart, as well as its role in cardiovascular diseases, are discussed. Mechanisms of cardiac signal transduction through 5-HT4-receptors and potential roles in cardiac diseases are addressed, along with future research directions and potential animal models. The potential clinical utility of 5-HT4-receptor agonists or antagonists is also discussed, considering the extensive studies on serotonin over the years.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

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Article Biochemistry & Molecular Biology

Biochemical Mechanisms Underlying Psychedelic-Induced Neuroplasticity

David E. Olson

Summary: In addition to their profound subjective effects, psychedelic compounds can induce long-lasting beneficial behavioral changes relevant to the treatment of neuropsychiatric disorders. This may be due to their ability to promote neuroplasticity in the prefrontal cortex, leading to synaptic connectivity restoration. Understanding the molecular mechanisms behind psychedelic-induced neuroplasticity is crucial for developing improved alternatives for treating these disorders.

BIOCHEMISTRY (2022)

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Review Clinical Neurology

Adverse effects of psychedelics: From anecdotes and misinformation to systematic science

Anne K. Schlag et al.

Summary: This narrative review examines the evidence for potential harms of classic psychedelics and emphasizes the importance of adhering to high safety and ethical standards. The review finds that medical risks are often minimal and many negative perceptions of psychological risks lack scientific support.

JOURNAL OF PSYCHOPHARMACOLOGY (2022)

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Article Pharmacology & Pharmacy

Amitriptyline functionally antagonizes cardiac H2 histamine receptors in transgenic mice and human atria

Joachim Neumann et al.

Summary: The study demonstrated that amitriptyline acts as an antagonist of contractility at H(2)Rs in H2R-TG mouse hearts and in the human heart. This finding may help explain the side effects of amitriptyline.

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY (2021)

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Review Pharmacology & Pharmacy

The Roles of Cardiovascular H2-Histamine Receptors Under Normal and Pathophysiological Conditions

Joachim Neumann et al.

Summary: This review discusses the pharmacological, structural, and functional relationships between H-2-histamine receptors and H-1-histamine receptors in the mammalian heart, focusing on their role in regulating heart force and rhythm, potential clinical applications in cardiac diseases, and the effects on cardiac arrhythmias. It also highlights novel findings, limitations in current understanding, and suggests future research directions, including the possible development of cardiomyocyte-specific H-2-histamine receptor agonists and antagonists.

FRONTIERS IN PHARMACOLOGY (2021)

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Article Pharmacology & Pharmacy

Histamine can be Formed and Degraded in the Human and Mouse Heart

Joachim Neumann et al.

Summary: This study explores the physiological role of histamine in the mouse and human heart, and demonstrates that inhibiting histamine-metabolizing enzymes can alter the beating rate and force of the human heart.

FRONTIERS IN PHARMACOLOGY (2021)

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Article Chemistry, Medicinal

A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H3 Receptor

Niklas Rosier et al.

Summary: The novel fluorescent H3R ligand UR-NR266 has been synthesized and characterized for its exceptional selectivity and pharmacological properties at the sub-nanomolar level. It shows fast association and dissociation kinetics at the H3R, making it a versatile pharmacological tool for analyzing future H3R ligands. UR-NR266 also exhibits low nonspecific binding and has been identified as a selective compound in off-target screening at 14 receptors.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Pharmacology & Pharmacy

Cardiac Effects of Novel Histamine H2 Receptor Agonists

Ulrich Gergs et al.

Summary: The three newly developed H-2 receptor agonists demonstrated increased cardiac effects in H-2-TG mice, but not in WT mice. These effects were antagonized by the H-2 receptor antagonist famotidine. The agonists also increased left ventricular ejection fraction in H-2-TG mice, suggesting potential therapeutic benefits for neurological disorders and congestive heart failure.

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2021)

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Article Neurosciences

Distinct acute effects of LSD, MDMA, and d-amphetamine in healthy subjects

Friederike Holze et al.

NEUROPSYCHOPHARMACOLOGY (2020)

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Article Pharmacology & Pharmacy

Characterization of Stressed Transgenic Mice Overexpressing H2-Cardiovascular Receptors in the Heart

Ulrich Gergs et al.

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2020)

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Article Pharmacology & Pharmacy

Pharmacokinetics and subjective effects of a novel oral LSD formulation in healthy subjects

Friederike Holze et al.

BRITISH JOURNAL OF CLINICAL PHARMACOLOGY (2019)

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Article Pharmacology & Pharmacy

Initial Characterization of Transgenic Mice Overexpressing Human Histamine H2 Receptors

U. Gergs et al.

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2019)

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Article Pharmacology & Pharmacy

Cytochrome P450 enzymes contribute to the metabolism of LSD to nor-LSD and 2-oxo-3-hydroxy-LSD: Implications for clinical LSD use

Dino Luethi et al.

BIOCHEMICAL PHARMACOLOGY (2019)

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Article Medical Laboratory Technology

Development and validation of an LC-MS/MS method to quantify lysergic acid diethylamide (LSD), iso-LSD, 2-oxo-3-hydroxy-LSD, and nor-LSD and identify novel metabolites in plasma samples in a controlled clinical trial

Patrick C. Dolder et al.

JOURNAL OF CLINICAL LABORATORY ANALYSIS (2018)

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Article Clinical Neurology

Does getting high hurt? Characterization of cases of LSD and psilocybin-containing mushroom exposures to national poison centers between 2000 and 2016

James B. Leonard et al.

JOURNAL OF PSYCHOPHARMACOLOGY (2018)

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Article Chemistry, Multidisciplinary

Highly Potent, Stable, and Selective Dimeric Hetarylpropylguanidine-Type Histamine H2 Receptor Agonists

Steffen Pockes et al.

ACS OMEGA (2018)

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Review Biochemistry & Molecular Biology

D-Lysergic Acid Diethylamide (LSD) as a Model of Psychosis: Mechanism of Action and Pharmacology

Danilo De Gregorio et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2016)

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Article Chemistry, Medicinal

[3H]UR-DE257: Development of a Tritium-Labeled Squaramide-Type Selective Histamine H2 Receptor Antagonist

Paul Baumeister et al.

CHEMMEDCHEM (2015)

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Article Clinical Neurology

LSD-assisted psychotherapy for anxiety associated with a life-threatening disease: A qualitative study of acute and sustained subjective effects

Peter Gasser et al.

JOURNAL OF PSYCHOPHARMACOLOGY (2015)

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Article Biochemistry & Molecular Biology

Cardiac Function Is Regulated by B56 α-mediated Targeting of Protein Phosphatase 2A (PP2A) to Contractile Relevant Substrates

Uwe Kirchhefer et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2014)

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Article Medicine, Legal

Determination of psilocin, bufotenine, LSD and its metabolites in serum, plasma and urine by SPE-LC-MS/MS

Rafaela Martin et al.

INTERNATIONAL JOURNAL OF LEGAL MEDICINE (2013)

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Article Pharmacology & Pharmacy

Human 5-HT4 receptor stimulation in atria of transgenic mice

Ulrich Gergs et al.

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY (2013)

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Letter Biochemistry & Molecular Biology

Antitumor properties of histamine in vivo

Fredrik B. Thoren et al.

NATURE MEDICINE (2011)

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Article Cardiac & Cardiovascular Systems

Cardiac overexpression of the human 5-HT4 receptor in mice

Ulrich Gergs et al.

AMERICAN JOURNAL OF PHYSIOLOGY-HEART AND CIRCULATORY PHYSIOLOGY (2010)

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Article Pharmacology & Pharmacy

Phosphorylation of phospholamban and troponin I through 5-HT4 receptors in the isolated human atrium

Ulrich Gergs et al.

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY (2009)

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Review Neurosciences

LSD-assisted psychotherapy in persons suffering from anxiety associated with advanced-stage life threatening diseases. A phase-II, double-blind, placebo-controlled dose-response pilot study

Torsten Passie et al.

CNS NEUROSCIENCE & THERAPEUTICS (2008)

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Article Cardiac & Cardiovascular Systems

A novel data mining approach to the identification of effective drugs or combinations for targeted endpoints - Application to chronic heart failure as a new form of evidence-based medicine

J Kim et al.

CARDIOVASCULAR DRUGS AND THERAPY (2004)

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Article Pharmacology & Pharmacy

Cloning, pharmacological characterisation and tissue distribution of a novel 5-HT4 receptor splice variant, 5-HT4(i)

T Brattelid et al.

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY (2004)

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Article Pharmacology & Pharmacy

Histamine H1 and H2 receptor gene and protein levels are differentially expressed in the hearts of rodents and humans

N Matsuda et al.

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2004)

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Article Cardiac & Cardiovascular Systems

Altered function in atrium of transgenic mice overexpressing triadin 1

U Kirchhefer et al.

AMERICAN JOURNAL OF PHYSIOLOGY-HEART AND CIRCULATORY PHYSIOLOGY (2002)

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Article Multidisciplinary Sciences

Salvinorin A:: A potent naturally occurring nonnitrogenous κ opioid selective agonist

BL Roth et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2002)

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Lysergic acid diethylamide stimulates cardiac human H2 histamine and cardiac human 5-HT4-serotonin receptors

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