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Harald H. Sitte

15 papers in the library · 375 citations · publishing 2011-2026

Papers

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Correction to "Next-Generation MDMA Analogue SDMA: Pharmacological and Metabolic Insights".

ACS Chem Neurosci March 4, 2026 Nina Kastner, Núria Nadal‐gratacós, Selina Hemmer et al. correction

Correction 1: Table 1.The analyses were conducted using the correct data, and all results, interpretations, and conclusions in the paper remain fully accurate.The issue is limited to the presentation of values in the table.Correction 2: p 4733, second paragraph, 1 st sentence.Thigmotaxis was evaluated to assess potential anxiety-like effects induced by the compounds.When comparing the tested...

Next-Generation MDMA Analogue SDMA: Pharmacological and Metabolic Insights

ACS Chemical Neuroscience December 2, 2025 Nina Kastner, Núria Nadal‐gratacós, Selina Hemmer et al.

3,4-Methylenedioxymethamphetamine (MDMA), commonly known as ecstasy, shows promise in treating depression and post-traumatic stress disorder (PTSD), resulting in breakthrough status. However, concerns regarding MDMA's abuse potential and cytotoxicity have sparked interest in developing safer analogues with similar therapeutic benefits. This study investigated the pharmacological properties of...

The psychedelic phenethylamine 25C-NBF, a selective 5-HT2A agonist, shows psychoplastogenic properties and rapid antidepressant effects in male rodents

Molecular Psychiatry November 14, 2025 Núria Nadal‐gratacós, Pol Puigseslloses, Laura Hernández‐guzmán et al.

Psychedelics have garnered significant interest for their therapeutic potential in mental health conditions such as depression, anxiety, and post-traumatic stress disorder. While research has primarily focused on well-studied psychedelics, phenethylamine derivatives have also gathered interest for their potential therapeutic applications. Thus, this study aims to investigate the pharmacological...

Bioisosteric analogs of MDMA: Improving the pharmacological profile?

Journal of Neurochemistry September 1, 2024 Ana Sofia Alberto-Silva, Selina Hemmer, Hailey A. Bock et al. 10 citations

3,4-Methylenedioxymethamphetamine (MDMA, 'ecstasy') is re-emerging in clinical settings as a candidate for the treatment of specific neuropsychiatric disorders (e.g. post-traumatic stress disorder) in combination with psychotherapy. MDMA is a psychoactive drug, typically regarded as an empathogen or entactogen, which leads to transporter-mediated monoamine release. Despite its therapeutic...

Bioisosteric analogs of MDMA with improved pharmacological profile.

bioRxiv : the preprint server for biology April 11, 2024 Ana Sofia Alberto-Silva, Selina Hemmer, Hailey A. Bock et al. preprint

3,4-Methylenedioxymethamphetamine (MDMA, ' ecstasy' ) is re-emerging in clinical settings as a candidate for the treatment of specific psychiatric disorders (e.g. post-traumatic stress disorder) in combination with psychotherapy. MDMA is a psychoactive drug, typically regarded as an empathogen or entactogen, which leads to transporter-mediated monoamine release. Despite its therapeutic...

Structure-activity relationships of serotonergic 5-MeO-DMT derivatives: insights into psychoactive and thermoregulatory properties

Molecular Psychiatry March 14, 2024 Pol Puigseslloses, Gabriel Ketsela, Nicola Weiss et al. 23 citations

Abstract Recent studies have sparked renewed interest in the therapeutic potential of psychedelics for treating depression and other mental health conditions. Simultaneously, the novel psychoactive substances (NPS) phenomenon, with a huge number of NPS emerging constantly, has changed remarkably the illicit drug market, being their scientific evaluation an urgent need. Thus, this study aims to...

Editorial: Old and new psychoactive substances: Pharmacology and potential applications

Frontiers in Psychiatry January 4, 2023 Felix P. Mayer, Dino Luethi, Lorena B. Areal et al. 1 citation

The consumption of psychoactive substances is inextricably linked with human history. Longstanding evidence supports the consumption of psychoactive substances that are found in plants and fungi (e.g. cathinone and muscimol, which are present in Catha edulis and Amanita muscaria, respectively) and alcoholic beverages. With the advent of more refined chemical approaches, isolated (e.g. cocaine)...

(2-Aminopropyl)benzo[β]thiophenes (APBTs) are novel monoamine transporter ligands that lack stimulant effects but display psychedelic-like activity in mice.

Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology March 1, 2022 Deborah Rudin, John D. Mccorvy, Grant C. Glatfelter et al. 18 citations

Derivatives of (2-aminopropyl)indole (API) and (2-aminopropyl)benzofuran (APB) are new psychoactive substances which produce stimulant effects in vivo. (2-Aminopropyl)benzo[β]thiophene (APBT) is a novel sulfur-based analog of API and APB that has not been pharmacologically characterized. In the current study, we assessed the pharmacological effects of six APBT positional isomers in vitro, and...

Interaction Profiles of Central Nervous System Active Drugs at Human Organic Cation Transporters 1-3 and Human Plasma Membrane Monoamine Transporter.

International Journal of Molecular Sciences November 30, 2021 Thomas J F Angenoorth, Stevan Stankovic, Marco Niello et al. 18 citations

Many psychoactive compounds have been shown to primarily interact with high-affinity and low-capacity solute carrier 6 (SLC6) monoamine transporters for norepinephrine (NET; norepinephrine transporter), dopamine (DAT; dopamine transporter) and serotonin (SERT; serotonin transporter). Previous studies indicate an overlap between the inhibitory capacities of substances at SLC6 and SLC22 human...

DARK Classics in Chemical Neuroscience: Aminorex Analogues

ACS Chemical Neuroscience September 30, 2018 Julian Maier, Felix P. Mayer, Simon D. Brandt et al. 15 citations

Aminorex (5-phenyl-4,5-dihydro-1,3-oxazol-2-amine) and 4-methylaminorex (4-methyl-5-phenyl-4,5-dihydro-1,3-oxazol-2-amine) are psychostimulants that have long been listed in Schedules IV and I of the UN Convention on Psychotropic Substances of 1971. However, a range of psychoactive analogues exist that are not internationally controlled and therefore often classified as new psychoactive...

The psychostimulant (±)-cis-4,4′-dimethylaminorex (4,4′-DMAR) interacts with human plasmalemmal and vesicular monoamine transporters

Neuropharmacology June 23, 2018 Julian Maier, Felix P. Mayer, Dino Luethi et al. 24 citations

(±)-cis-4,4′-Dimethylaminorex (4,4′-DMAR) is a new psychoactive substance (NPS) that has been associated with 31 fatalities and other adverse events in Europe between June 2013 and February 2014. We used in vitro uptake inhibition and transporter release assays to determine the effects of 4,4′-DMAR on human high-affinity transporters for dopamine (DAT), norepinephrine (NET) and serotonin...

Fluorinated phenmetrazine “legal highs” act as substrates for high-affinity monoamine transporters of the SLC6 family

Neuropharmacology October 12, 2017 Felix P. Mayer, Nadine V. Burchardt, Ann M Decker et al. 30 citations

A variety of new psychoactive substances (NPS) are appearing in recreational drug markets worldwide. NPS are compounds that target various receptors and transporters in the central nervous system to achieve their psychoactive effects. Chemical modifications of existing drugs can generate NPS that are not controlled by current legislation, thereby providing legal alternatives to controlled...

Salvinorin A regulates dopamine transporter function via a kappa opioid receptor and ERK1/2-dependent mechanism.

Neuropharmacology November 1, 2014 Bronwyn M Kivell, Zeljko Uzelac, Santhanalakshmi Sundaramurthy et al.

Salvinorin A (SalA), a selective κ-opioid receptor (KOR) agonist, produces dysphoria and pro-depressant like effects. These actions have been attributed to inhibition of striatal dopamine release. The dopamine transporter (DAT) regulates dopamine transmission via uptake of released neurotransmitter. KORs are apposed to DAT in dopamine nerve terminals suggesting an additional target by which...

The mechanistic basis for noncompetitive ibogaine inhibition of serotonin and dopamine transporters.

The Journal of biological chemistry May 25, 2012 Simon Bulling, Klaus Schicker, Yuan-Wei Zhang et al. 124 citations

Ibogaine, a hallucinogenic alkaloid proposed as a treatment for opiate withdrawal, has been shown to inhibit serotonin transporter (SERT) noncompetitively, in contrast to all other known inhibitors, which are competitive with substrate. Ibogaine binding to SERT increases accessibility in the permeation pathway connecting the substrate-binding site with the cytoplasm. Because of the structural...

The ugly side of amphetamines: short- and long-term toxicity of 3,4-methylenedioxymethamphetamine (MDMA, ‘Ecstasy’), methamphetamine and d-amphetamine

Biological Chemistry January 2, 2011 Thomas Steinkellner, Michael Freissmuth, Harald H. Sitte et al. 112 citations

Abstract Amphetamine (‘Speed’), methamphetamine (‘Ice’) and its congener 3,4-methylenedioxymethamphetamine (MDMA; ‘Ecstasy’) are illicit drugs abused worldwide for their euphoric and stimulant effects. Despite compelling evidence for chronic MDMA neurotoxicity in animal models, the physiological consequences of such toxicity in humans remain unclear. In addition, distinct differences in the...