Evidence map›Paper›PMID 38898705›Full record

ArticleJournal of neurochemistry2024

Bioisosteric analogs of MDMA: Improving the pharmacological profile?

Ana Sofia Alberto-Silva, Selina Hemmer, Hailey A Bock, Leticia Alves da Silva, Kenneth R Scott, Nina Kastner, Manan Bhatt, Marco Niello, Kathrin Jäntsch, Oliver Kudlacek and 7 more

Abstract read
In one paragraph

Article in Journal of neurochemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

7 citing papers in PubMed.

  1. Acute effects of MDMA, MDA, lysine-MDMA, and lysine-MDA in a randomized, double-blind, placebo-controlled, crossover trial in healthy participants.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2026
    Trial
  2. Interpol review of forensic drug chemistry, 2022-2025.Forensic science international. Synergy · 2026
    Review
  3. Review
  4. Article
  5. Article
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4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

17 authors.

Ana Sofia Alberto-SilvaCenter for Physiology and Pharmacology, Institute of Pharmacology, Medical University of Vienna, Vienna, Austria.ORCID 0000-0001-5662-0581
Selina HemmerDepartment of Experimental and Clinical Toxicology, Institute of Experimental and Clinical Pharmacology and Toxicology, Center for Molecular Signaling (PZMS), Saarland University, Homburg, Germany.ORCID 0009-0009-5534-0612
Hailey A BockDepartment of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin, USA.ORCID 0000-0002-3457-9319
Leticia Alves da SilvaCenter for Physiology and Pharmacology, Institute of Pharmacology, Medical University of Vienna, Vienna, Austria.ORCID 0000-0002-9620-3974
Kenneth R ScottDepartment of Pharmacology and Therapeutics, School of Medicine, Trinity Centre for Health Sciences, St James Hospital, Dublin, Ireland.ORCID 0009-0009-5113-7908
Nina KastnerCenter for Physiology and Pharmacology, Institute of Pharmacology, Medical University of Vienna, Vienna, Austria.ORCID 0000-0002-1576-9029
Manan BhattLaboratory of Cellular and Molecular Physiology, Department of Biotechnology and Life Sciences, University of Insubria, Varese, Italy.ORCID 0000-0002-5792-0081
Marco NielloCenter for Physiology and Pharmacology, Institute of Pharmacology, Medical University of Vienna, Vienna, Austria.ORCID 0000-0002-0518-5791
Kathrin JäntschCenter for Physiology and Pharmacology, Institute of Pharmacology, Medical University of Vienna, Vienna, Austria.
Oliver KudlacekCenter for Physiology and Pharmacology, Institute of Pharmacology, Medical University of Vienna, Vienna, Austria.ORCID 0000-0002-3086-8551
Elena BossiLaboratory of Cellular and Molecular Physiology, Department of Biotechnology and Life Sciences, University of Insubria, Varese, Italy.ORCID 0000-0002-9549-2153
Thomas StocknerCenter for Physiology and Pharmacology, Institute of Pharmacology, Medical University of Vienna, Vienna, Austria.ORCID 0000-0002-7071-8283
Markus R MeyerDepartment of Experimental and Clinical Toxicology, Institute of Experimental and Clinical Pharmacology and Toxicology, Center for Molecular Signaling (PZMS), Saarland University, Homburg, Germany.ORCID 0000-0003-4377-6784
John D McCorvyDepartment of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin, USA.ORCID 0000-0001-7555-9413
Simon D BrandtSchool of Pharmacy and Biomolecular Sciences, Liverpool John Moores University, Liverpool, UK.ORCID 0000-0001-8632-5372
Pierce KavanaghDepartment of Pharmacology and Therapeutics, School of Medicine, Trinity Centre for Health Sciences, St James Hospital, Dublin, Ireland.ORCID 0000-0002-1613-3305
Harald H SitteCenter for Physiology and Pharmacology, Institute of Pharmacology, Medical University of Vienna, Vienna, Austria.ORCID 0000-0002-1339-7444

Funding

Structure-based Design of Selective Serotonin Biased Agonists as Chemical Probes for Psychedelic PotentialR01MH133849 · NIMH · MEDICAL COLLEGE OF WISCONSIN · PI John D McCorvy · 2023 to 2026
$2.1M
Austrian Science Fund P32017Austrian Science Fund P35589Austrian Science Fund W1232Horizon 2020 Framework Programme 860954NIH HHS R01 MH133849NIMH NIH HHS R01 MH133849
6 · The paper itself

Abstract

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 potential, MDMA can induce dose-, individual-, and context-dependent untoward effects outside safe settings. In this study, we investigated whether three new methylenedioxy bioisosteres of MDMA improve its off-target profile. In vitro methods included radiotracer assays, transporter electrophysiology, bioluminescence resonance energy transfer and fluorescence-based assays, pooled human liver microsome/S9 fraction incubations, metabolic stability studies, isozyme mapping, and liquid chromatography coupled to high-resolution mass spectrometry. In silico methods included molecular docking. Compared with MDMA, all three MDMA bioisosteres (ODMA, TDMA, and SeDMA) showed similar pharmacological activity at human serotonin, dopamine, and norepinephrine transporters (hSERT, hDAT, and hNET, respectively) but decreased agonist activity at 5-HT

Indexed as

N-Methyl-3,4-methylenedioxyamphetamineAnimalsHallucinogensHEK293 CellsHumansMicrosomes, LiverMolecular Docking SimulationHallucinogensN-Methyl-3,4-methylenedioxyamphetamine

Identifiers

PMID38898705
PMCPMC11449655

What Socratic holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.