Evidence map›Paper›PMID 41915198›Full record

ArticleArchives of toxicology2026

TRACT assay-based in vitro characterization of substituted cathinones: inhibition and release at the serotonin transporter.

Axelle Timmerman, Eline Pottie, Christophe P Stove

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Article in Archives of toxicology, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

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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

1 citing paper in PubMed.

  1. Article
4 · The record

Corrections and comments

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5 · Who and what money

Authors and funding

3 authors.

Axelle TimmermanLaboratory of Toxicology, Department of Bioanalysis, Ghent University, 9000, Ghent, Belgium.
Eline PottieLaboratory of Toxicology, Department of Bioanalysis, Ghent University, 9000, Ghent, Belgium.
Christophe P StoveLaboratory of Toxicology, Department of Bioanalysis, Ghent University, 9000, Ghent, Belgium. christophe.stove@ugent.be.ORCID 0000-0001-7126-348X

Funding

Bijzonder Onderzoeksfonds UGent BOF21/DOC/248Bijzonder Onderzoeksfonds UGent BOF23/PDO/073
6 · The paper itself

Abstract

Synthetic cathinones are increasingly popular new psychoactive substances (NPS), with new structures often designed to evade legal restrictions. Besides presenting challenges for drug policy, this also results in a poor understanding of these compounds’ pharmacological effects, particularly concerning their interaction with monoamine transporters such as the serotonin transporter (SERT). Therefore, we optimized a previously developed SERT bioassay based on the TRACT (transporter activity through receptor activation) principle by developing a new human embryonic kidney (HEK) 293T cell line stably expressing SERT (HEK293T-SERT). The use of this cell line was evaluated in the TRACT protocol to determine uptake inhibition and SERT-mediated serotonin (5-HT) release. SERT effects are measured by means of a modified serotonin 2 A receptor (5-HT2AR), using functional complementation of a split-nanoluciferase. 5-HT2AR activation depends on extracellular serotonin levels, which are elevated either through inhibited or reversed 5-HT transport. The TRACT assay format for SERT inhibition with the new HEK293T-SERT cell line outperformed the transient transfection protocol. In addition, the use of the HEK293T-SERT cells in a fluorescence-based functional assay resulted in an identical ranking of the SERT inhibition activities of a set of eleven diversely substituted cathinones in both TRACT and fluorescence assays. These compounds carried key substitutions, including N-alkylation/arylation, ring substitution and α-alkylation. Furthermore, the TRACT assay format was suited to distinguish between SERT blockers and releasers, and allowed functional characterization. Overall, the dual functionality of the optimized TRACT assay provides a versatile tool for characterizing SERT-modulating NPS, with potential applications in therapeutic drug development.

Indexed as

AlkaloidsBiological AssayPsychotropic DrugsSelective Serotonin Reuptake InhibitorsSerotonin Plasma Membrane Transport ProteinsHEK293 CellsHumansReceptor, Serotonin, 5-HT2ASerotoninTransfectionAlkaloidscathinonePsychotropic DrugsReceptor, Serotonin, 5-HT2ASelective Serotonin Reuptake InhibitorsSerotoninSerotonin Plasma Membrane Transport Proteins5-HT releaseSerotonin 2A receptor (5-HT2AR)Serotonin transporter (SERT)SERT inhibitionSynthetic cathinonesTRACT assay

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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 OpenQuestion graph.