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Nina Kastner

4 papers in the library · 10 citations · publishing 2024-2026

Papers

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

Three new chemical variants of MDMA—ODMA, TDMA, and SeDMA—show similar activity at serotonin, dopamine, and norepinephrine transporters but reduced activity at 5-HT2A/2B/2C receptors compared to MDMA. They also differ in liver metabolism, with N-demethylation as the only shared route and no phase II metabolites formed. TDMA showed faster clearance. The analogs interacted more weakly with organic cation transporters and plasma membrane monoamine transporter. These bioisosteres may offer therapeutic alternatives to MDMA with a reduced off-target profile, but further studies are needed to determine if they pose lower risks.

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

A correction notice clarifies that two errors in the original paper do not affect the accuracy of the results, interpretations, or conclusions. The first correction addresses a presentation issue in Table 1, confirming the data are correct. The second correction clarifies that thigmotaxis, a measure of anxiety-like behavior, was evaluated in rats given SDA or SDMA compounds. Compared to saline, only the 10 mg/kg dose of SDA significantly increased thigmotaxis, meaning the rats spent less time in the center of the arena.

Next-Generation MDMA Analogue SDMA: Pharmacological and Metabolic Insights

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

Replacing the 1,3-benzodioxole group in MDMA (ecstasy) with a 1,3-benzoxathiole yields two analogues, SDA and SDMA, that interact with monoamine transporters similarly to MDMA but with key differences. SDA and SDMA inhibit dopamine and norepinephrine transporters more potently than MDMA and act as partial releasers at serotonin and dopamine transporters. Metabolism studies show SDA and SDMA are cleared faster, while MDMA and MDA degrade only weakly. In mice, SDMA does not produce rewarding effects, unlike MDMA, and SDA only shows a preference for the drug-paired compartment at the lowest dose. SDMA shares similar locomotor and hyperthermic profiles with MDMA, whereas SDA induces increased hyperlocomotion and more sustained hyperthermia. SDMA may be a safer candidate for further study.

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

Three new chemical variants of MDMA—ODMA, TDMA, and SeDMA—show similar activity at serotonin and dopamine transporters but reduced activity at serotonin 5-HT2A/2B/2C receptors, which may lower the risk of off-target side effects. They also differ from MDMA in how they are broken down by the liver, with fewer metabolic pathways and no phase II metabolites. The analogs interact more weakly with certain organic cation transporters. These findings suggest the new compounds could be promising therapeutic alternatives to MDMA for conditions like PTSD, though further research is needed to confirm whether they pose lower risks.