The authors synthesised and characterised three methylenedioxy bioisosteres of MDMA (ODMA, TDMA and SeDMA) that retain activity at human serotonin, dopamine and norepinephrine transporters but show reduced agonism at 5‑HT2A/2B/2C receptors, altered hepatic metabolism (no phase II metabolites, N‑demethylation conserved) and weaker interactions with hOCTs and hPMAT. These pharmacological and metabolic differences suggest they could be promising lower‑risk therapeutic alternatives to MDMA, warranting further preclinical and clinical evaluation.
- Published
- Journal
- Journal of Neurochemistry
- Authors
- Sofia, A., Hemmer, S., Bock, H. A., Alves Da Silva, L., Scott, K. R., Kastner, N., Bhatt, M., Niello, M., Jäntsch, K., Kudlacek, |. O., Bossi, E., Stockner, T., Meyer, M. R., Mccorvy, J. D., Brandt, S. D., Kavanagh, P., Sitte, H. H., Kudlacek, O.