Designer drugs: mechanism of action and adverse effects

D Luethi, ME Liechti - Archives of toxicology, 2020 - Springer
Psychoactive substances with chemical structures or pharmacological profiles that are
similar to traditional drugs of abuse continue to emerge on the recreational drug market …

[HTML][HTML] Molecular and clinical aspects of potential neurotoxicity induced by new psychoactive stimulants and psychedelics

D Rudin, ME Liechti, D Luethi - Experimental neurology, 2021 - Elsevier
New psychoactive stimulants and psychedelics continue to play an important role on the
illicit new psychoactive substance (NPS) market. Designer stimulants and psychedelics both …

Ligand coupling mechanism of the human serotonin transporter differentiates substrates from inhibitors

R Gradisch, K Schlögl, E Lazzarin, M Niello… - Nature …, 2024 - nature.com
The presynaptic serotonin transporter (SERT) clears extracellular serotonin following
vesicular release to ensure temporal and spatial regulation of serotonergic signalling and …

Serotonin-releasing agents with reduced off-target effects

FP Mayer, M Niello, D Cintulova, S Sideromenos… - Molecular …, 2023 - nature.com
Increasing extracellular levels of serotonin (5-HT) in the brain ameliorates symptoms of
depression and anxiety-related disorders, eg, social phobias and post-traumatic stress …

Allosteric modulation of neurotransmitter transporters as a therapeutic strategy

M Niello, R Gradisch, CJ Loland, T Stockner… - Trends in …, 2020 - cell.com
Neurotransmitter transporters (NTTs) are involved in the fine-tuning of brain neurotransmitter
homeostasis. As such, they are implicated in a plethora of complex behaviors, including …

Persistent binding at dopamine transporters determines sustained psychostimulant effects

M Niello, S Sideromenos, R Gradisch… - Proceedings of the …, 2023 - National Acad Sciences
Psychostimulants interacting with the dopamine transporter (DAT) can be used illicitly or for
the treatment of specific neuropsychiatric disorders. However, they can also produce severe …

Occlusion of the human serotonin transporter is mediated by serotonin-induced conformational changes in the bundle domain

R Gradisch, D Szöllősi, M Niello, E Lazzarin… - Journal of Biological …, 2022 - ASBMB
The human serotonin transporter (hSERT) terminates neurotransmission by removing
serotonin (5HT) from the synaptic cleft, an essential process for proper functioning of …

Computational chemistry in structure-based solute carrier transporter drug design: Recent advances and future perspectives

G Tu, T Fu, G Zheng, B Xu, R Gou, D Luo… - Journal of chemical …, 2024 - ACS Publications
Solute carrier transporters (SLCs) are a class of important transmembrane proteins that are
involved in the transportation of diverse solute ions and small molecules into cells. There are …

Psychoactive drugs—from chemical structure to oxidative stress related to dopaminergic neurotransmission. A review

G Jîtcă, BE Ősz, A Tero-Vescan, CE Vari - Antioxidants, 2021 - mdpi.com
Nowadays, more and more young people want to experience illegal, psychoactive
substances, without knowing the risks of exposure. Besides affecting social life …

[HTML][HTML] Role of amino terminal substitutions in the pharmacological, rewarding and psychostimulant profiles of novel synthetic cathinones

L Duart-Castells, N Nadal-Gratacós, M Muralter… - …, 2021 - Elsevier
The emergence of new synthetic cathinones continues to be a matter of public health
concern. In fact, they are quickly replaced by new structurally related alternatives. The main …