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

Autor: Ralph Gradisch, Katharina Schlögl, Erika Lazzarin, Marco Niello, Julian Maier, Felix P. Mayer, Leticia Alves da Silva, Sophie M. C. Skopec, Randy D. Blakely, Harald H. Sitte, Marko D. Mihovilovic, Thomas Stockner

Publikováno v: Nature Communications, Vol 15, Iss 1, Pp 1-15 (2024)

Abstract The presynaptic serotonin transporter (SERT) clears extracellular serotonin following vesicular release to ensure temporal and spatial regulation of serotonergic signalling and neurotransmitter homeostasis. Prescription drugs used to treat n

Externí odkaz: https://doaj.org/article/692fe13fc3064dfcb15c92bc73a03588

Handling of intracellular K+ determines voltage dependence of plasmalemmal monoamine transporter function

Autor: Shreyas Bhat, Marco Niello, Klaus Schicker, Christian Pifl, Harald H Sitte, Michael Freissmuth, Walter Sandtner

Publikováno v: eLife, Vol 10 (2021)

The concentrative power of the transporters for dopamine (DAT), norepinephrine (NET), and serotonin (SERT) is thought to be fueled by the transmembrane Na+ gradient, but it is conceivable that they can also tap other energy sources, for example, memb

Externí odkaz: https://doaj.org/article/f8319784533d4212a5b854d4f27eef80

Effects of Hydroxylated Mephedrone Metabolites on Monoamine Transporter Activity in vitro

Autor: Marco Niello, Daniela Cintulová, Philip Raithmayr, Marion Holy, Kathrin Jäntsch, Claire Colas, Gerhard F. Ecker, Harald H. Sitte, Marko D. Mihovilovic

Publikováno v: Frontiers in Pharmacology, Vol 12 (2021)

Mephedrone is a largely abused psychostimulant. It elicits the release of monoamines via the high affinity transporters for dopamine (DAT), norepinephrine (NET) and serotonin (SERT). Stereoselective metabolic reactions are involved in the inactivatio

Externí odkaz: https://doaj.org/article/cad0c2981194441b90dff4c025c6fe1c

Persistent binding at dopamine transporters determines sustained psychostimulant effects

Autor: Marco Niello, Spyridon Sideromenos, Ralph Gradisch, Ronan O´Shea, Jakob Schwazer, Julian Maier, Nina Kastner, Walter Sandtner, Kathrin Jäntsch, Carl R. Lupica, Alexander F. Hoffman, Gert Lubec, Claus J. Loland, Thomas Stockner, Daniela D. Pollak, Michael H. Baumann, Harald H. Sitte

Publikováno v: Niello, M, Sideromenos, S, Gradisch, R, O'Shea, R, Schwazer, J, Maier, J, Kastner, N, Sandtner, W, Jäntsch, K, Lupica, C R, Hoffman, A F, Lubec, G, Loland, C J, Stockner, T, Pollak, D D, Baumann, M H & Sitte, H H 2023, ' Persistent binding at dopamine transporters determines sustained psychostimulant effects ', Proceedings of the National Academy of Sciences of the United States of America, vol. 120, no. 6, e2114204120 . https://doi.org/10.1073/pnas.2114204120

Psychostimulants interacting with the dopamine transporter (DAT) can be used illicitly or for the treatment of specific neuropsychiatric disorders. However, they can also pro-duce severe and persistent adverse events. Often, their pharmacological pro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::df188dfc32dc6e8ac10ea0975a519aa7
https://doi.org/10.1073/pnas.2114204120

Interaction Profiles of Central Nervous System Active Drugs at Human Organic Cation Transporters 1–3 and Human Plasma Membrane Monoamine Transporter

Autor: Maier, Thomas J. F. Angenoorth, Stevan Stankovic, Marco Niello, Marion Holy, Simon D. Brandt, Harald H. Sitte, Julian

Publikováno v: International Journal of Molecular Sciences; Volume 22; Issue 23; Pages: 12995

Many psychoactive compounds have been shown to primarily interact with high-affinity and low-capacity solute carrier 6 (SLC6) monoamine transporters for norepinephrine (NET; norepinephrine transporter), dopamine (DAT; dopamine transporter) and seroto

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=multidiscipl::18b0b1afb468aed8a3c4b0a423410e7f