Marco Niello

@geco.iit.it

Postdoc
Genetics of Cognition Laboratory, Neuroscience area, Istituto Italiano di Tecnologia, Genova, Italy

Marco Niello


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https://researchid.co/mniell91

RESEARCH, TEACHING, or OTHER INTERESTS

Neuroscience, Pharmacology, Toxicology and Pharmaceutics
26

Scopus Publications

965

Scholar Citations

17

Scholar h-index

20

Scholar i10-index

Scopus Publications

  • Optimizing cognitive enhancement through dopamine transporter modulation
    Marco Niello, Predrag Kalaba, Anita Cybulska-Klosowicz, Michael Kirchhofer, Iva Spreitzer, Markus Spreitzer, Judith Wackerlig-Damle, Michele Santoni, Claudia Sagheddu, Simone B. Sartori, Karl Ebner, Jana Lubec, Ahmed M. Hussein, Tamara Stojanovic, Nicolas Singewald, Marco Pistis, Gert Lubec, Harald H. Sitte
    Neuropharmacology, 2026
    ) would enhance cognitive function more effectively. To test this, we evaluated a series of R-modafinil analogs using in vitro equilibrium and non-equilibrium measurements, in vivo fast-scan cyclic voltammetry, and highly translational cognitive assays in both healthy and scopolamine-treated rats modelling cognitive impairment. Our findings show that prolonging DAT occupancy improves dopamine signalling and leads to more robust enhancements in cognitive flexibility. Compounds with longer DAT resident time-such as S-MK-26 and (S,S)-CE-158-produced the strongest cognitive effects. These results highlight the importance of DAT binding kinetics in shaping the behavioural actions of psychostimulants and support the development of safer and more effective dopamine-based cognitive enhancers.
  • Cell membrane cholesterol affects serotonin transporter efflux due to altered transporter oligomerization
    Deborah Rudin, Dino Luethi, Marco Niello, Jae-Won Yang, Isabella Burger, Walter Sandtner, Ruth Birner-Gruenberger, Gerhard J. Schütz, Harald H. Sitte
    Molecular Psychiatry, 2026
    The human monoamine transporters (MATs) for serotonin (SERT), dopamine (DAT), and norepinephrine (NET) play a key role in neurotransmission by transporting neurotransmitters from the synaptic cleft back into the neuron. MATs are embedded in the cell membrane’s lipid bilayer, encompassing cholesterol, phospholipids, and sphingolipids as main components. Membrane cholesterol association has been shown for all MATs impacting transporter conformation, substrate affinity, transport velocity, and turnover rates. In the present study, we compared the regulatory impact of cholesterol on the uptake and efflux function, binding affinity, and transporter oligomerization across all three MATs. We observed that cholesterol depletion impairs transporter-mediated uptake in human transporter-transfected HEK293 cells and reduces the binding affinity of all MATs. Electrophysiological investigations in SERT-expressing cells revealed that cholesterol alterations affect the transition of the transporter from the outward to the inward-facing conformation in the presence of substrate. Upon cholesterol depletion, FRET imaging and single molecule microscopy studies indicated altered oligomerization behavior exclusively for SERT. Interestingly, reduction of membrane cholesterol selectively increased amphetamine-induced efflux via SERT, while efflux via DAT and NET was reduced. This effect was diminished in a mutant with reduced PIP 2 binding capacity. Hence, the increased efflux at SERT due to cholesterol depletion appears to depend on the ability of PIP 2 to bind to SERT. Thus, we hypothesize that the interaction profile between cholesterol and MATs may fine-tune the transporter functionality and influence MAT-dependent disorders.
  • Fluorescent PyrAte-(S)-citalopram conjugates enable imaging of the serotonin transporter in living tissue
    Oliver J. V. Belleza, Iakovos Saridakis, Nadja K. Singer, Xavier Westergaard, Sergio Armentia Matheu, Miran Lemmerer, Margaux Riomet, Pedro A. Sánchez-Murcia, Nina Kastner, Stefanie Rukavina, Yi Xiao, Kathrin Jäntsch, Marco Niello, Klaus Schicker, David Sulzer, Leticia González, Nuno Maulide, Harald H. Sitte
    Chemical Science, 2025
    We deploy a new class of fluorophores, PyrAtes, in the first-time use of small-molecule fluorophore–drug conjugates in imaging endogenous SERT ex vivo.
  • Self-experience of a negative event alters responses to others in similar states through prefrontal cortex CRF mechanisms
    Federica Maltese, Giada Pacinelli, Anna Monai, Fabrizio Bernardi, Ana Marta Capaz, Marco Niello, Roman Walle, Noelia de Leon, Francesca Managò, Felix Leroy, Francesco Papaleo
    Nature Neuroscience, 2025
  • Ligand coupling mechanism of the human serotonin transporter differentiates substrates from inhibitors
    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
    Nature Communications, 2024
    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 neurobehavioral disorders, including depression, anxiety, and obsessive-compulsive disorder, trap SERT by blocking the transport cycle. In contrast, illicit drugs of abuse like amphetamines reverse SERT directionality, causing serotonin efflux. Both processes result in increased extracellular serotonin levels. By combining molecular dynamics simulations with biochemical experiments and using a homologous series of serotonin analogues, we uncovered the coupling mechanism between the substrate and the transporter, which triggers the uptake of serotonin. Free energy analysis showed that only scaffold-bound substrates could initiate SERT occlusion through attractive long-range electrostatic interactions acting on the bundle domain. The associated spatial requirements define substrate and inhibitor properties, enabling additional possibilities for rational drug design approaches.
  • Bioisosteric analogs of MDMA: Improving the pharmacological profile?
    Ana Sofia Alberto‐Silva, Selina Hemmer, Hailey A. Bock, Leticia Alves da Silva, Kenneth R. Scott, Nina Kastner, Manan Bhatt, Marco Niello, Kathrin Jäntsch, Oliver Kudlacek, Elena Bossi, Thomas Stockner, Markus R. Meyer, John D. McCorvy, Simon D. Brandt, Pierce Kavanagh, Harald H. Sitte
    Journal of Neurochemistry, 2024
    3,4‐Methylenedioxymethamphetamine (MDMA, ‘ecstasy’) is re‐emerging in clinical settings as a candidate for the treatment of specific neuropsychiatric disorders (e.g. post‐traumatic stress disorder) in combination with psychotherapy. MDMA is a psychoactive drug, typically regarded as an empathogen or entactogen, which leads to transporter‐mediated monoamine release. Despite its therapeutic potential, MDMA can induce dose‐, individual‐, and context‐dependent untoward effects outside safe settings. In this study, we investigated whether three new methylenedioxy bioisosteres of MDMA improve its off‐target profile. In vitro methods included radiotracer assays, transporter electrophysiology, bioluminescence resonance energy transfer and fluorescence‐based assays, pooled human liver microsome/S9 fraction incubations, metabolic stability studies, isozyme mapping, and liquid chromatography coupled to high‐resolution mass spectrometry. In silico methods included molecular docking. Compared with MDMA, all three MDMA bioisosteres (ODMA, TDMA, and SeDMA) showed similar pharmacological activity at human serotonin, dopamine, and norepinephrine transporters (hSERT, hDAT, and hNET, respectively) but decreased agonist activity at 5‐HT2A/2B/2C receptors. Regarding their hepatic metabolism, they differed from MDMA, with N‐demethylation being the only metabolic route shared, and without forming phase II metabolites. In addition, TDMA showed an enhanced intrinsic clearance in comparison to its congeners. Additional screening for their interaction with human organic cation transporters (hOCTs) and plasma membrane monoamine transporter (hPMAT) revealed a weaker interaction of the MDMA analogs with hOCT1, hOCT2, and hPMAT. Our findings suggest that these new MDMA bioisosteres might constitute appealing therapeutic alternatives to MDMA, sparing the primary pharmacological activity at hSERT, hDAT, and hNET, but displaying a reduced activity at 5‐HT2A/2B/2C receptors and alternative hepatic metabolism. Whether these MDMA bioisosteres may pose lower risk alternatives to the clinically re‐emerging MDMA warrants further studies.image
  • Structure-activity relationships of serotonergic 5-MeO-DMT derivatives: insights into psychoactive and thermoregulatory properties
    Pol Puigseslloses, Núria Nadal-Gratacós, Gabriel Ketsela, Nicola Weiss, Xavier Berzosa, Roger Estrada-Tejedor, Mohammad Nazmul Islam, Marion Holy, Marco Niello, David Pubill, Jordi Camarasa, Elena Escubedo, Harald H. Sitte, Raúl López-Arnau
    Molecular Psychiatry, 2024
    Recent studies have sparked renewed interest in the therapeutic potential of psychedelics for treating depression and other mental health conditions. Simultaneously, the novel psychoactive substances (NPS) phenomenon, with a huge number of NPS emerging constantly, has changed remarkably the illicit drug market, being their scientific evaluation an urgent need. Thus, this study aims to elucidate the impact of amino-terminal modifications to the 5-MeO-DMT molecule on its interactions with serotonin receptors and transporters, as well as its psychoactive and thermoregulatory properties. Our findings demonstrated, using radioligand binding methodologies, that all examined 5-MeO-tryptamines exhibited selectivity for 5-HT1AR over 5-HT2AR. In fact, computational docking analyses predicted a better interaction in the 5-HT1AR binding pocket compared to 5-HT2AR. Our investigation also proved the interaction of these compounds with SERT, revealing that the molecular size of the amino group significantly influenced their affinity. Subsequent experiments involving serotonin uptake, electrophysiology, and superfusion release assays confirmed 5-MeO-pyr-T as the most potent partial 5-HT releaser tested. All tested tryptamines elicited, to some degree, the head twitch response (HTR) in mice, indicative of a potential hallucinogenic effect and mainly mediated by 5-HT2AR activation. However, 5-HT1AR was also shown to be implicated in the hallucinogenic effect, and its activation attenuated the HTR. In fact, tryptamines that produced a higher hypothermic response, mediated by 5-HT1AR, tended to exhibit a lower hallucinogenic effect, highlighting the opposite role of both 5-HT receptors. Moreover, although some 5-MeO-tryptamines elicited very low HTR, they still act as potent 5-HT2AR agonists. In summary, this research offers a comprehensive understanding of the psychopharmacological profile of various amino-substituted 5-MeO-tryptamines, keeping structural aspects in focus and accumulating valuable data in the frame of NPS. Moreover, the unique characteristics of some 5-MeO-tryptamines render them intriguing molecules as mixed-action drugs and provide insight within the search of non-hallucinogenic but 5-HT2AR ligands as therapeutical agents.
  • Identification of the potassium-binding site in serotonin transporter
    Eva Hellsberg, Danila Boytsov, Qingyang Chen, Marco Niello, Michael Freissmuth, Gary Rudnick, Yuan-Wei Zhang, Walter Sandtner, Lucy R. Forrest
    Proceedings of the National Academy of Sciences of the United States of America, 2024
    Clearance of serotonin (5-hydroxytryptamine, 5-HT) from the synaptic cleft after neuronal signaling is mediated by serotonin transporter (SERT), which couples this process to the movement of a Na + ion down its chemical gradient. After release of 5-HT and Na + into the cytoplasm, the transporter faces a rate-limiting challenge of resetting its conformation to be primed again for 5-HT and Na + binding. Early studies of vesicles containing native SERT revealed that K + gradients can provide an additional driving force, via K + antiport. Moreover, under appropriate conditions, a H + ion can replace K + . Intracellular K + accelerates the resetting step. Structural studies of SERT have identified two binding sites for Na + ions, but the K + site remains enigmatic. Here, we show that K + antiport can drive substrate accumulation into vesicles containing SERT extracted from a heterologous expression system, allowing us to study the residues responsible for K + binding. To identify candidate binding residues, we examine many cation binding configurations using molecular dynamics simulations, predicting that K + binds to the so-called Na2 site. Site-directed mutagenesis of residues in this site can eliminate the ability of both K + and H + to drive 5-HT accumulation into vesicles and, in patch clamp recordings, prevent the acceleration of turnover rates and the formation of a channel-like state by K + or H + . In conclusion, the Na2 site plays a pivotal role in orchestrating the sequential binding of Na + and then K + (or H + ) ions to facilitate 5-HT uptake in SERT.
  • Mephedrone induces partial release at human dopamine transporters but full release at human serotonin transporters
    Felix P. Mayer, Marco Niello, Simon Bulling, Yuan-Wei Zhang, Yang Li, Oliver Kudlacek, Marion Holy, Fatemeh Kooti, Walter Sandtner, Gary Rudnick, Diethart Schmid, Harald H. Sitte
    Neuropharmacology, 2023
    Mephedrone (4-methylmethcathinone) is a cathinone derivative that is recreationally consumed for its energizing and empathogenic effects. The stimulating properties are believed to arise from the ability of mephedrone to interact with the high-affinity transporters for dopamine (DA) (DAT) and norepinephrine (NET), whereas the entactogenic effect presumably relies on its activity at the serotonin (5-HT) transporter (SERT). Early studies found that mephedrone acts as a releaser at NET, DAT and SERT, and thus promotes efflux of the respective monoamines. Evidence linked drug-induced reverse transport of 5-HT via SERT to prosocial effects, whereas activity at DAT is strongly correlated with abuse liability. Consequently, we sought to evaluate the pharmacology of mephedrone at human (h) DAT and SERT, heterologously expressed in human embryonic kidney 293 cells, in further detail. In line with previous studies, we report that mephedrone evokes carrier-mediated release via hDAT and hSERT. We found this effect to be sensitive to the protein kinase C inhibitor GF109203X. Electrophysiological recordings revealed that mephedrone is actively transported by hDAT and hSERT. However, mephedrone acts as a full substrate of hSERT but as a partial substrate of hDAT. Furthermore, when compared to fully efficacious releasing agents at hDAT and hSERT (i.e. S(+)-amphetamine and para-chloroamphetamine, respectively) mephedrone displays greater efficacy as a releaser at hSERT than at hDAT. In summary, this study provides additional insights into the molecular mechanism of action of mephedrone at hDAT and hSERT.
  • Development and validation of an automated microfluidic perfusion platform for parallelized screening of compounds in vitro
    Francesca R. Brugnoli, Marion Holy, Marco Niello, Julian Maier, Marcus Hanreich, Mario Menzel, Matthias Haberler, Niklas Zulus, Thomas Pickl, Christa Ivanova, Lisa D. Muiznieks, Benjamin Garlan, Harald H. Sitte
    Basic and Clinical Pharmacology and Toxicology, 2023
    Monoamine transporters are of great interest for their role in the physiological activity of the body and their link to mental and behavioural disorders. Currently, static well‐plate assays or manual perfusion systems are used to characterize the interaction of psychostimulants, antidepressants and drugs of abuse with the transporters but still suffer from significant drawbacks caused by lack of automation, for example, low reproducibility, non‐comparability of results. An automated microfluidic platform was developed to address the need for more standardized procedures for cell‐based assays. An automated system was used to control and drive the simultaneous perfusion of 12 channels on a microfluidic chip, establishing a more standardized protocol to perform release assays to study monoamine transporter‐mediated substrate efflux. D‐Amphetamine, GBR12909 (norepinephrine transporter) andp‐chloroamphetamine, paroxetine (serotonin transporter) were used as control compounds to validate the system. The platform was able to produce the expected releasing (D‐Amphetamine,p‐chloroamphetamine) or inhibiting (GBR12909, paroxetine) profiles for the two transporters. The reduction of manual operation and introduction of automated flow control enabled the implementation of stronger standardized protocols and the possibility of obtaining higher throughput by increasing parallelization.
  • Persistent binding at dopamine transporters determines sustained psychostimulant effects
    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
    Proceedings of the National Academy of Sciences of the United States of America, 2023
  • Serotonin-releasing agents with reduced off-target effects
    Felix P. Mayer, Marco Niello, Daniela Cintulova, Spyridon Sideromenos, Julian Maier, Yang Li, Simon Bulling, Oliver Kudlacek, Klaus Schicker, Hideki Iwamoto, Fei Deng, Jinxia Wan, Marion Holy, Rania Katamish, Walter Sandtner, Yulong Li, Daniela D. Pollak, Randy D. Blakely, Marko D. Mihovilovic, Michael H. Baumann, Harald H. Sitte
    Molecular Psychiatry, 2023
  • The metabolic regulator USF-1 is involved in the control of affective behaviour in mice
    Spyros Sideromenos, Maria Nikou, Barbara Czuczu, Nikolas Thalheimer, Anna Gundacker, Orsolya Horvath, Laura Cuenca Rico, Peter Stöhrmann, Marco Niello, Timo Partonen, Daniela D. Pollak
    Translational Psychiatry, 2022
  • A Novel and Selective Dopamine Transporter Inhibitor, (S)-MK-26, Promotes Hippocampal Synaptic Plasticity and Restores Effort-Related Motivational Dysfunctions
    Shima Kouhnavardi, Alev Ecevitoglu, Vladimir Dragačević, Fabrizio Sanna, Edgar Arias-Sandoval, Predrag Kalaba, Michael Kirchhofer, Jana Lubec, Marco Niello, Marion Holy, Martin Zehl, Matthias Pillwein, Judith Wackerlig, Rita Murau, Andrea Mohrmann, Kathryn R. Beard, Harald H. Sitte, Ernst Urban, Claudia Sagheddu, Marco Pistis, Roberto Plasenzotti, John D. Salamone, Thierry Langer, Gert Lubec, Francisco J. Monje
    Biomolecules, 2022
  • Occlusion of the human serotonin transporter is mediated by serotonin-induced conformational changes in the bundle domain
    Ralph Gradisch, Dániel Szöllősi, Marco Niello, Erika Lazzarin, Harald H. Sitte, Thomas Stockner
    Journal of Biological Chemistry, 2022
  • Interaction profiles of central nervous system active drugs at human organic cation transporters 1–3 and human plasma membrane monoamine transporter
    Thomas J. F. Angenoorth, Stevan Stankovic, Marco Niello, Marion Holy, Simon D. Brandt, Harald H. Sitte, Julian Maier
    International Journal of Molecular Sciences, 2021
  • Handling of intracellular k+ determines voltage dependence of plasmalemmal monoamine transporter function
    Shreyas Bhat, Marco Niello, Klaus Schicker, Christian Pifl, Harald H Sitte, Michael Freissmuth, Walter Sandtner
    Elife, 2021
  • α-PPP and its derivatives are selective partial releasers at the human norepinephrine transporter: A pharmacological characterization of interactions between pyrrolidinopropiophenones and uptake1 and uptake2 monoamine transporters
    Julian Maier, Laurin Rauter, Deborah Rudin, Marco Niello, Marion Holy, Diethart Schmid, Joseph Wilson, Bruce E. Blough, Brenda M. Gannon, Kevin S. Murnane, Harald H. Sitte
    Neuropharmacology, 2021
  • Effects of Hydroxylated Mephedrone Metabolites on Monoamine Transporter Activity in vitro
    Marco Niello, Daniela Cintulová, Philip Raithmayr, Marion Holy, Kathrin Jäntsch, Claire Colas, Gerhard F. Ecker, Harald H. Sitte, Marko D. Mihovilovic
    Frontiers in Pharmacology, 2021
  • Role of amino terminal substitutions in the pharmacological, rewarding and psychostimulant profiles of novel synthetic cathinones
    L. Duart-Castells, N. Nadal-Gratacós, M. Muralter, B. Puster, X. Berzosa, R. Estrada-Tejedor, M. Niello, S. Bhat, D. Pubill, J. Camarasa, H.H. Sitte, E. Escubedo, R. López-Arnau
    Neuropharmacology, 2021
  • The Interaction of Organic Cation Transporters 1-3 and PMAT with Psychoactive Substances
    Julian Maier, Marco Niello, Deborah Rudin, Lynette C. Daws, Harald H. Sitte
    Handbook of Experimental Pharmacology, 2021
  • Allosteric Modulation of Neurotransmitter Transporters as a Therapeutic Strategy
    Marco Niello, Ralph Gradisch, Claus Juul Loland, Thomas Stockner, Harald H. Sitte
    Trends in Pharmacological Sciences, 2020
  • para-Trifluoromethyl-methcathinone is an allosteric modulator of the serotonin transporter
    Marco Niello, Daniela Cintulova, Eva Hellsberg, Kathrin Jäntsch, Marion Holy, Leila H. Ayatollahi, Nicholas V. Cozzi, Michael Freissmuth, Walter Sandtner, Gerhard F. Ecker, Marko D. Mihovilovic, Harald H. Sitte
    Neuropharmacology, 2019
  • Pronounced hyperactivity, cognitive dysfunctions, and BDNF dysregulation in dopamine transporter knock-out rats
    Damiana Leo, Ilya Sukhanov, Francesca Zoratto, Placido Illiano, Lucia Caffino, Fabrizio Sanna, Giulia Messa, Marco Emanuele, Alessandro Esposito, Mariia Dorofeikova, Evgeny A. Budygin, Liudmila Mus, Evgenia V. Efimova, Marco Niello, Stefano Espinoza, Tatyana D. Sotnikova, Marius C. Hoener, Giovanni Laviola, Fabio Fumagalli, Walter Adriani, Raul R. Gainetdinov
    Journal of Neuroscience, 2018
  • Neuropharmacology of synthetic cathinones
    Michael H. Baumann, Hailey M. Walters, Marco Niello, Harald H. Sitte
    Handbook of Experimental Pharmacology, 2018
  • Are reprogrammed cells a useful tool for studying dopamine dysfunction in psychotic disorders? A review of the current evidence
    Ulrich Sauerzopf, Roberto Sacco, Gaia Novarino, Marco Niello, Ana Weidenauer, Nicole Praschak‐Rieder, Harald Sitte, Matthäus Willeit
    European Journal of Neuroscience, 2017

RECENT SCHOLAR PUBLICATIONS

  • Optimizing Cognitive Enhancement through Dopamine Transporter Modulation
    M Niello, P Kalaba, A Cybulska-Klosowicz, M Kirchhofer, I Spreitzer, ...
    Neuropharmacology, 110969 , 2026
    2026
  • Cell membrane cholesterol affects serotonin transporter efflux due to altered transporter oligomerization
    D Rudin, D Luethi, M Niello, JW Yang, I Burger, W Sandtner, ...
    Molecular Psychiatry 31 (2), 963-975 , 2026
    2026
    Citations: 5
  • Fluorescent PyrAte-(S)-citalopram conjugates enable imaging of the serotonin transporter in living tissue
    OJV Belleza, I Saridakis, NK Singer, X Westergaard, SA Matheu, ...
    Chemical science 16 (14), 6003-6013 , 2025
    2025
    Citations: 1
  • Self-experience of a negative event alters responses to others in similar states through prefrontal cortex CRF mechanisms
    F Maltese, G Pacinelli, A Monai, F Bernardi, AM Capaz, M Niello, R Walle, ...
    Nature Neuroscience 28 (1), 122-136 , 2025
    2025
    Citations: 18
  • Bioisosteric analogs of MDMA: Improving the pharmacological profile?
    AS Alberto‐Silva, S Hemmer, HA Bock, LA da Silva, KR Scott, N Kastner, ...
    Journal of Neurochemistry 168 (9), 2022-2042 , 2024
    2024
    Citations: 10
  • Structure-activity relationships of serotonergic 5-MeO-DMT derivatives: insights into psychoactive and thermoregulatory properties
    P Puigseslloses, N Nadal-Gratacós, G Ketsela, N Weiss, X Berzosa, ...
    Molecular Psychiatry 29 (8), 2346-2358 , 2024
    2024
    Citations: 23
  • Identification of the potassium-binding site in serotonin transporter
    E Hellsberg, D Boytsov, Q Chen, M Niello, M Freissmuth, G Rudnick, ...
    Proceedings of the National Academy of Sciences of the United States of … , 2024
    2024
    Citations: 11
  • Ligand coupling mechanism of the human serotonin transporter differentiates substrates from inhibitors
    R Gradisch, K Schlögl, E Lazzarin, M Niello, J Maier, FP Mayer, ...
    Nature Communications 15 (1), 417 , 2024
    2024
    Citations: 25
  • Mephedrone induces partial release at human dopamine transporters but full release at human serotonin transporters
    FP Mayer, M Niello, S Bulling, YW Zhang, Y Li, O Kudlacek, M Holy, ...
    Neuropharmacology 240, 109704 , 2023
    2023
    Citations: 4
  • Development and validation of an automated microfluidic perfusion platform for parallelized screening of compounds in vitro
    FR Brugnoli, M Holy, M Niello, J Maier, M Hanreich, M Menzel, ...
    Basic & Clinical Pharmacology & Toxicology 133 (5), 535-547 , 2023
    2023
    Citations: 7
  • Persistent binding at dopamine transporters determines sustained psychostimulant effects
    M Niello, S Sideromenos, R Gradisch, R O´ Shea, J Schwazer, J Maier, ...
    Proceedings of the National Academy of Sciences 120 (6), e2114204120 , 2023
    2023
    Citations: 32
  • Serotonin-releasing agents with reduced off-target effects
    FP Mayer, M Niello, D Cintulova, S Sideromenos, J Maier, Y Li, S Bulling, ...
    Molecular Psychiatry 28 (2), 722-732 , 2023
    2023
    Citations: 43
  • The metabolic regulator USF-1 is involved in the control of affective behaviour in mice
    S Sideromenos, M Nikou, B Czuczu, N Thalheimer, A Gundacker, ...
    Translational Psychiatry 12 (1), 497 , 2022
    2022
    Citations: 6
  • A Novel and Selective Dopamine Transporter Inhibitor, (S) -MK-26, Promotes Hippocampal Synaptic Plasticity and Restores Effort-Related Motivational Dysfunctions
    S Kouhnavardi, A Ecevitoglu, V Dragačević, F Sanna, E Arias-Sandoval, ...
    Biomolecules 12 (7), 881 , 2022
    2022
    Citations: 25
  • 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, HH Sitte, T Stockner
    Journal of Biological Chemistry 298 (3) , 2022
    2022
    Citations: 28
  • Handling of intracellular K+ determines voltage dependence of plasmalemmal monoamine transporter function
    S Bhat, M Niello, K Schicker, C Pifl, HH Sitte, M Freissmuth, W Sandtner
    Elife 10, e67996 , 2021
    2021
    Citations: 33
  • α-PPP and its derivatives are selective partial releasers at the human norepinephrine transporter: a pharmacological characterization of interactions between …
    J Maier, L Rauter, D Rudin, M Niello, M Holy, D Schmid, J Wilson, ...
    Neuropharmacology 190, 108570 , 2021
    2021
    Citations: 28
  • Effects of Hydroxylated Mephedrone Metabolites on Monoamine Transporter Activity in vitro
    M Niello, D Cintulová, P Raithmayr, M Holy, K Jäntsch, C Colas, GF Ecker, ...
    Frontiers in pharmacology 12, 654061 , 2021
    2021
    Citations: 21
  • Role of amino terminal substitutions in the pharmacological, rewarding and psychostimulant profiles of novel synthetic cathinones
    L Duart-Castells, N Nadal-Gratacós, M Muralter, B Puster, X Berzosa, ...
    Neuropharmacology 186, 108475 , 2021
    2021
    Citations: 45
  • Interaction Profiles of Central Nervous System Active Drugs at Human Organic Cation Transporters 1–3 and Human Plasma Membrane Monoamine Transporter
    TJF Angenoorth, S Stankovic, M Niello, M Holy, SD Brandt, HH Sitte, ...
    International Journal of Molecular Sciences 22 (23), 12995 , 2021
    2021
    Citations: 18

MOST CITED SCHOLAR PUBLICATIONS

  • Pronounced hyperactivity, cognitive dysfunctions, and BDNF dysregulation in dopamine transporter knock-out rats
    D Leo, I Sukhanov, F Zoratto, P Illiano, L Caffino, F Sanna, G Messa, ...
    Journal of Neuroscience 38 (8), 1959-1972 , 2018
    2018
    Citations: 254
  • Neuropharmacology of synthetic cathinones
    MH Baumann, HM Walters, M Niello, HH Sitte
    New Psychoactive Substances: Pharmacology, Clinical, Forensic and Analytical … , 2018
    2018
    Citations: 172
  • Allosteric modulation of neurotransmitter transporters as a therapeutic strategy
    M Niello, R Gradisch, CJ Loland, T Stockner, HH Sitte
    Trends in pharmacological sciences 41 (7), 446-463 , 2020
    2020
    Citations: 80
  • Role of amino terminal substitutions in the pharmacological, rewarding and psychostimulant profiles of novel synthetic cathinones
    L Duart-Castells, N Nadal-Gratacós, M Muralter, B Puster, X Berzosa, ...
    Neuropharmacology 186, 108475 , 2021
    2021
    Citations: 45
  • Serotonin-releasing agents with reduced off-target effects
    FP Mayer, M Niello, D Cintulova, S Sideromenos, J Maier, Y Li, S Bulling, ...
    Molecular Psychiatry 28 (2), 722-732 , 2023
    2023
    Citations: 43
  • para-Trifluoromethyl-methcathinone is an allosteric modulator of the serotonin transporter
    M Niello, D Cintulova, E Hellsberg, K Jäntsch, M Holy, LH Ayatollahi, ...
    Neuropharmacology 161, 107615 , 2019
    2019
    Citations: 35
  • Handling of intracellular K+ determines voltage dependence of plasmalemmal monoamine transporter function
    S Bhat, M Niello, K Schicker, C Pifl, HH Sitte, M Freissmuth, W Sandtner
    Elife 10, e67996 , 2021
    2021
    Citations: 33
  • Persistent binding at dopamine transporters determines sustained psychostimulant effects
    M Niello, S Sideromenos, R Gradisch, R O´ Shea, J Schwazer, J Maier, ...
    Proceedings of the National Academy of Sciences 120 (6), e2114204120 , 2023
    2023
    Citations: 32
  • 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, HH Sitte, T Stockner
    Journal of Biological Chemistry 298 (3) , 2022
    2022
    Citations: 28
  • α-PPP and its derivatives are selective partial releasers at the human norepinephrine transporter: a pharmacological characterization of interactions between …
    J Maier, L Rauter, D Rudin, M Niello, M Holy, D Schmid, J Wilson, ...
    Neuropharmacology 190, 108570 , 2021
    2021
    Citations: 28
  • Ligand coupling mechanism of the human serotonin transporter differentiates substrates from inhibitors
    R Gradisch, K Schlögl, E Lazzarin, M Niello, J Maier, FP Mayer, ...
    Nature Communications 15 (1), 417 , 2024
    2024
    Citations: 25
  • A Novel and Selective Dopamine Transporter Inhibitor, (S) -MK-26, Promotes Hippocampal Synaptic Plasticity and Restores Effort-Related Motivational Dysfunctions
    S Kouhnavardi, A Ecevitoglu, V Dragačević, F Sanna, E Arias-Sandoval, ...
    Biomolecules 12 (7), 881 , 2022
    2022
    Citations: 25
  • The interaction of organic cation transporters 1-3 and PMAT with psychoactive substances
    J Maier, M Niello, D Rudin, LC Daws, HH Sitte
    Organic Cation Transporters in the Central Nervous System, 199-214 , 2021
    2021
    Citations: 25
  • Structure-activity relationships of serotonergic 5-MeO-DMT derivatives: insights into psychoactive and thermoregulatory properties
    P Puigseslloses, N Nadal-Gratacós, G Ketsela, N Weiss, X Berzosa, ...
    Molecular Psychiatry 29 (8), 2346-2358 , 2024
    2024
    Citations: 23
  • Effects of Hydroxylated Mephedrone Metabolites on Monoamine Transporter Activity in vitro
    M Niello, D Cintulová, P Raithmayr, M Holy, K Jäntsch, C Colas, GF Ecker, ...
    Frontiers in pharmacology 12, 654061 , 2021
    2021
    Citations: 21
  • Self-experience of a negative event alters responses to others in similar states through prefrontal cortex CRF mechanisms
    F Maltese, G Pacinelli, A Monai, F Bernardi, AM Capaz, M Niello, R Walle, ...
    Nature Neuroscience 28 (1), 122-136 , 2025
    2025
    Citations: 18
  • Interaction Profiles of Central Nervous System Active Drugs at Human Organic Cation Transporters 1–3 and Human Plasma Membrane Monoamine Transporter
    TJF Angenoorth, S Stankovic, M Niello, M Holy, SD Brandt, HH Sitte, ...
    International Journal of Molecular Sciences 22 (23), 12995 , 2021
    2021
    Citations: 18
  • Identification of the potassium-binding site in serotonin transporter
    E Hellsberg, D Boytsov, Q Chen, M Niello, M Freissmuth, G Rudnick, ...
    Proceedings of the National Academy of Sciences of the United States of … , 2024
    2024
    Citations: 11
  • Bioisosteric analogs of MDMA: Improving the pharmacological profile?
    AS Alberto‐Silva, S Hemmer, HA Bock, LA da Silva, KR Scott, N Kastner, ...
    Journal of Neurochemistry 168 (9), 2022-2042 , 2024
    2024
    Citations: 10
  • New Psychoactive Substances
    MH Baumann, HM Walters, M Niello, HH Sitte
    Springer , 2018
    2018
    Citations: 10

INDUSTRY EXPERIENCE

2017-01 to 2017-12: F. Hoffmann-La Roche (Basel, CH)
In vivo fast-scan cyclic voltammetry (FSCV) for detection of fast dopamine dynamics.