Article
Chemistry, Medicinal
Michal Galezowski, Charles-Henry Fabritius, Ullamari Pesonen, Harri Salo, Marta Olszak-Plachta, Klaudia Czerwinska, Justyna Adamczyk, Marcin Krol, Peteris Prusis, Magdalena Sieprawska-Lupa, Maciej Mikulski, Katja Kuokkanen, Radoslaw Obuchowicz, Timo Korjamo, Niina Jalava, Agnieszka Nikiforuk, Mateusz Nowak
Summary: This study presents the discovery and pharmacological characterization of a new series of 6-piperazinyl-7azaindoles, which demonstrate potent antagonism and selectivity against the 5-HT6 receptor. The research primarily focuses on optimizing the lead structure and investigating the structure-activity relationship (SAR) of these compounds. Compound 29 shows significant promise in terms of pharmacological, physicochemical, and ADME properties.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Neurosciences
Chen-Long Yang, Jun-Jie Jing, Si-Yin Fu, Yu-Ling Zhong, Xiu-Zhu Su, Zhong-Mou Shi, Xiao-Zhi Wu, Fei Yang, Guo-Zhong Chen
Summary: This study assessed the impact of ropivacaine-induced seizures on pain hypersensitivity and found that seizures caused pain hypersensitivity for up to 5 days, with enhanced pronociceptive effects on postsurgical pain and acute inflammatory pain. The involvement of spinal 5-HT/5-HT3R signaling was identified as a crucial factor in the pain sensitization caused by seizures, suggesting it as a potential target for precise treatment of local anesthetic toxicity.
Article
Multidisciplinary Sciences
Licong He, Qiaoyu Zhao, Jianzhong Qi, Yifan Wang, Wenyu Han, Zhangcheng Chen, Yao Cong, Sheng Wang
Summary: The cryo-EM structure of human 5-HT6R-Gs heterotrimer reveals key structural determinants for its constitutive activity, which can be targeted for the design of more effective medications for neuropsychiatric disorders. This study provides valuable insights into the molecular basis of constitutive activity and its therapeutic potential.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2023)
Article
Neurosciences
Martha Canto-Bustos, F. Kathryn Friason, Constanza Bassi, Anne-Marie M. Oswald
Summary: Inhibitory microcircuits play a crucial role in regulating cortical responses to sensory stimuli and the formation of sensory representations. This study using optogenetic approach in mice identifies that VIP interneurons mediate a disinhibitory circuit that controls synaptic plasticity during the formation of olfactory representations.
JOURNAL OF NEUROSCIENCE
(2022)
Article
Neurosciences
P. Hayley, C. Tuchek, S. Dalla, J. Borrell, M. D. Murphy, R. J. Nudo, D. J. Guggenmos
Summary: This study aims to investigate the crosstalk between sensorimotor cortical areas and its relationship with recovery. The results suggest that even with damage to the primary motor cortex, sensory stimulation can still elicit neural activity in the motor cortex, and stimulation in the motor cortex can modulate the sensory response in the sensory cortex.
FRONTIERS IN NEUROSCIENCE
(2023)
Article
Clinical Neurology
Anna Castane, Montserrat Cano, Luis Ruiz-Avila, Lluis Miquel-Rio, Pau Celada, Francesc Artigas, Maurizio S. Riga
Summary: This study reports on the potential antipsychotic activity of FPPQ, a dual serotonin receptor antagonist with pro-cognitive properties. In animal experiments, FPPQ was able to reverse symptoms related to schizophrenia and improve brain oscillations. These findings suggest that simultaneous blockade of 5-HT3 and 5-HT6 receptors could be a new direction in antipsychotic drug development.
INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY
(2022)
Article
Behavioral Sciences
Elena Amoruso, Devin B. Terhune, Maria Kromm, Stephen Kirker, Dollyane Muret, Tamar R. Makin
Summary: Studies have shown that amputees and individuals with congenital one-handers can perceive facial touch as arising from their phantom hand, but this perception is not necessarily related to cortical plasticity. This study investigated the influence of demand characteristics on referred sensations reports, and found that the stimulation methods and frequency of referred sensations were similar in amputees and control groups.
Article
Neurosciences
Sebastian M. Frank, Alexandra Otto, Gregor Volberg, Peter U. Tse, Takeo Watanabe, Mark W. Greenlee
Summary: This study demonstrates that tactile learning can transfer to untrained body parts that are coactivated with the trained body part. The researchers found that the transfer of tactile learning was greater from the trained foot to the untrained hand compared to the other way around. The results suggest that the neural mechanisms underlying tactile learning involve somatotopic representation in the primary somatosensory cortex.
JOURNAL OF NEUROSCIENCE
(2022)
Article
Neurosciences
Hui-Xin Qi, Jamie L. Reed, Feng Wang, Christopher L. Gross, Xin Liu, Li Min Chen, Jon H. Kaas
Summary: The study demonstrates significant post-lesion behavioral recovery and cortical reactivation in squirrel monkeys with dorsal column lesions, particularly showing higher magnitude of fMRI responses in the specific training group. The use of specific kinematic measures in hand movements predicts recovery time better than overall task performance success. CBV scans may provide stronger signals for studying cortical reactivation process after sensory deprivations. The reactivation by digit 2 stimulation correlates best with overall behavioral recovery.
Article
Neurosciences
Vincent Dupuy, Matthieu Prieur, Anne Pizzoccaro, Clara Margarido, Emmanuel Valjent, Joel Bockaert, Tristan Bouschet, Philippe Marin, Severine Chaumont-Dubel
Summary: This study demonstrates the expression and localization of serotonin 5-HT6 receptor (5-HT6R) in the mouse brain at different developmental stages. The receptor is found in various brain regions during early development and is preferentially expressed in specific neuron types and astrocytes in adulthood. The localization of the receptor changes during neonatal stages, suggesting its involvement in neuronal differentiation and psychiatric disorders of neurodevelopmental origin.
NEUROBIOLOGY OF DISEASE
(2023)
Review
Neurosciences
Abhishek Banerjee, Bin A. Wang, Jasper Teutsch, Fritjof Helmchen, Burkhard Pleger
Summary: Evolution has shaped the sensory capacities of different species. Rodents rely heavily on the whisker-based somatosensory system for environmental exploration and navigation, while humans rely more on visual and auditory inputs. Recent research has found surprisingly similar processing rules for detecting tactile stimuli and rule learning across species. This article reviews how the brain utilizes these processing rules during tactile learning and discusses the challenges and relevance of cross-species research.
PROGRESS IN NEUROBIOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Dorota Lazewska, Malgorzata Wiecek, Grzegorz Satala, Paulina Chalupnik, Ewa Zeslawska, Ewelina Honkisz-Orzechowska, Monika Tarasek, Gniewomir Latacz, Wojciech Nitek, Ewa Szymanska, Jadwiga Handzlik
Summary: With the increasing number of Alzheimer's disease patients, there is an urgent need for new and effective drugs to slow down or prevent the progression of the disease. 1,3,5-Triazine derivatives have shown potential as potent ligands for the serotonin 5-HT6 receptor (5-HT6R), which is a promising therapeutic target for AD. A new derivative of MST4 compound was designed and tested for its affinity towards 5-HT6R and other receptors. Compound 3 showed promising results as a potent and selective 5-HT6R ligand, making it a potential candidate for further pharmacological studies.
Article
Chemistry, Analytical
Vijai Krishnan, Lauren C. Wade-Kleyn, Ron R. Israeli, Galit Pelled
Summary: Peripheral nerve injury leads to altered activity of inhibitory interneurons, affecting sensory processing. Injury impacts interhemispheric communication, resulting in an overall decrease in inhibitory interneuron activity.
Article
Biochemistry & Molecular Biology
Wuzhou Yang, Harsh Kanodia, Silvia Arber
Summary: The study reveals the anatomical and functional connections between the cortical regions and medulla in mice, showing that distinct cortical regions generate synaptic columns in the lateral medulla that match the positions of postsynaptic neurons tuned to specific forelimb action phases. Additionally, cortical neurons extend collaterals to other subcortical structures through a segregated channel interaction logic. The findings clarify the interaction principles between the cortical and medulla structures.
Article
Pharmacology & Pharmacy
Sahika Guner, Tamila Akhayeva, Charles D. Nichols, Hakan Gurdal
Summary: The interaction between serotonin receptors and epidermal growth factor receptors (EGFR) was investigated in this study, with a focus on their role in vascular constriction. It was found that EGFR, Src, and PI3K play a role in serotonin-induced vasoconstriction, especially in the mesenteric artery. The upstream mediators of EGFR transactivation by serotonin were identified as Ca2+/CaM, Src, and PI3K, with Erk1/2 and Akt activation playing a partial role. Furthermore, different subtypes of serotonin receptors (5-HT2A and 5-HT1B) have varying effects on EGFR transactivation through Src and/or PI3K, with 5-HT2A having a greater impact than 5-HT1B receptors.
BIOCHEMICAL PHARMACOLOGY
(2022)
Article
Developmental Biology
Audrey Touzot, Nuria Ruiz-Reig, Tania Vitalis, Michele Studer
Article
Multidisciplinary Sciences
Ludovic Telley, Subashika Govindan, Julien Prados, Isabelle Stevant, Serge Nef, Emmanouil Dermitzakis, Alexandre Dayer, Denis Jabaudon
Article
Behavioral Sciences
Maria I. Cordero, Dominik A. Moser, Aurelia Manini, Francesca Suardi, Ana Sancho-Rossignol, Raffaella Torrisi, Michel F. Rossier, Francois Ansermet, Alexandre G. Dayer, Sandra Rusconi-Serpa, Daniel S. Schechter
HORMONES AND BEHAVIOR
(2017)
Article
Psychology, Developmental
Sebastien Weibel, Jean-Arthur Micoulaud-Franchi, Laura Brandejsky, Regis Lopez, Paco Prada, Rosetta Nicastro, Stefano Ardu, Alexandre Dayer, Christophe Lancon, Nader Perroud
JOURNAL OF ATTENTION DISORDERS
(2019)
Article
Multidisciplinary Sciences
Sarah Frazer, Julien Prados, Mathieu Niquille, Christelle Cadilhac, Foivos Markopoulos, Lucia Gomez, Ugo Tomasello, Ludovic Telley, Anthony Holtmaat, Denis Jabaudon, Alexandre Dayer
NATURE COMMUNICATIONS
(2017)
Review
Cell Biology
Tania Vitalis, Jean Mariani
NEURAL REGENERATION RESEARCH
(2018)
Article
Clinical Neurology
Z. Csaba, T. Vitalis, C. Charriaut-Marlangue, I. Margaill, B. Coqueran, P. -L. Leger, I. Parente, A. Jacquens, L. Titomanlio, C. Constans, C. Demene, M. D. Santin, S. Lehericy, N. Perriere, F. Glacial, S. Auvin, M. Tanter, J. -F. Ghersi-Egea, H. Adle-Biassette, J. -F. Aubry, P. Gressens, P. Dournaud
Summary: The impairment of blood-brain barrier is involved in various neurological diseases, and reliable imaging of increased BBB permeability is crucial for research. This study introduces a novel approach based on agonist-induced internalization of neuronal G protein-coupled receptor, providing a simple way to assess BBB dysfunction and development in different conditions.
NEUROPATHOLOGY AND APPLIED NEUROBIOLOGY
(2021)
Article
Multidisciplinary Sciences
Quentin Perrenoud, Clemence Leclerc, Helene Geoffroy, Tania Vitalis, Kevin Richetin, Claire Rampon, Thierry Gallopin
Summary: This study compares the electrophysiological and molecular properties of GABAergic interneurons in the hilus and primary sensory cortex of mice. The results suggest that the commonly used features for defining these classes do not have strong discriminative capabilities in the hilus.
Article
Clinical Neurology
Cindy Bokobza, Alice Jacquens, David Guenoun, Blandine Bianco, Anne Galland, Maxime Pispisa, Alexandra Cruz, Manuela Zinni, Valerie Faivre, Anne Roumier, Sophie Lebon, Tania Vitalis, Zsolt Csaba, Tifenn Le Charpentier, Leslie Schwendimann, Pierrette Young-Ten, Vincent Degos, Patricia Monteiro, Pascal Dournaud, Pierre Gressens, Juliette Van Steenwinckel
Summary: Approximately 15 million babies are born prematurely every year, and many of them will face motor and cognitive deficits in their lifetime. Systemic inflammation-induced neuroinflammation is a prominent process of perinatal brain injuries, especially white matter injuries (WMI). Serotonin and its receptors, particularly HTR7, play a significant role in inflammation regulation. The study suggests that targeting HTR7 may serve as an innovative therapeutic strategy to protect the developing brain from preterm brain injuries.
JOURNAL OF NEURAL TRANSMISSION
(2023)
Article
Biochemistry & Molecular Biology
Philippe Bonnin, Tania Vitalis, Leslie Schwendimann, Alexandre Boutigny, Nassim Mohamedi, Valerie C. Besson, Christiane Charriaut-Marlangue
Summary: PJ34 treatment in neonatal mice after hypoxic brain injury showed reduced BBB permeability, decreased astrocyte demise, and tissue loss. These results suggest a protective effect of PJ34 on hypoxic brain injury.
CURRENT ISSUES IN MOLECULAR BIOLOGY
(2021)
Article
Neurosciences
Nicolas Hurni, Marta Kolodziejczak, Ugo Tomasello, Joan Badia, Moritz Jacobshagen, Julien Prados, Alexandre Dayer
Article
Behavioral Sciences
Daniel S. Schechter, Dominik A. Moser, Virginie C. Pointet, Tatjana Aue, Ludwig Stenz, Ariane Paoloni-Giacobino, Wafae Adouan, Aurelia Manini, Francesca Suardi, Marylene Vital, Ana Sancho Rossignol, Maria I. Cordero, Molly Rothenberg, Francois Ansermet, Sandra Rusconi Serpa, Alexandre G. Dayer
BEHAVIOURAL BRAIN RESEARCH
(2017)
Article
Psychiatry
Pierre Cole, Sebastien Weibel, Rosetta Nicastro, Roland Hasler, Alexandre Dayer, Jean-Michel Aubry, Paco Prada, Nader Perroud
PSYCHIATRIA DANUBINA
(2016)
Article
Neurosciences
Tania Vitalis, Luce Dauphinot, Pierre Gressens, Marie-Claude Potier, Jean Mariani, Patricia Gaspar
Article
Psychiatry
Rosetta Nicastro, Paco Prada, Anne-Lise Kung, Virginie Salamin, Alexandre Dayer, Jean-Michel Aubry, Florence Guenot, Nader Perroud
BORDERLINE PERSONALITY DISORDER AND EMOTION DYSREGULATION
(2016)
