Article
Pharmacology & Pharmacy
M. Y. Dron, A. S. Zhigulin, D. B. Tikhonov, O. I. Barygin
Summary: Phenytoin inhibits CI-AMPARs and CP-AMPARs with similar potency, resembling the characteristics of the CI-AMPARs pore blocker pentobarbital. This action suggests a common binding site and mechanism of inhibition, different from classical competitive inhibitors, negative allosteric inhibitors, and CP-AMPARs selective channel blockers.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Pharmacology & Pharmacy
Arseniy S. Zhigulin, Oleg I. Barygin
Summary: In this study, the effects of several drugs on native NMDA receptors in rat hippocampal pyramidal neurons were investigated. It was found that nafamostat, furamidine, and gabexate were able to inhibit the activity of NMDA receptors, while camostat was ineffective. Nafamostat and furamidine showed voltage-dependent inhibition, while gabexate showed voltage-independent inhibition. Nafamostat and furamidine demonstrated a 'foot-in-the-door' mechanism of action. Furamidine, nafamostat, and gabexate have structural similarities to the previously studied diminazene.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Arseniy S. Zhigulin, Oleg I. Barygin
Summary: This study investigated the inhibition mechanism of N-methyl-D-aspartate (NMDA) receptors by sepimostat, an amidine-containing serine protease inhibitor with neuroprotective properties. The results showed that sepimostat inhibits NMDA receptors through a complex voltage-dependent mechanism, with both shallow and deep binding sites. Compared to other structurally-related amidine and guanidine compounds, sepimostat demonstrated similar affinity to the shallow site but lower affinity to the deep site.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Health Care Sciences & Services
Andrea Salmaggi, Cristina Corno, Marta Maschio, Sara Donzelli, Annachiara D'Urso, Paola Perego, Emilio Ciusani
Summary: Perampanel alone exhibits pro-apoptotic effects on glioblastoma cell lines, possibly through increased GluR2/3 expression, while a strong synergistic effect is observed when combined with temozolomide in certain cell lines. Further investigation into the impact of this combination on oncologic outcomes in glioblastoma is warranted.
JOURNAL OF PERSONALIZED MEDICINE
(2021)
Article
Pharmacology & Pharmacy
Arseniy S. Zhigulin, Denis B. Tikhonov, Oleg I. Barygin
Summary: This study investigated the mechanisms of action of various cationic compounds on acid-sensing ion channels (ASICs) and proposed a predictive analysis method for designing new drugs. Among them, nafamostat showed potential application value in the treatment of diseases related to ASIC dysfunction.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2023)
Review
Clinical Neurology
Fabio Perversi, Cinzia Costa, Angelo Labate, Simona Lattanzi, Claudio Liguori, Marta Maschio, Stefano Meletti, Lino Nobili, Francesca Felicia Operto, Andrea Romigi, Emilio Russo, Carlo Di Bonaventura
Summary: Glutamate is the brain's main excitatory neurotransmitter, and an imbalance of excitatory and inhibitory activities may lead to epilepsy or other neurological and psychiatric conditions. AMPA receptors, as the predominant mediator of glutamate-induced excitatory neurotransmission, are a major drug target for modulating brain functions. Perampanel (PER), a selective AMPA antagonist, has shown potential in treating various conditions beyond epilepsy. Evaluating new studies on AMPA antagonism and PER in different neurological conditions, this review aims to provide insights for future research on the use of PER and other AMPA receptor antagonists.
FRONTIERS IN NEUROLOGY
(2023)
Article
Pharmacology & Pharmacy
Maria V. Yelshanskaya, Appu K. Singh, Chamali Narangoda, Robin S. B. Williams, Maria G. Kurnikova, Alexander I. Sobolevsky
Summary: This study characterized the interaction of trans-4-butylcyclohexane carboxylic acid (4-BCCA) with AMPA receptors, revealing it acts as a low-affinity inhibitor at specific sites in the transmembrane domain. The dynamic binding of 4-BCCA at these sites distinguishes it from other inhibitors like perampanel and ion channel blockers. Further research may explore the potential synergistic use of these inhibitors in treating epilepsy and other neurological disorders.
BRITISH JOURNAL OF PHARMACOLOGY
(2022)
Review
Pharmacology & Pharmacy
Fritz Markwardt
Summary: Patch clamp investigations help understand the molecular function of single ion channels. The human P2X7 receptor is an ATP-gated ion channel involved in inflammatory and nociceptive reactions. Specific residues and domains play crucial roles in ion channel function.
BIOCHEMICAL PHARMACOLOGY
(2021)
Article
Neurosciences
Guillermo Gonzalez-Burgos, Takeaki Miyamae, Nita Reddy, Sidney Dawkins, Chloe Chen, Avyi Hill, John Enwright, Bard Ermentrout, David A. Lewis
Summary: In primates, the DLPFC and PPC cortices play crucial roles in the working memory network, with higher frequency oscillations observed in DLPFC. The higher frequency in DLPFC may be attributed to a greater quantity of synapses in the basal dendrites, leading to stronger synaptically evoked excitation and subsequently, increased oscillation frequency and power. These findings provide insights into the mechanisms underlying regional differences in oscillation properties between brain regions.
Article
Neurosciences
Yu Izumisawa, Kenji Ito, Keisuke Sugita, Tazuyo Arai, Hina Kokudo, Naoki Kitamura, Izumi Shibuya
Summary: The study demonstrates that GABA inhibits the AII-induced [Ca2+1i increase through both GABAA and GABAB receptors, with GABAB receptors associated with Gi proteins suppressing Ca2+ entry through VGCCs in SFO neurons.
Review
Neurosciences
Payam Tabaee Damavandi, Francesco Pasini, Gaia Fanella, Giulia Sofia Cereda, Gabriele Mainini, Jacopo C. DiFrancesco, Eugen Trinka, Simona Lattanzi
Summary: Brain tumor-related epilepsy (BTRE) is a common comorbidity in patients with brain neoplasms. Glutamate receptors antagonist Perampanel (PER) may have therapeutic potential in reducing tumor growth and controlling epileptiform activity. Both pre-clinical and clinical studies suggest that PER can be an effective and well-tolerated option for patients with BTRE, but more research is needed for further understanding of its effects on tumor progression.
Article
Biochemistry & Molecular Biology
Shanti Pal Gangwar, Laura Y. Yen, Maria V. Yelshanskaya, Aryeh Korman, Drew R. Jones, Alexander I. Sobolevsky
Summary: The study reveals the role of auxiliary subunits in fine-tuning the structure and function of synaptic complexes, which is crucial for understanding neurotransmission and designing therapeutic drugs for diseases.
NATURE STRUCTURAL & MOLECULAR BIOLOGY
(2023)
Review
Multidisciplinary Sciences
Hamidreza Shaye, Benjamin Stauch, Cornelius Gati, Vadim Cherezov
Summary: GABA(B) receptors play a crucial role in inhibitory neurotransmission in the brain, modulating neuronal signaling and being linked to various neurological disorders. Recent cryo-EM studies have provided detailed insights into the activation mechanism of GABA(B) receptors, offering potential for the discovery of new therapeutic drugs and neuromodulators. The structures of the receptor in different conformational states and bound to various ligands contribute to a comprehensive understanding of the receptor's activation process.
Article
Biochemistry & Molecular Biology
Shanti Pal Gangwar, Laura Y. Yen, Maria V. Yelshanskaya, Aryeh Korman, Drew R. Jones, Alexander I. Sobolevsky
Summary: The cryo-EM structures of GluA2 AMPAR complexes with CNIH2 and γ5 subunits reveal the impact of these auxiliary subunits on the activation and desensitization gating, polyamine block, and inhibition by the antiepileptic drug perampanel. These findings provide important insights into the structure and function of synaptic complexes and have implications for the development of therapeutics.
NATURE STRUCTURAL & MOLECULAR BIOLOGY
(2023)
Article
Neurosciences
Naoki Kogo, Felix B. Kern, Thomas Nowotny, Raymond van Ee, Richard van Wezel, Takeshi Aihara
Summary: In this study, a hybrid system was developed to construct a mutual inhibition circuit between two real-life pyramidal neurons, revealing bistable behavior when the neurons are simultaneously activated. By adding modeled synaptic noise and varying activation strength, the dynamics of the circuit were found to closely resemble the properties of bistable visual perception.
JOURNAL OF NEUROSCIENCE
(2021)
Article
Neurosciences
Vasily A. Morozov, Dmitrii E. Korzhevskii, Denis B. Tihonov, Oleg I. Barygin, Anna V. Isaeva, Maria N. Portsel, Timur D. Vlasov
JOURNAL OF STROKE & CEREBROVASCULAR DISEASES
(2015)
Article
Neurosciences
Tatiana B. Tikhonova, Elina I. Nagaeva, Oleg I. Barygin, Natalia N. Potapieva, Konstantin V. Bolshakov, Denis B. Tikhonov
Article
Neurosciences
Vasily A. Morozov, Dmitrii E. Korzhevskii, Denis B. Tihonov, Oleg I. Barygin, Anna V. Isaeva, Maria N. Portsel, Timur D. Vlasov
JOURNAL OF STROKE & CEREBROVASCULAR DISEASES
(2015)
Article
Biochemistry & Molecular Biology
Oleg I. Barygin, Eugene V. Grishin, Denis B. Tilchonov
Article
Neurosciences
Oleg I. Barygin, Margarita S. Komarova, Tatiana B. Tikhonova, Denis B. Tikhonov
EUROPEAN JOURNAL OF NEUROSCIENCE
(2015)
Article
Chemistry, Organic
Nikita M. Chernov, Roman V. Shutov, Oleg I. Barygin, Mikhail Y. Dron, Galina L. Starova, Nikolay N. Kuz'mich, Igor P. Yakovlev
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2018)
Article
Pharmacology & Pharmacy
Vasilii Y. Shteinikov, Oleg Barygin, Valery E. Gmiro, Denis B. Tikhonov
EUROPEAN JOURNAL OF PHARMACOLOGY
(2019)
Article
Neurosciences
Mikhail Y. Dron, Arseniy S. Zhigulin, Leg Barygin
EUROPEAN JOURNAL OF NEUROSCIENCE
(2020)
Article
Pharmacology & Pharmacy
M. Y. Dron, A. S. Zhigulin, D. B. Tikhonov, O. I. Barygin
Summary: Phenytoin inhibits CI-AMPARs and CP-AMPARs with similar potency, resembling the characteristics of the CI-AMPARs pore blocker pentobarbital. This action suggests a common binding site and mechanism of inhibition, different from classical competitive inhibitors, negative allosteric inhibitors, and CP-AMPARs selective channel blockers.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Pharmacology & Pharmacy
Arseniy S. Zhigulin, Oleg I. Barygin
Summary: In this study, the effects of several drugs on native NMDA receptors in rat hippocampal pyramidal neurons were investigated. It was found that nafamostat, furamidine, and gabexate were able to inhibit the activity of NMDA receptors, while camostat was ineffective. Nafamostat and furamidine showed voltage-dependent inhibition, while gabexate showed voltage-independent inhibition. Nafamostat and furamidine demonstrated a 'foot-in-the-door' mechanism of action. Furamidine, nafamostat, and gabexate have structural similarities to the previously studied diminazene.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2022)
Article
Pharmacology & Pharmacy
Arseniy S. Zhigulin, Denis B. Tikhonov, Oleg I. Barygin
Summary: This study investigated the mechanisms of action of various cationic compounds on acid-sensing ion channels (ASICs) and proposed a predictive analysis method for designing new drugs. Among them, nafamostat showed potential application value in the treatment of diseases related to ASIC dysfunction.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2023)
Review
Chemistry, Medicinal
Dania A. Belinskaia, Mariia A. Belinskaia, Oleg Barygin, Nina P. Vanchakova, Natalia N. Shestakova
Article
Biochemistry & Molecular Biology
Oleg I. Barygin, Margarita S. Komarova, Tatyana B. Tikhonova, Anastasiia S. Korosteleva, Maxim V. Nikolaev, Lev G. Magazanik, Denis B. Tikhonov
Article
Neurosciences
Oleg I. Barygin, Elina I. Nagaeva, Denis B. Tikhonov, Darya A. Belinskaya, Nina P. Vanchakova, Natalia N. Shestakova
Article
Neurosciences
Song Xue, Feng Kong, Yiying Song, Jia Liu
Summary: This study used resting-state functional magnetic resonance imaging to explore the relationship between individual's spontaneous neural activity and social interaction anxiety in a nonclinical population. The results showed that social interaction anxiety was correlated with the fractional amplitude of low-frequency fluctuations in several brain regions, and that emotional intelligence partially mediated this relationship. This study provides evidence for the neural basis of social interaction anxiety in the normal population and highlights the role of emotional intelligence in this anxiety.
NEUROSCIENCE LETTERS
(2024)
Article
Neurosciences
Katsuyuki Yamaguchi, Takuya Yazawa
Summary: This study provides morphometric data on the development of the human medullary arcuate nucleus (AN) by examining the brains of preterm and perinatal infants. The results show that AN morphology demonstrates asymmetry and individual variability during the fetal period. The volume and neuronal number of AN increase exponentially with age, while neuronal density decreases exponentially. The AN may undergo neuron death and neuroblasts production after mid-gestation.
NEUROSCIENCE LETTERS
(2024)
Article
Neurosciences
Zhan Zhou, Weixin Dai, Tianxiao Liu, Min Shi, Yi Wei, Lifei Chen, Yubo Xie
Summary: Studies have shown that propofol-induced neurotoxicity is caused by disruption of mitochondrial fission and fusion, leading to an energy supply imbalance for developing neurons. Healthy mitochondria released by astrocytes can migrate to compromised neurons to mitigate propofol-induced neurotoxicity, but the exact mechanisms involved still need further clarification.
NEUROSCIENCE LETTERS
(2024)
Article
Neurosciences
An Chen, Song Hao, Yongpeng Han, Yang Fang, Yibei Miao
Summary: This study explores the efficacy of two forms of BCI attention training games and finds that physical games may be more effective than video games. The research also offers valuable insights for future game design from a neuroscience perspective.
NEUROSCIENCE LETTERS
(2024)
Article
Neurosciences
Lina Liu, Luran Liu, Yunting Lu, Tianyuan Zhang, Wenting Zhao
Summary: This study reveals that GDI1 serves as a potential diagnostic biomarker for AD and inhibition of GDI1 can attenuate Aβ-induced neurotoxicity. The findings offer new insights for the treatment of AD.
NEUROSCIENCE LETTERS
(2024)
Article
Neurosciences
Zahra Gholami, Ava Soltani Hekmat, Ali Abbasi, Kazem Javanmardi
Summary: This study investigated the effects of alamandine on allodynia in a rat model and found the presence of MrgD receptors in the vlPAG and RVM regions. Microinjection of alamandine resulted in a significant increase in paw withdrawal threshold and could be blocked by an MrgD receptor antagonist. Upregulation of MrgD receptor expression following allodynia induction suggests a potential compensatory mechanism in response to pain.
NEUROSCIENCE LETTERS
(2024)
Article
Neurosciences
Mingliang Xu, Lei Xia, Junjie Li, Yehong Du, Zhifang Dong
Summary: This study found that DHF effectively alleviates sevoflurane-induced cognitive impairment in developing mice by restoring the balance between tau O-GlcNAcylation and phosphorylation. Therefore, DHF has the potential to be a therapeutic agent for treating cognitive impairment associated with anesthetics, such as sevoflurane.
NEUROSCIENCE LETTERS
(2024)
Article
Neurosciences
Tsubasa Mitsutake, Hisato Nakazono, Takanori Taniguchi, Hisayoshi Yoshizuka, Maiko Sakamoto
Summary: The posterior parietal cortex plays a crucial role in postural stability, and transcranial electrical stimulation of this region can modulate physical control responses. This study found that cathodal stimulation significantly decreased joint angular velocity in multiple directions, while there were no significant differences with transcranial random noise stimulation.
NEUROSCIENCE LETTERS
(2024)
Article
Neurosciences
Xishuai Yang, Wei Zhang, Xueli Chang, Zuopeng Li, Runquan Du, Junhong Guo
Summary: This study aims to evaluate the efficacy of low-dose rituximab (RTX) in patients with muscle-specific kinase antibody positive myasthenia gravis (MuSK-MG). The results showed that low-dose RTX treatment led to significant improvements in clinical symptoms and quality of life for patients with MuSK-MG.
NEUROSCIENCE LETTERS
(2024)
Article
Neurosciences
Jian Zhang, Shunyuan Guo, Rong Tao, Fan Wang, Yihong Xie, Huizi Wang, Lan Ding, Yuejian Shen, Xiaoli Zhou, Junli Feng, Qing Shen
Summary: This study established an Alzheimer's disease (AD) model of zebrafish induced by AlCl3 and found that marine-derived plasmalogens (Pls) could alleviate cognitive impairments of AD zebrafish by reversing athletic impairment and altering the expression levels of genes related to oxidative stress, ferroptosis, synaptic dysfunction, and apoptosis.
NEUROSCIENCE LETTERS
(2024)
Article
Neurosciences
Lu Li, Jiaqi Ren, Qi Fang, Liqiang Yu, Jintao Wang
Summary: ICU-AW is a common and severe neuromuscular complication in critically ill patients. Electrophysiological examination is essential for accurate diagnosis and early prediction of the disease. This study aimed to establish and validate an ICU-AW predictive model in SIRS patients, providing a practical tool for early clinical prediction.
NEUROSCIENCE LETTERS
(2024)
Article
Neurosciences
Ahmad Alipour, Roghayeh Mohammadi
Summary: The present study aimed to investigate the separate and combined effects of anodal transcranial direct current stimulation (tDCS) over the primary motor cortex (M1) and left dorsolateral prefrontal cortex (F3) regions on pain relief in patients with type-2 diabetes suffering from neuropathic pain (NP). The results showed that tDCS had the potential to induce pain relief in patients with type-2 diabetes suffering from NP. The mean perceived pain intensity in the posttest was lower in the M1 stimulation group than in the F3 stimulation group. However, more trials with larger sample sizes are necessary to define clinically relevant effects.
NEUROSCIENCE LETTERS
(2024)
Article
Neurosciences
Eduardo J. Fusse, Franciele F. Scarante, Maria A. Vicente, Mariana M. Marrubia, Flavia Turcato, Davi S. Scomparin, Melissa A. Ribeiro, Maria J. Figueiredo, Tamires A. V. Brigante, Francisco S. Guimaraes, Alline C. Campos
Summary: Repeated exposure to psychosocial stress alters the endocannabinoid system and affects brain regions associated with emotional distress. Enhancing the effects of endocannabinoids through pharmacological inhibition induces an anti-stress behavioral effect, possibly mediated by the mTOR signaling pathway.
NEUROSCIENCE LETTERS
(2024)
Article
Neurosciences
Giulia Agostoni, Luca Bischetti, Federica Repaci, Margherita Bechi, Marco Spangaro, Irene Ceccato, Elena Cavallini, Luca Fiorentino, Francesca Martini, Jacopo Sapienza, Mariachiara Buonocore, Michele Francesco D'Incalci, Federica Cocchi, Carmelo Guglielmino, Roberto Cavallaro, Marta Bosia, Valentina Bambini
Summary: This study found a general impairment in humor comprehension in individuals with schizophrenia, with mental jokes being more difficult for both patients and controls. Humor comprehension was closely associated with the patients' overall pragmatic and linguistic profile, while the association with Theory of Mind (ToM) was minimal. Another notable finding was the increased appreciation of humor in individuals with schizophrenia, who rated jokes as funnier than controls did, regardless of whether they were correctly or incorrectly completed. The funniness ratings were not predicted by any measure, suggesting a dimension of humor untied to cognition or psychopathology.
NEUROSCIENCE LETTERS
(2024)
Article
Neurosciences
Xiuping Gong, Qi Li, Yang Liu
Summary: This study demonstrates that Sev targets CREBBP to inhibit ALG13 transcription, leading to hippocampal damage and cognitive impairment.
NEUROSCIENCE LETTERS
(2024)
