Article
Behavioral Sciences
Juan Francisco Rodriguez-Landa, Gabriel Guillen-Ruiz, Fabiola Hernandez-Lopez, Jonathan Cueto-Escobedo, Eduardo Rivadeneyra-Dominguez, Blandina Bernal-Morales, Emma Virginia Herrera-Huerta
Summary: Chrysin is able to attenuate anxiety-like behavior that occurs naturally in rats during the ovarian cycle phases, with its effects mediated by actions on GABA(A) receptors.
BEHAVIOURAL BRAIN RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Veronica Rivi, Cristina Benatti, Joan M. C. Blom, Luca Pani, Nicoletta Brunello, Filippo Drago, Francesco Papaleo, Filippo Caraci, Federica Geraci, Sebastiano Alfio Torrisi, Gian Marco Leggio, Fabio Tascedda
Summary: Cognitive impairment in schizophrenia is a challenging problem that hasn't been solved clinically or pharmacologically. Dysfunctional dysbindin and dopamine receptor D3 have been found to improve cognitive functions, but the underlying molecular mechanisms are not fully understood.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Behavioral Sciences
Huiling Sun, Jinrong Li, Junbao Yan, Bo Sun, Xiaojing Wei, Lin Song, Jianqun Yan
Summary: The absence of dopamine D3 receptors decreases sweet-taste sensitivity and alters the mRNA expression levels of taste-related molecules in mice.
Article
Biochemistry & Molecular Biology
Peiyu Xu, Sijie Huang, Chunyou Mao, Brian E. Krumm, X. Edward Zhou, Yangxia Tan, Xi-Ping Huang, Yongfeng Liu, Dan-Dan Shen, Yi Jiang, Xuekui Yu, Hualiang Jiang, Karsten Melcher, Bryan L. Roth, Xi Cheng, Yan Zhang, H. Eric Xu
Summary: The study reported two cryo-EM structures of human D3R in complex with an inhibitory G protein and bound to D3R-selective agonists PD128907 and pramipexole, revealing distinct agonist binding modes and conformational signatures for ligand-induced receptor activation, providing insights for designing specific ligands to treat CNS diseases targeting the dopaminergic system.
Review
Biochemistry & Molecular Biology
Kathryn Lanza, Christopher Bishop
Summary: Parkinson's Disease (PD) and long-term L-DOPA treatment induce plasticity that contributes to L-DOPA-induced dyskinesia (LID), with the dopamine D3 receptor (D3R) emerging as a promising target in LID management due to its upregulation in LID. D3R undergoes dynamic changes in both PD and LID, and recent genetic and pharmacologic tools have helped clarify its role in LID.
Article
Chemistry, Medicinal
Gui-Long Tian, Chia-Ju Hsieh, Michelle Taylor, Aladdin A. Riad, Robert R. Luedtke, Robert H. Mach
Summary: The difference in the secondary binding site between D2R and D3R has been utilized to design compounds with selectivity for D3R. This study prepared a series of bitopic ligands based on Fallypride to improve the selectivity for D3R using various secondary binding fragments. The results showed that compounds with a small alkyl group containing a heteroatom exhibited improved D3R selectivity.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Medicine, Research & Experimental
Xiaoyan Ding, Mengdie Yang, Ning Wu, Jin Li, Rui Song
Summary: Abnormal fear memory can lead to stress disorders such as PTSD. Therefore, intervention in the formation of abnormal fear memory can be a new strategy for preventing and treating PTSD.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Review
Biochemistry & Molecular Biology
Jeong Joo Kim, Ryan E. Hibbs
Summary: GABAA receptors are important in mediating fast neuronal inhibition in the brain and have rich pharmacology. Recent efforts in structural biology have provided insights into how important drug classes and natural products interact with these receptors, laying a foundation for drug design. The focus has been on subunit assemblies of the receptor found at synapses.
TRENDS IN BIOCHEMICAL SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Pramisha Adhikari, Bing Xie, Ana Semeano, Alessandro Bonifazi, Francisco O. Battiti, Amy H. Newman, Hideaki Yano, Lei Shi
Summary: The study focuses on developing D3R selective agonists over D2R and identifies compound AB04-88 with significant D3R selectivity and G protein bias. The chirality of the primary pharmacophore is key in conferring improved D3R potency, selectivity, and G protein signaling bias.
Article
Biochemistry & Molecular Biology
Boeun Lee, Michelle Taylor, Suzy A. Griffin, Tamara McInnis, Nathalie Sumien, Robert H. Mach, Robert R. Luedtke
Summary: The study showed that N-phenylpiperazine analogs can selectively bind to the human D3 dopamine receptor with significant D3 vs. D2 binding selectivity, potentially leading to the development of pharmacotherapeutics for levodopa-induced dyskinesia in patients with Parkinson's disease.
Article
Pharmacology & Pharmacy
Cristina Cosi, Jean-Claude Martel, Agnes L. Auclair, Ginetta Collo, Laura Cavalleri, Peter Heusler, Ludovic Leriche, Florence Gaudoux, Pierre Sokoloff, Paul C. Moser, Silvia Gatti-McArthur
Summary: F17464 is a new potential antipsychotic with a unique profile, showing high affinity for dopamine receptor subtype 3 and serotonin receptor subtype 1a, while having lower affinity for dopamine receptor subtype 2. It has demonstrated various neurochemistry and behavioral effects, suggesting therapeutic potential for schizophrenia and autism.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Colleen M. Noviello, Jakob Kreye, Jinfeng Teng, Harald Pruess, Ryan E. Hibbs
Summary: Autoantibodies targeting neuronal membrane proteins can cause encephalitis and neurological abnormalities. Cryo-electron microscopy structures reveal the inhibitory mechanisms of these antibodies on neurotransmission.
Article
Neurosciences
Ruotong Li, Yong Wang, Yaxin Yang, Zhongheng Wu, Ling Wang, Guoyi Tang, Jie Yang, Jian Liu
Summary: This study found that GABAA receptor-mediated inhibitory transmission in the avBNST is involved in Parkinson's disease (PD)-related anxiety. Injection of GABAA receptor agonist produced anxiolytic-like effects, inhibited the firing activity of GABAergic neurons and activated the dopaminergic neurons in VTA and serotonergic neurons in DRN, leading to an increase in dopamine and 5-HT release in the amygdala.
Article
Chemistry, Medicinal
Xenia Simeone, Margot Ernst, Thomas Seidel, Joerg Heider, Doris Enz, Serena Monticelli, Florian Daniel Vogel, Filip Koniuszewski, Thierry Langer, Petra Scholze, Vittorio Pace, Margherita Miele
Summary: This study investigates a series of loreclezole derivatives as potential selective drugs targeting alpha 6 beta 3 gamma 2 receptors. The researchers improved the synthetic routes to some previously published ligands, and synthesized a new derivative based on computational docking results. The new loreclezole derivative was found to display stronger modulatory action compared to its counterpart, providing valuable guidance for the future design of selective therapeutics.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Neurosciences
Shi-Zhuang Wei, Xiao-Yu Yao, Chen-Tao Wang, An-Qi Dong, Dan Li, Yu-Ting Zhang, Chao Ren, Jin-Bao Zhang, Cheng-Jie Mao, Fen Wang, Chun-Feng Liu
Summary: Depression is a strong predictor of quality of life in PD patients, but there is lack of clear guidance on its treatment. Pramipexole, a dopamine agonist, has shown clinically useful effects in treating depression in PD along with improvements in bradykinesia. The antidepressive effect of pramipexole is mediated by DRD3 but not DRD2, suggesting the need for novel dopamine agonists specifically targeting DRD3 for future depression treatment in PD.
BRAIN RESEARCH BULLETIN
(2021)
Review
Clinical Neurology
Susana Lopez-Ortiz, Simone Lista, Pedro L. Valenzuela, Jose Pinto-Fraga, Ricardo Carmona, Filippo Caraci, Giuseppe Caruso, Nicola Toschi, Enzo Emanuele, Audrey Gabelle, Robert Nistico, Francesco Garaci, Alejandro Lucia, Alejandro Santos-Lozano
Summary: The study summarizes the relationship between physical activity and the development of Alzheimer's disease, as well as the impact of exercise on patients with Alzheimer's disease. The findings suggest that physical activity can lower the risk of Alzheimer's disease and exercise has positive effects on cognitive function, physical performance, and functional independence.
JOURNAL OF NEUROLOGY
(2023)
Article
Nutrition & Dietetics
Justyna Godos, Marialaura Bonaccio, Wahidah H. Al-Qahtani, Wolfgang Marx, Melissa M. Lane, Gian Marco Leggio, Giuseppe Grosso
Summary: This study aimed to investigate the relationship between consumption of ultra-processed foods (UPFs) and depressive symptoms in younger Italian adults. The results showed that individuals with higher UPF consumption had a higher likelihood of having depressive symptoms. This association remained significant even after adjusting for potential confounding factors, indicating a potential link between UPF consumption and depressive symptoms in younger Italian individuals.
Article
Geriatrics & Gerontology
Justyna Godos, Giuseppe Grosso, Raffaele Ferri, Filippo Caraci, Giuseppe Lanza, Wahidah H. Al-Qahtani, Giuseppe Caruso, Sabrina Castellano
Summary: Studies show that adhering to the Mediterranean diet is associated with better mental and cognitive health, quality of life, and successful aging in middle-age and older adults. The results of this study indicate that individuals who adhere to the Mediterranean diet are less likely to have cognitive impairment and depressive symptoms, and are more likely to have good quality of life, good sleep quality, and successful aging.
EXPERIMENTAL GERONTOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Martina Di Bartolomeo, Tibor Stark, Serena Di Martino, Fabio Arturo Iannotti, Jana Ruda-Kucerova, Giovanni Luca Romano, Martin Kuchar, Samuele Laudani, Petr Palivec, Fabiana Piscitelli, Carsten T. Wotjak, Claudio Bucolo, Filippo Drago, Vincenzo Di Marzo, Claudio D'Addario, Vincenzo Micale
Summary: Adolescent exposure to cannabinoids, such as THC, may increase the risk of psychosis in individuals exposed to perinatal insult. In this study, the researchers examined the effects of peripubertal THC exposure on rats that were also exposed to prenatal methylazoxymethanol acetate (MAM) or perinatal THC (pTHC). They found that the rats exposed to MAM or pTHC exhibited adult phenotypes relevant to schizophrenia, including social withdrawal and cognitive impairment. The researchers also observed changes in gene expression and DNA methylation, suggesting potential molecular mechanisms underlying these effects.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Veronica Rivi, Cristina Benatti, Joan M. C. Blom, Luca Pani, Nicoletta Brunello, Filippo Drago, Francesco Papaleo, Filippo Caraci, Federica Geraci, Sebastiano Alfio Torrisi, Gian Marco Leggio, Fabio Tascedda
Summary: Cognitive impairment in schizophrenia is a challenging problem that hasn't been solved clinically or pharmacologically. Dysfunctional dysbindin and dopamine receptor D3 have been found to improve cognitive functions, but the underlying molecular mechanisms are not fully understood.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Giuseppe Caruso, Claudia G. Fresta, Annamaria Fidilio, Francesca Lazzara, Nicolo Musso, Vincenzo Cardaci, Filippo Drago, Filippo Caraci, Claudio Bucolo
Summary: Age-related macular degeneration (AMD) is a progressive eye disease that irreversibly impairs central vision, but no effective treatment is available. Accumulation of amyloid-beta (A beta) peptide, which is implicated in Alzheimer's disease, has been observed in drusen under the retinal pigment epithelium (RPE), an early sign of AMD. In this study, using an in vitro model of AMD, researchers found that exposure to A beta oligomers decreased cell viability, increased inflammation and oxidative stress, and disrupted tight junction protein in ARPE-19 cells. However, treatment with carnosine, a dipeptide reduced in AMD patients, counteracted these molecular alterations. These findings highlight the potential neuroprotective effects of carnosine in AMD pathology.
Article
Nutrition & Dietetics
Walter Currenti, Justyna Godos, Amer M. Alanazi, Giuseppe Lanza, Raffaele Ferri, Filippo Caraci, Giuseppe Grosso, Fabio Galvano, Sabrina Castellano
Summary: The increase in life expectancy has led to a higher prevalence of age-related neurological diseases, such as cognitive impairment, dementia, and Alzheimer's disease. This study aimed to examine the association between specific categories and subcategories of dietary fats and cognitive status in older Italian adults. The results showed that moderate consumption of certain types of saturated fatty acids and monounsaturated fatty acids was associated with a lower risk of cognitive impairment, while moderate intake of linoleic acid was associated with a higher risk of cognitive impairment.
Article
Biochemistry & Molecular Biology
Giuseppe Caruso, Anna Privitera, Miriam Wissam Saab, Nicolo Musso, Salvatore Maugeri, Annamaria Fidilio, Anna Provvidenza Privitera, Alessandra Pittala, Renaud Blaise Jolivet, Luca Lanzano, Giuseppe Lazzarino, Filippo Caraci, Angela Maria Amorini
Summary: The activity of microglia plays a crucial role in various physiological processes and its imbalance can lead to neurodegenerative disorders. Carnosine, a naturally occurring molecule, has antioxidant and anti-inflammatory activities, and can modulate immune cell response and energy metabolism. Understanding microglia characteristics and their response to environmental challenges is important for therapeutic strategies.
Review
Nutrition & Dietetics
Maria P. Mogavero, Justyna Godos, Giuseppe Grosso, Filippo Caraci, Raffaele Ferri
Summary: This review focuses on the relationship between sleep-wake regulation and appetite control, emphasizing the inhibitory effect of OREXIN, a neurotransmitter, on REM sleep. It further examines the intricate relationship between OREXIN, REM sleep, and appetite regulation, shedding light on their interconnected nature in both physiological conditions and diseases. Understanding this complex relationship is crucial for unraveling the mechanisms underlying sleep-wake patterns and metabolic control, and for developing novel therapeutic approaches to sleep disorders and metabolic conditions associated with OREXIN dysregulation.
Article
Psychiatry
Antonino Messina, Filippo Caraci, Eugenio Aguglia, Maria Salvina Signorelli
Summary: The study revealed a significant relationship between blunted affect and psychomotor slowing, representing the two-faced Janus of immobility. Furthermore, the longer the duration of schizophrenia, the more prominent the aggregation of symptoms in CLB, leading to a specific pattern of immune activation.
ANNALS OF GENERAL PSYCHIATRY
(2023)
Review
Biochemistry & Molecular Biology
Samuele Laudani, Justyna Godos, Federica Martina Di Domenico, Ignazio Barbagallo, Cinzia Lucia Randazzo, Gian Marco Leggio, Fabio Galvano, Giuseppe Grosso
Summary: Hypertension and cardiovascular disease are major global causes of death, and increased oxidative stress and inflammation are associated with endothelial dysfunction. Anthocyanins, with their antioxidant and cardioprotective effects, have garnered significant interest, but their detection in blood serum is limited due to metabolism by gut microbiota. This review summarizes the main findings from clinical studies on the cardioprotective effects of anthocyanins, as well as the role of gut microbiota in their metabolism, bioavailability, and impact on microbiota composition. Further research is needed to clarify which molecules and doses of anthocyanins offer vascular benefits, while considering the crucial role of the microbiota.
Article
Neurosciences
Sebastiano A. Torrisi, Silvia Rizzo, Samuele Laudani, Alessandro Ieraci, Filippo Drago, Gian Marco Leggio
Summary: Several studies have shown that chronic stress has a negative effect on recognition memory, but the effects of acute stress on this cognitive ability have not been well studied. This study aimed to investigate the impact of acute stress on recognition memory consolidation in a sex-dependent manner. The results showed that acute stress did not affect memory performance in male and female mice immediately after training, but it altered memory performance after a 24-hour delay, with sex-dependent effects.
NEUROBIOLOGY OF STRESS
(2023)
Article
Chemistry, Medicinal
Salvatore Giunta, Agata Grazia D'Amico, Grazia Maugeri, Claudio Bucolo, Giovanni Luca Romano, Settimio Rossi, Chiara M. Eandi, Elisabetta Pricoco, Velia D'Agata
Summary: In the area of drug discovery, repurposing strategies are used to discover new uses of approved drugs. In this study, the effects of DMF on early injury associated with diabetic retinopathy were investigated. The results showed that DMF can counteract the inflammatory process and the oxidative response in diabetic retinopathy.
Article
Clinical Neurology
Hannah Meijs, Helena Voetterl, Alexander T. Sack, Hanneke van Dijk, Bieke De Wilde, Jan Van Hecke, Peter Niemegeers, Evian Gordon, Jurjen J. Luykx, Martijn Arns
Summary: This study used a polygenic score (PGS) and electroencephalography (EEG) data analysis to identify potential predictors for treatment outcomes in major depressive disorder (MDD). The results suggest the existence of a stable EEG network related to antidepressant-response that has potential as a predictor for MDD treatment, particularly in the case of venlafaxine.
EUROPEAN NEUROPSYCHOPHARMACOLOGY
(2024)