Article
Pharmacology & Pharmacy
Francesco Petragnano, Irene Fasciani, Clotilde Mannoury la Cour, Benjamin di Cara, Gabriella Aloisi, Marco Carli, Shivakumar Kolachalam, Mario Rossi, Francesco Marampon, Marco Scarselli, Mark J. Millan, Roberto Maggio
Summary: This study investigates the affinity and activation of (+)-4-Propyl-9-hydroxynaphthoxazine on various monoamine receptors. It is found to have high affinity for hD(4.4), h5-HT1A, and h5-HT7 receptors, as well as hD(3) and hD(2L) receptors. It also strongly activates dopamine hD(3)-hD(2L) heterodimers. These findings are important for interpreting PET studies and may have implications for the treatment of Parkinson's disease and other disorders.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2022)
Article
Chemistry, Medicinal
Francisco O. Battiti, Saheem A. Zaidi, Vsevolod Katritch, Amy Hauck Newman, Alessandro Bonifazi
Summary: This study investigates the role of regio- and stereochemistry in cyclic aliphatic linkers tethering pharmacophores targeting dopamine D-2 and D-3 receptors, introducing potent and selective agonists while modulating subtype selectivity in a stereospecific manner. The findings demonstrate a novel approach to modulate dopaminergic ligand pharmacology and introduce a new class of optically active cyclic linkers that can be utilized in expanding bitopic drug design towards other GPCRs. Extensive molecular docking studies support the pharmacological observations presented in the study.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Prashant Donthamsetti, David B. Konrad, Belinda Hetzler, Zhu Fu, Dirk Trauner, Ehud Y. Isacoff
Summary: G protein-coupled receptors (GPCRs) are common drug discovery targets, but the complexity of in vivo receptor activation has hindered drug development. Photopharmacology offers the potential to control drug action using light. Recent advances include a photoswitchable allosteric agonist that selectively activates receptors.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2021)
Article
Psychiatry
Stanislav V. Ivanov, Anatoly B. Smulevich, Evgeniya I. Voronova, Kausar K. Yakhin, Tangyul Z. Beybalaeva, Alena A. Katok
Summary: The study evaluated the initial effects of cariprazine in schizophrenia patients with predominantly negative symptoms, showing improvement in 75% of patients within 28 days of treatment. Significant reductions in negative symptoms were observed, suggesting an early effect of cariprazine on negative symptoms in some patients.
FRONTIERS IN PSYCHIATRY
(2022)
Review
Psychiatry
Borjanka Batinic, Ivan Ristic, Milica Zugic, David S. Baldwin
Summary: Cariprazine is a medication approved for the treatment of schizophrenia, bipolar disorder, and major depressive disorder, showing efficacy across a wide array of symptoms and a favorable side effect profile. It may be a drug of choice for patients with predominant negative and cognitive symptoms of schizophrenia. Its longer half-life and delayed time to relapse in patients with schizophrenia compared to other antipsychotics suggest potential advantages in clinical practice.
FRONTIERS IN PSYCHIATRY
(2021)
Article
Pharmacology & Pharmacy
Kwang-Hyun Hur, Seong-Eon Kim, Shi-Xun Ma, Bo-Ram Lee, Yong-Hyun Ko, Jee-Yeon Seo, Seon-Kyung Kim, Young-Jung Kim, Su-Jeong Sung, Youyoung Lee, Young Hoon Jung, Yong-Sup Lee, Seok-Yong Lee, Choon-Gon Jang
Summary: The study demonstrates that methoxphenidine exhibits addictive and schizophrenia-like behaviors, inducing neurochemical changes in brain regions associated with these behaviors. These findings suggest that methoxphenidine could be utilized in developing animal disease models and calls for legal restrictions on its recreational use.
BRITISH JOURNAL OF PHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Hana Brozka, Daniela Alexova, Dominika Radostova, Martina Janikova, Branislav Krajcovic, Stepan Kubik, Jan Svoboda, Ales Stuchlik
Summary: Treatment with quinpirole reduces immediate early gene expression in the hippocampus of rats during stereotypical checking, potentially affecting the plasticity-related activity in this brain region.
Article
Clinical Neurology
D'bora Dreher Nabinger, Stefani Altenhofen, Alexis Buatois, Amanda Facciol, Julia Vasconcellos Peixoto, Julia Maria Kuhl da Silva, Diptendu Chatterjee, Gabriel Rubensam, Robert Gerlai, Carla Denise Bonan
Summary: This study investigated the effects of the dopamine D2/D3 receptor agonist quinpirole on the behavior, brain-derived neurotrophic factor (BDNF), and neurotransmitter levels in adult zebrafish. The results showed that quinpirole administration caused decreased locomotor activity, increased anxiety-like behaviors, memory impairment, and stereotypic swimming in zebrafish. Furthermore, quinpirole treatment also decreased the number of BDNF-immunoreactive cells and altered glutamate and serotonin levels in the zebrafish brain. These findings suggest that quinpirole administration in adult zebrafish can be a useful tool for studying the mechanisms underlying neurological disorders related to the dopaminergic system.
PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY
(2023)
Article
Cell Biology
Carlos Pereira Martins, Rodrigo Sebben Paes, Gabriela Mantovani Baldasso, Eduarda Gomes Ferrarini, Rahisa Scussel, Rubya Pereira Zaccaron, Ricardo Andrez Machado-de-Avila, Paulo Cesar Lock Silveira, Rafael Cypriano Dutra
Summary: The dopamine receptor agonist pramipexole was found to alleviate pain and mood dysfunction in a fibromyalgia mouse model, and restore dopamine levels in the spinal cord and frontal cortex. Additionally, pramipexole exhibited antioxidant effects and reduced oxidative damage.
NEURAL REGENERATION RESEARCH
(2022)
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
Biochemistry & Molecular Biology
Kinga Salat, Anna Furgala-Wojas
Summary: Fibromyalgia, characterized by lowered pain threshold and mood disorders, poses a challenge for diagnosis and treatment. This study evaluated the effects of two drugs on fibromyalgia symptoms in mice, showing pain reduction and distinct emotional effects.
Article
Multidisciplinary Sciences
Mifuka Ouchi, Takeya Kitta, Hiroki Chiba, Madoka Higuchi, Mio Togo, Yui Abe-Takahashi, Nobuo Shinohara
Summary: This study found that rotigotine can suppress an overactive bladder and improve the micturition reflex in a rat model of Parkinson's disease, suggesting its potential clinical application.
SCIENTIFIC REPORTS
(2022)
Article
Biochemistry & Molecular Biology
Nermin Eissa, Karthikkumar Venkatachalam, Petrilla Jayaprakash, Markus Falkenstein, Mariam Dubiel, Annika Frank, David Reiner-Link, Holger Stark, Bassem Sadek
Summary: The study demonstrated that the novel multi-targeting ligand ST-2223 showed promising effects in alleviating ASD-related repetitive behaviors and improving anxiety levels. Reference drugs memantine and aripiprazole also exhibited similar effects, supporting the potential of ST-2223 as a pharmacological intervention for ASD behaviors.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Medicinal
Nermin Eissa, Karthikkumar Venkatachalam, Petrilla Jayaprakash, Priya Yuvaraju, Markus Falkenstein, Holger Stark, Bassem Sadek
Summary: The study demonstrates the significant mitigating effects of a multiple-active H3R/D2R/D3R antagonist on social deficits related to ASD.
Article
Neurosciences
Kendall Woodlief, Mia I. Allen, Jeremy C. Cornelissen, Matthew L. Banks, Amy Hauck Newman, Michael A. Nader
Summary: Recent studies suggest that dopamine D3 receptors (D3R) may be a therapeutic target for opioid use disorders (OUD). This study examined the effects of the D3R partial agonist (+/-)VK4-40 and the D3R-selective antagonist (+/-)VK4-116, compared to the mu-opioid receptor antagonist naltrexone (NTX), in nonhuman primate models of OUD and antinociception. The results suggest that (+/-)VK4-40 may be a novel pharmacotherapy for OUD.
NEUROPSYCHOPHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
L. Cavalleri, E. Merlo Pich, M. J. Millan, C. Chiamulera, T. Kunath, P. F. Spano, G. Collo
MOLECULAR PSYCHIATRY
(2018)
Editorial Material
Cell Biology
Ginetta Collo, Emilio Merlo Pich
NEURAL REGENERATION RESEARCH
(2018)
Article
Neurosciences
Cristiano Chiamulera, Marzia di Chio, Laura Cavalleri, Marco Venniro, Laura Padovani, Ginetta Collo
Article
Neurosciences
Ginetta Collo, Laura Cavalleri, Federica Bono, Cristina Mora, Stefania Fedele, Roberto William Invernizzi, Massimo Gennarelli, Giovanna Piovani, Tilo Kunath, Mark J. Millan, Emilio Merlo Pich, PierFranco Spano
Article
Pharmacology & Pharmacy
Ginetta Collo, Laura Cavalleri, Michele Zoli, Uwe Maskos, Emiliangelo Ratti, Emilio Merlo Pich
FRONTIERS IN PHARMACOLOGY
(2018)
Article
Biochemistry & Molecular Biology
Cinzia Cameli, Elena Bacchelli, Maria De Paola, Giuliano Giucastro, Stefano Cifiello, Ginetta Collo, Maria Michela Cainazzo, Luigi Alberto Pini, Elena Maestrini, Michele Zoli
EUROPEAN JOURNAL OF HUMAN GENETICS
(2018)
Article
Multidisciplinary Sciences
Stefania Fedele, Ginetta Collo, Katharina Behr, Josef Bischofberger, Stephan Mueller, Tilo Kunath, Klaus Christensen, Anna Lisa Guendner, Martin Graf, Ravi Jagasia, Verdon Taylor
SCIENTIFIC REPORTS
(2017)
Article
Neurosciences
Ginetta Collo, Laura Cavalleri, Cristiano Chiamulera, Emilio Merlo Pich
Article
Neurosciences
Ginetta Collo, Laura Cavalleri, Cristiano Chiamulera, Emilio Merlo Pich
Article
Pharmacology & Pharmacy
Carlo Matera, Federica Bono, Silvia Pelucchi, Ginetta Gollo, Leonardo Bontempi, Cecilia Gotti, Michele Zoli, Marco De Amici, Cristina Missale, Chiara Fiorentini, Clelia Dallanoce
BIOCHEMICAL PHARMACOLOGY
(2019)
Review
Neurosciences
Ginetta Collo, Armida Mucci, Giulia M. Giordano, Emilio Merlo Pich, Silvana Galderisi
FRONTIERS IN NEUROSCIENCE
(2020)
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
Multidisciplinary Sciences
Glenn Dallerac, Xia Li, Pierre Lecouflet, Nadege Morisot, Silvia Sacchi, Rachel Asselot, Thu Ha Pham, Brigitte Potier, David J. G. Watson, Staffan Schmidt, Gregoire Levasseur, Pascal Fossat, Andrey Besedin, Jean-Michel Rivet, Joseph T. Coyle, Ginetta Collo, Loredano Pollegioni, Jan Kehr, Micaela Galante, Kevin C. Fone, Alain M. Gardier, Thomas Freret, Angelo Contarino, Mark J. Millan, Jean-Pierre Mothet
Summary: The study reveals the crucial role of D-serine in regulating glutamatergic transmission in the prefrontal cortex through D1 and D3 receptors, which are essential components in the dopamine-glutamate dialogue. In vivo microdialysis showed that D1 and D3 receptors modulate extracellular levels and activity of D-serine in the PFC via the cAMP/PKA signaling cascade. Furthermore, D-serine is necessary for the cognitive enhancement by D3 receptor blockade, as demonstrated in novel object recognition memory test.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2021)
Correction
Neurosciences
Ginetta Collo, Armida Mucci, Giulia M. M. Giordano, Emilio Merlo Pich, Silvana Galderisi
FRONTIERS IN NEUROSCIENCE
(2021)
Article
Pharmacology & Pharmacy
Rosamaria Orlando, Roxana Paula Ginerete, Laura Cavalleri, Vincenza Aliperti, Tiziana Imbriglio, Giuseppe Battaglia, Anna Rita Zuena, Ferdinando Nicoletti, Emilio Merlo Pich, Ginetta Collo
Summary: The combination of L-acetylcarnitine (LAC) and L-methylfolate (MF) has a synergistic effect in the treatment of depression caused by chronic stress. It improves symptoms by reducing immobility time, increasing BDNF protein levels, and enhancing mGlu2 protein levels. Additionally, LAC and MF exert their effects through mechanisms such as acetylation of NF kappa B p65, and promote the development of dopamine neurons in cultured hiPSCs.
FRONTIERS IN PHARMACOLOGY
(2022)
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)