Review
Behavioral Sciences
Sarah Kittel-Schneider, Boris B. Quednow, Anna Linda Leutritz, Rhiannon McNeill, Andreas Reif
Summary: This review focuses on analyzing the association of maternal ADHD with pregnancy, birth outcomes, early parent-child interaction, and child development in the first 3 years, as well as the impact of parental ADHD on early parent-child interaction and child development. Additionally, it also reviews the risks of stimulant and non-stimulant treatment for ADHD in pregnancy and lactation.
NEUROSCIENCE AND BIOBEHAVIORAL REVIEWS
(2021)
Article
Chemistry, Medicinal
Anil Karbhari Shinde, Rajesh Kumar Badange, Veena Reballi, Pramod Kumar Achanta, Kumar Bojja, Sravanthi Manchineella, Nageswara Rao Muddana, Ramkumar Subramanian, Raghava Choudary Palacharla, Vijay Benade, Pradeep Jayarajan, Jagadeesh Babu Thentu, Bujji Babu Lingavarapu, Sivasekhar Yarra, Narendra Kagita, Mallikarjuna Rao Doguparthi, Abdul Rasheed Mohammed, Ramakrishna Nirogi
Summary: Compound 45 e, developed through a series of chemical optimizations, has been identified as a potent and selective H3R inverse agonist, with robust efficacy in fighting against dipsogenia induced by histamine. It has shown good oral exposure and half-life, along with significant effects in object recognition task and acetylcholine levels, suggesting potential for further treatment of cognitive disorders associated with Alzheimer's disease.
Article
Pharmacology & Pharmacy
Joachim Neumann, Rafaela Voss, Ulrich Laufs, Christian Werner, Ulrich Gergs
Summary: Histamine exerts cAMP-dependent positive inotropic effects (PIE) on the left and right atria of transgenic mice which overexpress the human H-2-receptor, with PDE 3 and PDE 4 regulating the effects on inotropic response, while PDE 2 and PDE 4 play a role in regulating the positive chronotropic effects on heart beat rate.
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Nele Wagener, Wolfgang Lehmann, Lukas Weiser, Katharina Jaeckle, Pietro Di Fazio, Arndt F. Schilling, Kai O. Boeker
Summary: Attention deficit hyperactivity disorder (ADHD) is a common mental disorder in children, young people and adults. The abuse of ADHD-related drugs is increasing, and this study found that three cognitive enhancers negatively influence the differentiation and migration of bone-forming cells.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Thomas J. F. Angenoorth, Stevan Stankovic, Marco Niello, Marion Holy, Simon D. Brandt, Harald H. Sitte, Julian Maier
Summary: The study highlights the interactions between psychoactive substances and SLC6 monoamine transporters, as well as the potential interactions with human OCTs and hPMAT. The findings suggest the importance of investigating these interactions for regulating monoamine concentrations and drug clearance in the body.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Editorial Material
Pediatrics
Susan J. Keam
Summary: Pitolisant (WAKIX) is a histamine H-3 receptor antagonist/inverse agonist developed by Bioprojet Pharma and approved for use in adults with narcolepsy with or without cataplexy in the EU and USA. In February 2023, based on clinical data in patients aged 6 to < 18 years, pitolisant received its first approval in adolescents and children from the age of 6 years for the treatment of narcolepsy with or without cataplexy in the EU. This article provides an overview of the milestones in the development of pitolisant leading to this pediatric first approval.
Review
Chemistry, Medicinal
Joachim Neumann, Britt Hofmann, Uwe Kirchhefer, Stefan Dhein, Ulrich Gergs
Summary: Histamine can affect cardiac contraction force and beating rate in mammals, including humans, but there are significant differences between species and regions. The mammalian heart produces and contains histamine, which may have autocrine or paracrine effects. Cardiomyocytes express histamine receptors, including H-1 and H-2, but their functional role is not fully understood. This review aims to identify gaps in knowledge and highlight the potential of histamine H-1 receptors as therapeutic targets in the human heart, particularly in diseases.
Article
Biochemistry & Molecular Biology
Kamil J. Kuder, Magdalena Kotanska, Katarzyna Szczepanska, Kamil Mika, David Reiner-Link, Holger Stark, Katarzyna Kiec-Kononowicz
Summary: Researchers designed a series of dual acting histamine H-3 receptor ligands, with compound 16 demonstrating strong antioxidant properties and moderate hH(3)R affinity. These compounds could serve as potential tools for treating neurological disorders.
Article
Clinical Neurology
Nathaniel F. Watson, Craig W. Davis, Donna Zarycranski, Ben Vaughn, Jeffrey M. Dayno, Yves Dauvilliers, Jean-Charles Schwartz
Summary: Pitolisant treatment showed onset of clinical response for excessive daytime sleepiness and/or cataplexy within the first 2-3 weeks in patients with narcolepsy, with significant improvement in symptoms observed through the end of treatment.
Article
Neurosciences
Ramakrishna Nirogi, Vijay Benade, Saivishal Daripelli, Ramkumar Subramanian, Venkatesh Kamuju, Gopinadh Bhyrapuneni, Nageswara Rao Muddana, Venkat Reddy Mekala, Surendra Petlu, Pradeep Jayarajan, Rajesh Badange, Anil Shinde, Venkat Jasti
Summary: Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor inverse agonist with demonstrated efficacy in modulating wakefulness and anti-cataplectic effects, making it a potential treatment for sleep-related disorders. Preclinical studies have shown that Samelisant has high binding affinity for both human and rat H3 receptors, and can modulate neurotransmitter levels in the brain to promote wakefulness and reduce cataplexy.
PSYCHOPHARMACOLOGY
(2021)
Review
Behavioral Sciences
Nathalie Brunkhorst-Kanaan, Berit Libutzki, Andreas Reif, Henrik Larsson, Rhiannon V. McNeill, Sarah Kittel-Schneider
Summary: Studies have shown an increased risk of accidents and injuries in individuals with ADHD across different age groups, with medication appearing to be effective in reducing this risk. However, there is a lack of direct comparison studies on accident/injury types and medication effects in different age groups or in older age. Furthermore, comorbidities associated with ADHD, such as substance abuse, seem to further elevate the risk of accidents/injuries.
NEUROSCIENCE AND BIOBEHAVIORAL REVIEWS
(2021)
Article
Pharmacology & Pharmacy
Zsolt Nemethy, Bela Kiss, Natasha Lethbridge, Paul Chazot, Tunde Hajnik, Attila Toth, Laszlo Detari, Eva Schmidt, Andras Czurko, Diana Kostyalik, Vilmos Olah, Istvan Hernadi, Ottilia Balazs, E. Sylvester Vizi, Istvan Ledneczki, Sandor Maho, Viktor Roman, Balazs Lendvai, Gyorgy Levay
Summary: The histamine H-3 receptor is a promising target for treating cognitive deficits. In this study, the authors investigated the in vitro and in vivo characteristics of RGH-235, a new H-3 receptor antagonist/inverse agonist developed by Gedeon Richter Plc. They found that RGH-235 displayed high affinity to H-3 receptors and showed procognitive effects in rodent and primate tests, as well as in models of attention deficit hyperactive disorder (ADHD). The results suggest that antagonism/inverse agonism of H-3 receptors may have beneficial cognitive effects.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2022)
Article
Chemistry, Medicinal
Steffen Pockes, Katharina Tropmann
Summary: Radioligands have been a powerful tool in investigating the histamine H-2 receptor (H2R) and its functions, with tritium labeling primarily used for in vitro assays and carbon-14 labeling preferred for metabolic studies. The recent development of a G protein-biased radioligand represents a step forward in understanding the potentially unknown role of H2R in the central nervous system through future studies.
FUTURE MEDICINAL CHEMISTRY
(2021)
Article
Immunology
Xiaoyi Zhao, Shady Younis, Hui Shi, Shu Hu, Amin Zia, Heidi H. Wong, Eileen E. Elliott, Tiffany Chang, Michelle S. Bloom, Wei Zhang, Xiangyang Liu, Tobias Volker Lanz, Orr Sharpe, Zelda Z. Love, Qian Wang, William H. Robinson
Summary: This study investigated the role of mast cells in osteoarthritis (OA) through RNA-Seq analysis and pharmacological blockade of histamine activity. The findings suggest that mast cells in OA synovium are correlated with disease severity, and inhibiting histamine activity has the potential to improve OA outcome.
CLINICAL IMMUNOLOGY
(2022)
Article
Neurosciences
Chiara Toschi, Mona El-Sayed Hervig, Parisa Moazen, Maximilian G. Parker, Jeffrey W. Dalley, Ulrik Gether, Trevor W. Robbins
Summary: This study found that high impulsive rats showed superior performance and earned more reinforcers on tasks requiring rapid responding, unlike low impulsive rats. Dopaminergic agents like methylphenidate and amphetamine, as well as the alpha-2a adrenoceptor antagonist atipamezole, improved performance on short inter-trial interval trials and increased impulsivity, mimicking the behavioral profile of high impulsive rats. In contrast, the noradrenergic agents atomoxetine and phenylephrine impaired performance on short inter-trial interval trials and decreased impulsivity, resembling the behavioral profile of low impulsive rats.
PSYCHOPHARMACOLOGY
(2021)
Article
Pharmacology & Pharmacy
Pierre Morissette, Hillary K. Regan, Kevin Fitzgerald, Sylvain Bernasconi, Pamela Gerenser, Jeffrey Travis, Patrick Fanelli, Frederick Sannajust, Christopher P. Regan
JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS
(2015)
Article
Gastroenterology & Hepatology
Christopher P. Regan, Pierre Morissette, Hillary K. Regan, Jeffery J. Travis, Pamela Gerenser, Jianzhong Wen, Kevin Fitzgerald, Shaun Gruver, Joseph J. DeGeorge, Frederick J. Sannajust
Article
Pharmacology & Pharmacy
P. Morissette, C. Regan, K. Fitzgerald, P. Gerenser, J. Travis, S. Wang, P. Fanelli, F. Sannajust
JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS
(2016)
Article
Pharmacology & Pharmacy
Christopher P. Regan, Gary L. Stump, Theodore J. Detwiler, Li Chen, Hillary K. Regan, David B. Gilberto, Joseph J. DeGeorge, Frederick J. Sannajust
JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS
(2016)
Article
Chemistry, Medicinal
Douglas C. Beshore, Nigel J. Liverton, Charles J. McIntyre, Christopher F. Claiborne, Brian Libby, J. Christopher Culberson, Joseph J. Salata, Christopher P. Regan, Joseph J. Lynch, Laszlo Kiss, Robert H. Spencer, Stephanie A. Kane, Rebecca B. White, Suzie Yeh, George D. Hartman, Christopher J. Dinsmore
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2010)
Article
Chemistry, Medicinal
Austin Chen, Louis-Charles Campeau, Elizabeth Cauchon, Amandine Chefson, Yves Ducharme, Daniel Dube, Jean-Pierre Falgueyret, Pierre-Andre Fournier, Sebastien Gagne, Erich Grimm, Yongxin Han, Robert Houle, Jing-Qi Huang, Patrick Lacombe, Sebastien Laliberte, Jean-Francois Levesque, Susana Liu, Dwight MacDonald, Bruce Mackay, Dan McKay, M. David Percival, Chris Regan, Hillary Regan, Rene St-Jacques, Sylvie Toulmond
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2011)
Article
Cardiac & Cardiovascular Systems
Behzad B. Pavri, Howard E. Greenberg, Walter K. Kraft, Nicole Lazarus, Joseph J. Lynch, Joseph J. Salata, Mark T. Bilodeau, Christopher P. Regan, Gary Stump, Li Fan, Anish Mehta, John A. Wagner, David E. Gutstein, Daniel Bloomfield
CIRCULATION-ARRHYTHMIA AND ELECTROPHYSIOLOGY
(2012)
Article
Cardiac & Cardiovascular Systems
Joseph J. Lynch, Theodore J. Detwiler, Stefanie A. Kane, Christopher P. Regan
JOURNAL OF CARDIOVASCULAR PHARMACOLOGY
(2010)
Article
Cardiac & Cardiovascular Systems
Joseph J. Lynch, Christopher P. Regan, Gregory N. Beatch, Gilbert W. Gleim, Christopher J. Morabito
JOURNAL OF CARDIOVASCULAR PHARMACOLOGY
(2013)
Article
Biochemistry & Molecular Biology
Sophie Parmentier-Batteur, Eleftheria N. Finger, Raghu Krishnan, Hemaka A. Rajapakse, John M. Sanders, Geeta Kandpal, Hong Zhu, Keith P. Moore, Christopher P. Regan, Sujata Sharma, J. Fred Hess, Theresa M. Williams, Ian J. Reynolds, Joseph P. Vacca, Robert J. Mark, Philippe G. Nantermet
JOURNAL OF NEUROCHEMISTRY
(2011)
Article
Pharmacology & Pharmacy
Christopher A. Salvatore, Eric L. Moore, Amy Calamari, Jacquelynn J. Cook, Maria S. Michener, Stacey O'Malley, Patricia J. Miller, Cyrille Sur, David L. Williams, Zhizhen Zeng, Andrew Danziger, Joseph J. Lynch, Christopher P. Regan, John F. Fay, Yui S. Tang, Chi-Chung Li, Nicole T. Pudvah, Rebecca B. White, Ian M. Bell, Steven N. Gallicchio, Samuel L. Graham, Harold G. Selnick, Joseph P. Vacca, Stefanie A. Kane
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
(2010)
Article
Neurosciences
Kelley A. Foster, Hillary K. Regan, Andrew P. Danziger, Theodore Detwiler, Nancy Kwon, Keith Rickert, Joseph J. Lynch, Christopher P. Regan
NEUROSCIENCE RESEARCH
(2009)
Article
Pharmacology & Pharmacy
Christopher Regan, Cherrie Shepherd, Alison Strack, David Weinberg, Ravi Nargund, Zhixiong Ye, Patrick Pollard, Tung Fong, Ian Reynolds, Joseph Lynch
Article
Multidisciplinary Sciences
Lei Ma, Matthew Seager, Marion Wittmann, Marlene Jacobson, Denise Bickel, Maryann Burno, Keith Jones, Valerie Kuzmick Graufelds, Guangping Xu, Michelle Pearson, Alexander McCampbell, Renee Gaspar, Paul Shughrue, Andrew Danziger, Christopher Regan, Rose Flick, Danette Pascarella, Susan Garson, Scott Doran, Constantine Kreatsoulas, Lone Veng, Craig W. Lindsley, William Shipe, Scott Kuduk, Cyrille Sur, Gene Kinney, Guy R. Seabrook, William J. Ray
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2009)
Article
Chemistry, Medicinal
Ian M. Bell, Steven N. Gallicchio, Michael R. Wood, Amy G. Quigley, Craig A. Stump, C. Blair Zartman, John F. Fay, Chi-Chung Li, Joseph J. Lynch, Eric L. Moore, Scott D. Mosser, Thomayant Prueksaritanont, Christopher P. Regan, Shane Roller, Christopher A. Salvatore, Stefanie A. Kane, Joseph P. Vacca, Harold G. Selnick
ACS MEDICINAL CHEMISTRY LETTERS
(2010)