Article
Behavioral Sciences
Yu Hu, Haixia Li, Cheng Zhou, Ying Liu, Zhen Ma
Summary: The study investigated the effects of different concentrations of the serotonin receptor agonist on aggressive behavior in juvenile pufferfish, showing that activation of the serotonergic system can suppress both aggressive behavior and locomotor activity in the fish.
AGGRESSIVE BEHAVIOR
(2022)
Article
Neurosciences
Ria Gupta, Sidharth Mehan, Pranshul Sethi, Aradhana Prajapati, Abdulrahman Alshammari, Metab Alharbi, Haneen A. Al-Mazroua, Acharan S. Narula
Summary: This study investigated the neuroprotective effects of Purmorphamine, a smoothened-sonic-hedgehog agonist, in a rat model of obsessive-compulsive disorder (OCD). The results demonstrated that Purmorphamine attenuated OCD-like behaviors, oxidative stress, inflammation, apoptosis, and neurotransmitter imbalance induced by 8-hydroxy-2-(di-n-propylamino)-tetralin injection. The neuroprotective effect of Purmorphamine was comparable to the standard drug for OCD, fluvoxamine, and the combination of Purmorphamine and fluvoxamine showed a more significant restoration of these pathological changes.
Article
Chemistry, Medicinal
Ying-Ting Hsu, Shen-Ren Chen, Yung-Chiao Chang, Hsiao-Fu Chang, Teng-Kuang Yeh, Jian-Ying Chuang, Horace H. Loh, Hsing-Pang Hsieh, Shau-Hua Ueng, Shiu-Hwa Yeh
Summary: The demand for a non-addictive analgesic medication is increasing due to clinical misuse. Compound 14 is a dual agonist of the mu opioid receptor (MOR) and nociceptin-orphanin FQ opioid peptide (NOP) receptor, providing pain relief at very small doses and reducing unwanted side effects. Evaluating its effects in wild type and humanized mice can help develop a safer prescription analgesic drug.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Zachary W. Reichenbach, Kelly DiMattio, Suren Rajakaruna, David Ambrose, William D. Cornwell, Ronald J. Tallarida, Thomas Rogers, Lee-Yuan Liu-Chen, Ronald F. Tuma, Sara Jane Ward
Summary: Non-selective cannabinoid (CB) agonists can enhance the analgesic effects of morphine but inhibit its antinociceptive tolerance. Activation of CB2 receptors can reverse allodynia and hyperalgesia in chronic pain models, and co-administration of CB2 receptor selective agonists with morphine can synergistically enhance the effects. However, the interactions between CB2 receptor selective agonist O-1966 and morphine depend on the order of administration.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Behavioral Sciences
Pia R. Stettler, Diogo F. Antunes, Barbara Taborsky
Summary: The study found that the 5-HT1A receptor plays an important role in regulating aggressive, submissive, and affiliative behavior in the cooperatively-breeding cichlid Neolamprologus pulcher. The agonist increased aggression and decreased submission and affiliation, while the antagonist had opposite effects.
HORMONES AND BEHAVIOR
(2021)
Article
Dermatology
Claudia Cervantes-Duran, Miguel Avalos-Viveros, Luz Torner, Sandra-Guadalupe Sanchez-Ceja, Alain-Raimundo Rodriguez-Orozco, Hector-Eduardo Martinez-Flores, Martha-Estrella Garcia-Perez
Summary: The study found that in the IMQ-induced psoriasis mice model, the development of secondary chronic allodynia and hyperalgesia could be modulated by anti-inflammatory agents and compound 48/80, and the activation of 5-HT1A receptor might regulate these nociceptive behaviours. Additionally, it was observed that the long-lasting pain resulting from psoriasis inflammation is associated with the serotonergic system, indicating that the 5-HT1A receptor could be a potential therapeutic target for psoriasis pain modulation.
EXPERIMENTAL DERMATOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Mengna Zhang, Biao Xu, Ning Li, Run Zhang, Qinqin Zhang, Dan Chen, Syed Faheem Askari Rizvi, Kangtai Xu, Yonghang Shi, Bowen Yu, Quan Fang
Summary: This study designed and synthesized a novel cyclic disulfide analogue of DN-9, OFP011, which exhibited multifunctional agonistic effects at the mu-opioid and NPFF1/NPFF2 receptors. It also showed improved antinociceptive activity, especially in oral administration.
ACS CHEMICAL NEUROSCIENCE
(2022)
Article
Chemistry, Medicinal
Qian He, Yuanyuan Wei, Xiao Liu, Rongrong Ye, Linghui Kong, Zixiang Li, Shuang Jiang, Linqian Yu, Jingrui Chai, Qiong Xie, Wei Fu, Yujun Wang, Wei Li, Zhuibai Qiu, Jinggen Liu, Liming Shao
Summary: In search for safer selective kappa OR agonists, a series of m-substituted analogs were designed and synthesized resulting in compound 6c (SLL-1206) with single-digit nanomolar activities. Compound 6c showed subtype selectivity by significantly reducing affinity for mu OR and delta OR, leading to improved physicochemical and pharmacokinetic properties compared to SLL-039.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Charlene Gadais, Justyna Piekielna-Ciesielska, Jolien De Neve, Charlotte Martin, Anna Janecka, Steven Ballet
Summary: Opioid agonists are commonly used for pain relief, but their side effects can be problematic. Designed multiple ligands (DMLs) offer a promising approach by targeting both opioid and non-opioid pathways involved in pain perception. Newly designed opioid agonist-NK2 or -NK3 antagonists show potential for future opioid hybrid development.
Article
Endocrinology & Metabolism
Zhenglan Han, Guofei Jin, Jiancai Tang, Hanyan Wang, Dongmei Guo, Jingping Zhang
Summary: The chimeric peptide EN-9 acts as a bifunctional agonist for x-opioid/neuropeptide FF receptors and modulates chronic pain without tolerance. It interacts with the mu-opioid receptor pathway, especially in antinociception and tolerance. The study also investigated the cross-tolerance of EN-9 with other mu-opioid receptor agonists such as EM-2, DAMGO, and morphine.
Article
Neurosciences
X. Tao, A. Newman-Tancredi, M. A. Varney, K. A. Razak
Summary: Fragile X Syndrome (FXS) is a genetic cause of Autism Spectrum Disorders (ASD) and intellectual disabilities. FXS is characterized by sensory hypersensitivity, especially in the auditory domain, which can lead to delayed language development and high anxiety. In a mouse model of FXS, the Fmr1 KO mouse, auditory hypersensitivity and audiogenic seizures are observed. The activation of serotonin-1A receptor (5-HT1A) can reduce audiogenic seizures in Fmr1 KO mice.
Article
Neurosciences
Salvador Sierra, Karan H. Muchhala, Donald K. Jessup, Katherine M. Contreras, Urjita H. Shah, David L. Stevens, Jennifer Jimenez, Xiomara K. Cuno Lavilla, Mario de la Fuente Revenga, Kumiko M. Lippold, Shanwei Shen, Justin L. Poklis, Liya Y. Qiao, William L. Dewey, Hamid I. Akbarali, M. Imad Damaj, Javier Gonzalez-Maeso
Summary: Opioid-sparing therapies that enhance the analgesic effect while reducing the side effects and abuse liability of opioids are important for clinical use. Recent research has shown that there are sex differences in the antinociceptive response to opioids, but the underlying mechanisms are still not well understood. This study suggests that the 5-HT2A receptor antagonist volinanserin can enhance the potency of the opioid analgesic oxycodone in male mice, but not in female mice. The results also indicate that the signaling crosstalk mechanism involving 5-HT2AR expression in mouse dorsal root ganglion neurons may play a role in the sex-specific response.
Article
Neurosciences
C. Austin Zamarripa, Tanya Pareek, Hayley M. Schrock, Thomas E. Prisinzano, Bruce E. Blough, Kenneth J. Sufka, Kevin B. Freeman
Summary: Triazole 1.1 is a novel KOR agonist that can reduce the reinforcing effects of oxycodone and enhance oxycodone-induced antinociception to a degree similar to typical KOR agonists. Developing MOR-KOR agonist combinations from the triazole 1.1 series may lead to new pain therapeutics with reduced abuse liability.
PSYCHOPHARMACOLOGY
(2021)
Article
Behavioral Sciences
Susanne Nikolaus, Owen Y. Chao, Markus Beu, Jan Henke, Christina Antke, An-Li Wang, Benedetta Fazari, Eduards Mamlins, Joseph P. Huston, Frederik L. Giesel
Summary: In this study, the effect of the 5-HT1A receptor agonist 8-OH-DPAT on motor and exploratory behaviors, object and place recognition, and dopamine and serotonin transporter binding in the rat brain was examined. The results showed that 8-OH-DPAT dose-dependently affected the behavior and memory of rats, potentially through modulating dopamine levels.
NEUROBIOLOGY OF LEARNING AND MEMORY
(2023)
Article
Physiology
Isabelle Vivodtzev, Glen Picard, Kevin O'Connor, J. Andrew Taylor
Summary: In individuals with acute high-level SCI, the use of Buspirone improves cardiorespiratory adaptations to FES-exercise training, resulting in increased peak oxygen consumption and peak ventilation, which are closely related to improved respiratory function.
EUROPEAN JOURNAL OF APPLIED PHYSIOLOGY
(2021)
Article
Medicine, Research & Experimental
Shinya Fuse, Yoichiro Sugiyama, Keiko Hashimoto, Toshiro Umezaki, Yoshitaka Oku, Mathias Dutschmann, Shigeru Hirano
Article
Anesthesiology
Thomas Muders, Henning Luepschen, Torsten Meier, Andreas Wolfgang Reske, Joerg Zinserling, Stefan Kreyer, Robert Pikkemaat, Enn Maripu, Steffen Leonhardt, Goran Hedenstierna, Christian Putensen, Hermann Wrigge
Article
Neurosciences
Rishi R. Dhingra, Thomas E. Dick, Werner I. Furuya, Roberto F. Galan, Mathias Dutschmann
JOURNAL OF PHYSIOLOGY-LONDON
(2020)
Article
Multidisciplinary Sciences
Felix Girrbach, Tobias Landeck, Dominic Schneider, Stefan U. Reske, Gunther Hempel, Soren Hammermueller, Udo Gottschaldt, Peter Salz, Katharina Noreikat, Sebastian N. Stehr, Hermann Wrigge, Andreas W. Reske
Article
Physiology
Werner I. Furuya, Rishi R. Dhingra, Andrew L. Gundlach, Mohammad Akhter Hossain, Mathias Dutschmann
RESPIRATORY PHYSIOLOGY & NEUROBIOLOGY
(2020)
Article
Medicine, Research & Experimental
Liselotte Hol, Sunny G. L. H. Nijbroek, Ary Serpa Neto, Marcelo Gama de Abreu, Paolo Pelosi, Sabrine N. T. Hemmes, Leon P. H. J. Aarts, Ronald D. L. Akkerman, Juliette J. E. Albersen, Caterina Aurilio, Denise Battaglini, Hans D. de Boer, Annemieke Boom, Christa Boer, Tammo Brouwer, Wolfgang F. F. A. Buhre, Carolina S. E. Bulte, Gitara M. Edward-Rutten, Marc B. Godfried, Hendrik J. F. Helmerhorst, Jan Hofland, Hester Hoogenboom, W. Ten Hoope, Bernard M. Houweling, Ragnar Huhn, Wanda Konijn, Ankie W. M. M. Koopman-van Gemert, Dianne J. De Korte-de Boer, Minke C. Kortekaas, Felix Van Lier, Benedikt Preckel, Mandana Rad, Pasquale Sansone, Andre Stamkot, Robert Jan Stolker, Bram Thiel, Johannes F. H. Ubben, Michel M. R. F. Struys, Bastiaan A. In 't Veld, Hermann Wrigge, Miriam Zeillemaker-Hoekstra, Tim van der Zwan, Johannes H. M. J. Zwijsen, Markus W. Hollmann, Marcus J. Schultz
Article
Infectious Diseases
L. Ehmann, P. Simon, D. Busse, D. Petroff, C. Dorn, W. Huisinga, A. Dietrich, M. Zeitlinger, H. Wrigge, C. Kloft
CLINICAL MICROBIOLOGY AND INFECTION
(2020)
Article
Physiology
Christian Arias-Reyes, Natalia Zubieta-DeUrioste, Liliana Poma-Machicao, Fernanda Aliaga-Raudan, Favio Carvajal-Rodriguez, Mathias Dutschmann, Edithm Schneider-Gasser, Gustavo Zubieta-Calleja, Jorge Soliz
RESPIRATORY PHYSIOLOGY & NEUROBIOLOGY
(2020)
Article
Pharmacology & Pharmacy
David Busse, Philipp Simon, Robin Michelet, Lisa Ehmann, Frank Mehner, Christoph Dorn, Alexander Kratzer, Wilhelm Huisinga, Hermann Wrigge, David Petroff, Charlotte Kloft
Summary: This study investigated and analyzed the variability of RR values in non-obese and obese patients, finding that patient-related factors were the main contributor to variability in RR, followed by factors related to the catheter. Fat mass in obese patients affected RR, but only explained a portion of the variability.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Emergency Medicine
P. Hilbert-Carius, H. Wrigge, R. Koch
NOTFALL & RETTUNGSMEDIZIN
(2021)
Article
Multidisciplinary Sciences
Christian Arias-Reyes, Favio Carvajal-Rodriguez, Liliana Poma-Machicao, Fernanda Aliaga-Raduan, Danuzia A. Marques, Natalia Zubieta-DeUrioste, Roberto Alfonso Accinelli, Edith M. Schneider-Gasser, Gustavo Zubieta-Calleja, Mathias Dutschmann, Jorge Soliz
Summary: Research shows that in the American continent, the transmission rate and severity of COVID-19 decrease with increasing altitude, with areas above 1000 meters being less affected by the pandemic.
Article
Biochemistry & Molecular Biology
Isaline Mees, Shanshan Li, Leah C. Beauchamp, Kevin J. Barnham, Mathias Dutschmann, Anthony J. Hannan, Thibault Renoir
Summary: Tau protein is associated with neurodegenerative diseases. The presence of hyperphosphorylated tau has been found in the brains of Huntington's disease (HD) patients. However, the role of tau in the development of HD is not well understood. This study investigates the impact of tau expression and knockout in an HD mouse model and finds that tau expression or ablation does not affect the progression of HD symptoms.
HUMAN MOLECULAR GENETICS
(2022)
Article
Neurosciences
Ryota Yamamoto, Yoichiro Sugiyama, Keiko Hashimoto, Shota Kinoshita, Akiyo Takemura, Shinya Fuse, Mami Kaneko, Shigeyuki Mukudai, Toshiro Umezaki, Mathias Dutschmann, Takashi Nakagawa, Shigeru Hirano
Summary: This research investigates sensory-motor integration during oropharyngeal swallowing from different sensory sources. The study found that electrical stimulation of the superior laryngeal nerve and oral injections can trigger swallowing responses, and the modulation of neuronal activity may contribute to the coordination of bolus transfer during swallowing.
NEUROSCIENCE RESEARCH
(2022)
Article
Anesthesiology
N. Carius, M. Bauer, H. Wrigge, B. Kern, P. Hilbert-Carius, J. Jakubetz, G. Hofmann
ANASTHESIOLOGIE & INTENSIVMEDIZIN
(2020)
Meeting Abstract
Critical Care Medicine
P. Simon, F. Girrbach, N. Schliewe, G. Hempel, D. Petroff, M. Lange, A. Dietrich, T. Bluth, M. Gama de Abreu, H. Wrigge
AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE
(2020)