Review
Pharmacology & Pharmacy
Rashid Giniatullin
Summary: 5-hydroxytryptamine (5-HT) is considered a key mediator in migraine, but the role of 5-HT3 receptors in pain transmission remains controversial. The applicability of currently available 5-HT3 antagonists in migraine treatment is not clearly supported by clinical data.
BRITISH JOURNAL OF PHARMACOLOGY
(2022)
Article
Immunology
Minjie Wan, Zhanchuan Ma, Jiawen Han, Min Rao, Feng Hu, Pujun Gao, Xiaocong Wang
Summary: The 5-HT/5-HT7R signaling pathway helps to constrain inflammation through functional Bregs in ulcerative colitis.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2023)
Article
Psychiatry
Jan Terock, Antoine Weihs, Alexander Teumer, Johanna Klinger-Koenig, Deborah Janowitz, Hans J. Grabe
Summary: Previous studies have suggested a connection between childhood trauma, serotonergic neurotransmission, and alexithymia. The study found that childhood trauma and the rs6295 polymorphism have a significant interaction effect on alexithymia in male subjects.
PSYCHIATRY RESEARCH
(2021)
Article
Chemistry, Physical
Liping Fang, Shan He, Peng Yin, Ning Wang, Bin Zhang, Haixiao Jin
Summary: This study presents the design, synthesis, and evaluation of a series of novel tryptamine derivatives with 5-HT 1B R activation. Several compounds were identified as more potent 5-HT 1B R activators compared to the FDA-approved drug sumatriptan. The molecular docking results provided insights into the binding mode and interactions between the compounds and 5-HT 1B R.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Medicine, Research & Experimental
Elias B. Nascimento Jr., R. L. Romero, Marcela M. G. B. Dutra, Bernd L. Fiebich, Igor D. G. Duarte, Marcio M. Coelho
Summary: The activation of 5-HT1D and 5-HT7 receptors plays a role in mechanical allodynia induced by 5-HT in mice, while peripheral 5-HT3 receptors have an inhibitory role in the nociceptive response induced by 5-HT or carrageenan.
BIOMEDICINE & PHARMACOTHERAPY
(2021)
Review
Neurosciences
Yan Cai, Xiaolong Li, Hongli Zhou, Jiyin Zhou
Summary: Both peripheral and central serotonergic systems play a vital role in blood glucose regulation and the development of diabetes and its complications, suggesting their potential clinical significance as therapeutic targets.
FRONTIERS IN CELLULAR NEUROSCIENCE
(2022)
Review
Biochemistry & Molecular Biology
Yuya Sakimoto, Paw Min-Thein Oo, Makoto Goshima, Itsuki Kanehisa, Yutaro Tsukada, Dai Mitsushima
Summary: The hippocampus plays a key role in contextual memory, with long-term strengthening of glutamatergic transmission and enhancement of GABA(A) receptor-mediated inhibitory synapses after learning. Rapid plasticity at inhibitory synapses following contextual learning may facilitate encoding of memories and prevent cognitive dysfunction in hippocampal pathologies such as Alzheimer's disease, autism spectrum disorders, and epilepsy.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Multidisciplinary Sciences
Marie-Lise Jobin, Sana Siddig, Zsombor Koszegi, Yann Lanoiselee, Vladimir Khayenko, Titiwat Sungkaworn, Christian Werner, Kerstin Seier, Christin Misigaiski, Giovanna Mantovani, Markus Sauer, Hans M. Maric, Davide Calebiro
Summary: GABA(B) receptors are precisely located and regulated by dynamic interactions with Filamin A, which is a cytoskeletal protein. This study provides evidence that the spatial organization and diffusion of GABA(B) receptors on the plasma membrane are governed by Filamin A, and these interactions modulate the kinetics of G alpha(i) protein activation in response to GABA stimulation.
NATURE COMMUNICATIONS
(2023)
Article
Chemistry, Medicinal
Michal Galezowski, Charles-Henry Fabritius, Ullamari Pesonen, Harri Salo, Marta Olszak-Plachta, Klaudia Czerwinska, Justyna Adamczyk, Marcin Krol, Peteris Prusis, Magdalena Sieprawska-Lupa, Maciej Mikulski, Katja Kuokkanen, Radoslaw Obuchowicz, Timo Korjamo, Niina Jalava, Agnieszka Nikiforuk, Mateusz Nowak
Summary: This study presents the discovery and pharmacological characterization of a new series of 6-piperazinyl-7azaindoles, which demonstrate potent antagonism and selectivity against the 5-HT6 receptor. The research primarily focuses on optimizing the lead structure and investigating the structure-activity relationship (SAR) of these compounds. Compound 29 shows significant promise in terms of pharmacological, physicochemical, and ADME properties.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Behavioral Sciences
Amin Charousaei, Mohammad Nasehi, Vahab Babapour, Salar Vaseghi, Mohammad-Reza Zarrindast
Summary: The study demonstrated the involvement of CA3 5-HT4 receptors in D-AP5-induced anxiolytic-like behaviors in rats. Specifically, the experimental results showed that these receptors play an important role in modulating anxiety-related behaviors in rats.
BEHAVIOURAL BRAIN RESEARCH
(2021)
Article
Neurosciences
Dhamyaa Abed Najm Al-Halboosi, Olena Savchenko, Lora K. Heisler, Sergiy Sylantyev
Summary: Obesity is a global health challenge caused by excessive calorie intake. The brain plays a crucial role in controlling food intake, and NAG neurons, which co-express NPY, AgRP, and GABA, are identified as hunger and food intake stimulators. Activation of 5-HT1BR leads to a decrease in food intake by suppressing NAG neuron activity and neurotransmitter release.
Article
Chemistry, Physical
Jolanta Jaskowska, Anna Karolina Drabczyk, Pawel Sliwa, Przemyslaw Jodlowski, Edyta Pindelska, Damian Kulaga, Przemyslaw Zareba, Zbigniew Majka, Agata Siwek, Malgorzata Wolak, Marcin Kolaczkowski
Summary: In our research, we used ultrasound to support a new synthesis method to find dual 5-HT1A/5-HT7 ligands from the long-chain arylpiperazine (LCAP) family. We tested the synthesis method on approved drugs with arylpiperazine structures and achieved satisfactory results. We then obtained compounds from the LCAPs group using the sonochemical method and selected two selective 5-HT1A/5-HT7 ligands.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Clinical Neurology
Tristan J. Philippe, Lexia Bao, Maya E. Koblanski, Victor Viau
Summary: This study found that male and female rats showed region-specific changes in 5-HT 1A receptor function after repeated restraint, which may be explained by changes in receptor availability.
INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY
(2022)
Article
Cardiac & Cardiovascular Systems
Olivier Schussler, Luc Maroteaux, Ramadan Jashari, Pierre Falcoz, Marco Alifano, Yves Lecarpentier, Jean-Marie Launay
Summary: This study quantitatively measured the expression of 5-HTR serotonin receptors on animal or human valvular tissues, identifying several new and robustly expressed proteins and observing correlations between different levels of 5-HTR expression. These findings provide insights into the signaling mechanisms involved in valvular fibrosis and degeneration.
FRONTIERS IN CARDIOVASCULAR MEDICINE
(2022)
Article
Pharmacology & Pharmacy
Laura Bayon-Cordero, Blanca Isabel Ochoa-Bueno, Asier Ruiz, Marina Ozalla, Carlos Matute, Maria Victoria Sanchez-Gomez
Summary: This study discovered that GABAR agonists attenuate AMPA-induced apoptotic excitotoxicity in oligodendrocytes by interfering with the expression of GluR subunits in the cell membrane and calcium-dependent intracellular signaling pathways. These findings suggest that GABAR agonists could potentially serve as protectants for oligodendrocytes in central nervous system disorders.
FRONTIERS IN PHARMACOLOGY
(2022)