Results 81 to 90 of about 15,215 (194)

Membrane Receptor-Induced Changes of the Protein Kinases A and C Activity May Play a Leading Role in Promoting Developmental Synapse Elimination at the Neuromuscular Junction

Frontiers in Molecular Neuroscience, 2017
Synapses that are overproduced during histogenesis in the nervous system are eventually lost and connectivity is refined. Membrane receptor signaling leads to activity-dependent mutual influence and competition between axons directly or with the ...
Josep M. Tomàs, Neus Garcia, Maria A. Lanuza, Laura Nadal, Marta Tomàs, Erica Hurtado, Anna Simó, Víctor Cilleros   +7 more
doaj   +1 more source

ERNEST COST action overview on the (patho)physiology of GPCRs and orphan GPCRs in the nervous system

British Journal of Pharmacology, Volume 182, Issue 14, Page 3178-3210, July 2025.
G protein‐coupled receptors (GPCRs) are a large family of cell surface receptors that play a critical role in nervous system function by transmitting signals between cells and their environment. They are involved in many, if not all, nervous system processes, and their dysfunction has been linked to various neurological disorders representing important
Necla Birgül Iyison, Clauda Abboud, Dayana Abboud, Abdulrasheed O. Abdulrahman, Ana‐Nicoleta Bondar, Julie Dam, Zafiroula Georgoussi, Jesús Giraldo, Anemari Horvat, Christos Karoussiotis, Alba Paz‐Castro, Miriam Scarpa, Hannes Schihada, Nicole Scholz, Bilge Güvenc Tuna, Nina Vardjan   +15 more
wiley   +1 more source

Design, Synthesis, and Evaluation of a New Fluorescent Ligand for the M₂ Muscarinic Acetylcholine Receptor. [PDF]

ACS Med Chem Lett
The M2 muscarinic acetylcholine receptor (M2R) is a G protein-coupled receptor involved in regulating cardiovascular functions and mediation of central muscarinic effects, such as movement, temperature control, and antinociceptive responses.
Szabó R, Szepesi Kovács D, Kiss DJ, Yazdi ZN, Tóth AD, Brea J, Loza MI, Meszéna D, Wittner L, Ulbert I, Volk B, Hunyady L, Keserű GM.   +12 more
europepmc   +2 more sources

Cholinergic dysregulation produced by selective inactivation of the dystonia-associated protein torsinA

Neurobiology of Disease, 2012
DYT1 dystonia, a common and severe primary dystonia, is caused by a 3-bp deletion in TOR1A which encodes torsinA, a protein found in the endoplasmic reticulum.
Giuseppe Sciamanna, Robert Hollis, Chelsea Ball, Giuseppina Martella, Annalisa Tassone, Andrea Marshall, Dee Parsons, Xinru Li, Fumiaki Yokoi, Lin Zhang, Yuqing Li, Antonio Pisani, David G. Standaert   +12 more
doaj   +1 more source

Progress on the development of Class A GPCR‐biased ligands

British Journal of Pharmacology, Volume 182, Issue 14, Page 3249-3300, July 2025.
Class A G protein‐coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target these receptors, over 60% GPCRs remain unexploited. Moreover, the adverse effects triggered by the available unbiased GPCR modulators, limit their use and
Paula Morales, Magdalena M. Scharf, Marcel Bermudez, Attila Egyed, Rafael Franco, Olivia K. Hansen, Nadine Jagerovic, Jan Jakubík, György M. Keserű, Dóra Judit Kiss, Pawel Kozielewicz, Olav Larsen, Maria Majellaro, Ana Mallo‐Abreu, Gemma Navarro, Rubén Prieto‐Díaz, Mette M. Rosenkilde, Eddy Sotelo, Holger Stark, Tobias Werner, Laura M. Wingler   +20 more
wiley   +1 more source

Chemogenetic Control of Striatal Astrocytes Improves Parkinsonian Motor Deficits in Mice

Glia, Volume 73, Issue 6, Page 1188-1202, June 2025.
Main Points Dopamine depletion reduces locomotion‐induced calcium activity in dorsal striatal astrocytes. Chemogenetic activation facilitates astrocyte locomotion responses and improves motor behavior in dopamine lesioned animals. ABSTRACT Parkinson's disease (PD) is characterized by the degeneration of dopaminergic nigrostriatal inputs, which causes ...
Wesley R. Evans, Sindhuja S. Baskar, Angelica Vellore, Ana Raquel Castro E. Costa, Cynthia Jacob, Sanya Ravoori, Abimbola Arigbe, Rafiq Huda   +7 more
wiley   +1 more source

Novel drugs approved by the EMA, the FDA and the MHRA in 2024: A year in review

British Journal of Pharmacology, Volume 182, Issue 7, Page 1416-1445, April 2025.
Abstract In the past year, the European Medicines Agency (EMA), the Food and Drug Administration (FDA) and the Medicines and Healthcare Products Regulatory Agency (MHRA) authorised 53 novel drugs. While the 2024 harvest is not as rich as in 2023, when 70 new chemical entities were approved, the number of ‘orphan’ drug authorisations in 2024 (21) is ...
Stavros Topouzis, Andreas Papapetropoulos, Steve P. H. Alexander, Miriam Cortese‐Krott, Dave A. Kendall, Kirill Martemyanov, Claudio Mauro, Nithyanandan Nagercoil, Reynold A. Panettieri Jr, Hemal H. Patel, Rainer Schulz, Barbara Stefanska, Gary J. Stephens, Mauro M. Teixeira, Nathalie Vergnolle, Xin Wang, Péter Ferdinandy   +16 more
wiley   +1 more source

Synergistic Antiemetic Effects of Nerolidol on Domperidone, Hyoscine, and Ondansetron: In Vivo and in Silico Investigations on Receptor Binding Affinity

ChemistryOpen, Volume 14, Issue 3, March 2025.
Nerolidol shows prominent antiemetic activity and mitigates CuSO4.H2O‐mediated retching in chicks efficiently through its peripheral action. Additionally, the in silico studies have also shown possible antiemetic effects with greater binding affinity against muscarinic (specially, M2 and M3) and dopaminergic receptors.
Sharmita Ghosh Situ, Md. Shimul Bhuia, Raihan Chowdhury, Sakib Al Hasan, Siddique Akber Ansari, Irfan Aamer Ansari, Arman Ali, Muhammad Torequl Islam   +7 more
wiley   +1 more source

Differential regulation of cAMP-mediated gene transcription by m1 and m4 muscarinic acetylcholine receptors. Preferential coupling of m4 receptors to Gi alpha-2

Journal of Biological Chemistry, 1994
We have used a luciferase reporter gene under the transcriptional control of a cAMP response element as a sensitive monitor of the regulation by muscarinic acetylcholine receptors (mAChRs) of intracellular cAMP levels and cAMP-regulated gene expression. Treatment with the muscarinic agonist carbachol results in an increase in luciferase activity in JEG-
J C, Migeon, N M, Nathanson
openaire   +2 more sources

Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4)

Journal of biomolecular screening, 2015
Muscarinic acetylcholine receptors (mAChRs) have long been viewed as viable targets for novel therapeutic agents for the treatment of Alzheimer’s disease and other disorders involving impaired cognitive function. In an attempt to identify orthosteric and
Emery Smith, Peter S. Chase, C. Niswender, T. Utley, Douglas J. Sheffler, M. Noetzel, A. Lamsal, M. Wood, P. J. Conn, C. Lindsley, Franck Madoux, M. Acosta, L. Scampavia, T. Spicer, P. Hodder   +14 more
semanticscholar   +1 more source