Results 11 to 20 of about 10,564,162 (159)

Synthesis and Evaluation of Fluorinated Peptidomimetics Enabling the Development of ¹⁸F-Labeled Radioligands Targeting Muscarinic Acetylcholine Receptor Subtype M3. [PDF]

ChemMedChem
Fluorinated peptidomimetics targeting muscarinic acetylcholine receptor subtype M3: Fluorinated peptidomimetic compounds based on a β‐alanine‐glycine scaffold, with lead compound 24 demonstrating high M3 selectivity and submicromolar potency. The first M3‐selective positron emission tomography radioligand, [18F]24, is synthesized and will be evaluated ...
Herrera-Rueda MA, Boateng MA, Wuest M, West FG, Wuest F.   +4 more
europepmc   +2 more sources

A Novel Rat Infant Model of Medial Temporal Lobe Epilepsy Reveals New Insight into the Molecular Biology and Epileptogenesis in the Developing Brain. [PDF]

Neural Plast
Although several adult rat models of medial temporal lobe epilepsy (mTLE) have been described in detail, our knowledge of mTLE epileptogenesis in infant rats is limited. Here, we present a novel infant rat model of mTLE (InfRPil‐mTLE) based on a repetitive, triphasic injection regimen consisting of low‐dose pilocarpine administrations (180 mg/kg. i.p.)
Wormuth C, Papazoglou A, Henseler C, Ehninger D, Broich K, Haenisch B, Hescheler J, Köhling R, Weiergräber M.   +8 more
europepmc   +2 more sources

Herbal Amara extract induces gastric fundus relaxation via inhibition of the M2 muscarinic receptor. [PDF]

Neurogastroenterol Motil
This preclinical study demonstrates the relaxant effect of Amara herbal extract (containing nine different plant extracts) on fundus smooth muscles dissected from guinea pigs. This relaxant effect occurs via inhibition of M2 muscarinic receptor activity.
Piqué-Borràs MR, Röhrl J, Künstle G.
europepmc   +2 more sources

Polypharmacy with tiagabine, levetiracetam, and perampanel in status epilepticus: Insights from EEG, biochemical, and histopathological studies in rats. [PDF]

Epilepsia Open
Abstract Objective Status epilepticus (SE) is a condition of neurological emergency, which precipitates various functional and morphological changes in the brain. Due to the risk of drug resistance associated with SE, this study aimed to evaluate a multitargeted approach to treat SE by combining clinically used antiseizure drugs. Methods In this study,
Javaid S, Alqahtani F, Parveen A, Ashraf W, Rehman Z, Anjum SMM, Ahmad T, Imran I.   +7 more
europepmc   +2 more sources

Improved PIEZO1 agonism through 4‐benzoic acid modification of Yoda1

British Journal of Pharmacology, Volume 180, Issue 16, Page 2039-2063, August 2023., 2023
Background and Purpose The protein PIEZO1 forms mechanically activated, calcium‐permeable, non‐selective cation channels in numerous cell types from several species. Options for pharmacological modulation are limited and so we modified a small‐molecule agonist at PIEZO1 channels (Yoda1) to increase the ability to modulate these channels.
Gregory Parsonage, Kevin Cuthbertson, Naima Endesh, Nicoletta Murciano, Adam J. Hyman, Charlotte H. Revill, Oleksandr V. Povstyan, Eulashini Chuntharpursat‐Bon, Marjolaine Debant, Melanie J. Ludlow, Timothy Simon Futers, Laeticia Lichtenstein, Jacob A. Kinsella, Fiona Bartoli, Maria Giustina Rotordam, Nadine Becker, Andrea Brüggemann, Richard Foster, David J. Beech   +18 more
wiley   +1 more source

N-SDM/N-SDM: N-SDM v1.0.0

, 2022
First N-SDM ...
AnAdde, N-SDM
core   +1 more source

Histamine via histamine H1 receptor enhances the muscarinic receptor‐induced calcium response to acetylcholine in an enterochromaffin cell model

Clinical and Experimental Pharmacology and Physiology, Volume 49, Issue 10, Page 1059-1071, October 2022., 2022
Abstract As a prerequisite for serotonin secretion, the P‐STS ileal enterochromaffin cell line responds to acetylcholine (ACh) stimulation with an increase in intracellular calcium mediated by the muscarinic ACh receptor M3 (M3R). Histamine increases intracellular calcium via histamine H1 receptor (H1R) in P‐STS cells and pre‐incubation with histamine ...
Beatrix Pfanzagl, Roswitha Pfragner, Erika Jensen‐Jarolim   +2 more
wiley   +1 more source

Brain glycogen content is increased in the acute and interictal chronic stages of the mouse pilocarpine model of epilepsy

Epilepsia Open, Volume 7, Issue 2, Page 361-367, June 2022., 2022
Abstract Glucose is the main brain fuel in fed conditions, while astrocytic glycogen is used as supplemental fuel when the brain is stimulated. Brain glycogen levels are decreased shortly after induced seizures in rodents, but little is known about how glycogen levels are affected interictally in chronic models of epilepsy. Reduced glutamine synthetase
Gi Young Seo, Elliott S. Neal, Felicity Han, Diana Vidovic, Fathima Nooru‐Mohamed, Gerald A. Dienel, Mitchell A. Sullivan, Karin Borges   +7 more
wiley   +1 more source

miR‐485's anti‐drug resistant epilepsy effects by regulating SV2A/PSD‐95 and targeting ABCC1 and neuronal signaling‐transduction proteins in hippocampus of rats

Brain and Behavior, Volume 11, Issue 8, August 2021., 2021
MiR‐485 was a potential targets for anti‐DRE, and this effects might be partially via miR‐485‐5p/homeostatic‐synaptic plasticity‐molecule axis and/or targeting efflux transporter (ABCC1) and other neuronal signaling‐transduction proteins (LRP4, MDM4,p53 and TMBIM1).
Kaixuan Wang, Jing Wu, Jiangping Wang, Kewen Jiang   +3 more
wiley   +1 more source

The cellular function and molecular mechanism of formaldehyde in cardiovascular disease and heart development

Journal of Cellular and Molecular Medicine, Volume 25, Issue 12, Page 5358-5371, June 2021., 2021
Abstract As a common air pollutant, formaldehyde is widely present in nature, industrial production and consumer products. Endogenous formaldehyde is mainly produced through the oxidative deamination of methylamine catalysed by semicarbazide‐sensitive amine oxidase (SSAO) and is ubiquitous in human body fluids, tissues and cells.
Ying Zhang, Yanyan Yang, Xiangqin He, Panyu Yang, Tingyu Zong, Pin Sun, Rui‐cong Sun, Tao Yu, Zhirong Jiang   +8 more
wiley   +1 more source