Results 71 to 80 of about 33,509 (296)

Nicotinic acetylcholine receptors: Therapeutic targets for novel ligands to treat pain and inflammation

Pharmacological Research, 2023
Nicotinic acetylcholine receptors (nAChRs) have been historically defined as ligand-gated ion channels and function as such in the central and peripheral nervous systems. Recently, however, non-ionic signaling mechanisms via nAChRs have been demonstrated
Arik J. Hone, J. Michael McIntosh
doaj   +1 more source

NSAIDS AS MODULATORS OF CATION CHANNELS: FENAMATES REPURPOSING IN CHANNELOPATHIES

ChemMedChem, Accepted Article.
Cationic ion channels are transmembrane proteins that regulate the flux of cations (potassium, sodium, and calcium) across cell membrane, playing a pivotal role in many cellular functions. Disruptions of their activity can lead to the so‐called genetic or acquired channelopathies, a heterogeneous group of diseases that affect multiple human systems ...
Paola Laghetti, Concetta Altamura, Simone Dell’Atti, Jean-François Desaphy, Ilaria Saltarella   +4 more
wiley   +1 more source

Nicotinic receptor agonists as neuroprotective/neurotrophic drugs. Progress in molecular mechanisms [PDF]

, 2006
In the present work we reviewed recent advances concerning neuroprotective/neurotrophic effects of acute or chronic nicotine exposure, and the signalling pathways mediating these effects, including mechanisms implicated in nicotine addiction and nAChR ...
BELLUARDO, Natale, Fuxe, K., MUDO', Giuseppa   +2 more
core   +2 more sources

Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Multiple Ascending Doses and Dose Titration of Bexicaserin in Healthy Participants in a Randomized, Double‐Blind, Placebo‐Controlled Study

Clinical Pharmacology in Drug Development, EarlyView.
Abstract Bexicaserin (LP352) is a selective superagonist of the 5‐hydroxytryptamine 2C (5‐HT2C) receptor currently in development for the treatment of seizures that arise from developmental and epileptic encephalopathies. This phase 1, double‐blind, placebo‐controlled multiple ascending dose (MAD) study assessed the safety, tolerability, and ...
Jonathan Williams, Rosa Chan, Chad Orevillo, Gale O'Connell, Dewey McLin, Shikha Polega, Nuggehally R. Srinivas, Randall Kaye   +7 more
wiley   +1 more source

Expression of the α7 nicotinic acetylcholine receptor in human lung cells

Respiratory Research, 2005
Background We and others have shown that one of the mechanisms of growth regulation of small cell lung cancer cell lines and cultured pulmonary neuroendocrine cells is by the binding of agonists to the α7 neuronal nicotinic acetylcholine receptor.
Schuller Hildegard M, Dhar Madhu, Plummer Howard K   +2 more
doaj   +1 more source

Identification of critical residues in loop E in the 5-HT(3AS)R binding site [PDF]

, 2002
BACKGROUND: The serotonin type 3 receptor (5-HT(3)R) is a member of a superfamily of ligand gated ion channels. All members of this family share a large degree of sequence homology and presumably significant structural similarity.
Joshi, Prasad R, Muthalagi, Mani, Schulte, Marvin K, Venkatachalan, Srinivasan P, Venkataraman, Padmavati   +4 more
core   +3 more sources

Antinociceptive property of the nicotinic agonist AG-4 in rodents [PDF]

Drug Development Research, 1997
AG-4 has been characterized as a nicotinic agonist by binding (K i = 26 ± 1.4 μM) and in vitro functional assays. The antinociceptive effect of AG-4 was examined in mice and rats, using the hot plate, abdominal constriction, and paw-pressure tests.
GHELARDINI, CARLA, GALEOTTI, NICOLETTA, GUALTIERI, FULVIO, BELLUCCI, CRISTINA, MANETTI, DINA, P. BOREA, BARTOLINI, ALESSANDRO   +6 more
openaire   +4 more sources

Precision therapies for genetic epilepsies in 2025: Promises and pitfalls

Epilepsia Open, EarlyView.
Abstract By targeting the underlying etiology, precision therapies offer an exciting paradigm shift to improve the stagnant outcomes of drug‐resistant epilepsies, including developmental and epileptic encephalopathies. Unlike conventional antiseizure medications (ASMs) which only treat the symptoms (seizures) but have no effect on the underlying ...
Shuyu Wang, Emilio Perucca, Samuel F. Berkovic, Piero Perucca   +3 more
wiley   +1 more source

Acetylcholine receptor based chemogenetics engineered for neuronal inhibition and seizure control assessed in mice

Nature Communications
Epilepsy is a prevalent disorder involving neuronal network hyperexcitability, yet existing therapeutic strategies often fail to provide optimal patient outcomes. Chemogenetic approaches, where exogenous receptors are expressed in defined brain areas and
Quynh-Anh Nguyen, Peter M. Klein, Cheng Xie, Katelyn N. Benthall, Jillian Iafrati, Jesslyn Homidan, Jacob T. Bendor, Barna Dudok, Jordan S. Farrell, Tilo Gschwind, Charlotte L. Porter, Annahita Keravala, G. Steven Dodson, Ivan Soltesz   +13 more
doaj   +1 more source

The Novel, Nicotinic Alpha7 Receptor Partial Agonist, BMS-933043, Improves Cognition and Sensory Processing in Preclinical Models of Schizophrenia. [PDF]

PLoS ONE, 2016
The development of alpha7 nicotinic acetylcholine receptor agonists is considered a promising approach for the treatment of cognitive symptoms in schizophrenia patients. In the present studies we characterized the novel agent, (2R)-N-(6-(1H-imidazol-1-yl)
Linda J Bristow, Amy E Easton, Yu-Wen Li, Digavalli V Sivarao, Regina Lidge, Kelli M Jones, Debra Post-Munson, Christopher Daly, Nicholas J Lodge, Lizbeth Gallagher, Thaddeus Molski, Richard Pieschl, Ping Chen, Adam Hendricson, Ryan Westphal, James Cook, Christiana Iwuagwu, Daniel Morgan, Yulia Benitex, Dalton King, John E Macor, Robert Zaczek, Richard Olson   +22 more
doaj   +1 more source