Results 131 to 140 of about 31,985 (308)

Antipsychotic profiles of TASP0443294, a novel and orally active positive allosteric modulator of metabotropic glutamate 2 receptor

Journal of Pharmacological Sciences, 2015
Glutamatergic dysfunction has been implicated in psychiatric disorders such as schizophrenia. The stimulation of metabotropic glutamate (mGlu) 2 receptor has been shown to be effective in a number of animal models of schizophrenia.
Hirohiko Hikichi, Tetsuaki Hiyoshi, Toshiyuki Marumo, Yasumitsu Tomishima, Ayaka Kaku, Izumi Iida, Hiroki Urabe, Tomoko Tamita, Akito Yasuhara, Jun-ichi Karasawa, Shigeyuki Chaki   +10 more
doaj   +1 more source

Cyclic nucleotide-gated channels: structural basis of ligand efficacy and allosteric modulation [PDF]

, 1997
Most working proteins, including metabolic enzymes, transcription regulators, and membrane receptors, transporters, and ion channels, share the property of allosteric coupling. The term 'allosteric' means that these proteins mediate indirect interactions
Lester, Henry A., Li, Jun, Zagotta, William N.   +2 more
core   +1 more source

Inosine triphosphate pyrophosphatase activity as a potential predictor of methotrexate remission in juvenile idiopathic arthritis

Arthritis &Rheumatology, Accepted Article.
Background Methotrexate (MTX) is the first‐line therapy for juvenile idiopathic arthritis (JIA), but up to 40% of patients don't respond. Low inosine‐triphosphate‐pyrophosphatase (ITPA) activity has been associated with reduced clinical remission. We investigated ITPA role and the underlying mechanisms in vitro.
Sofia Sindici Forgiarini, Marianna Lucafò, Debora Curci, Davide Selvestrel, Valentina Moressa, Sofia Pagarin, Barbara Bellich, Martina Franzin, Alberto Tommasini, Mara L. Becker, Laura B. Ramsey, Susan D. Thompson, Carl D. Langefeld, Federica Corba, Edoardo Marrani, Gabriele Simonini, Gabriele Stocco, Giuliana Decorti, Andrea Taddio, Serena Pastore   +19 more
wiley   +1 more source

Thiol-reactive analogues of galanthamine, codeine and morphine as potential probes to interrogate allosteric binding within nAChRs [PDF]

, 2016
Alkaloids including galanthamine (1) and codeine (2) are reported to be positive allosteric modulators of nicotinic acetylcholine receptors (nAChRs) but the binding sites responsible for this activity are not known with certainty.
Balle, Thomas, Chebib, Mary, Gallagher, Ryan, McLeod, Malcolm   +3 more
core   +1 more source

Cannabinoids and drug–drug pharmacokinetic interactions: Deciphering the risks

British Journal of Clinical Pharmacology, EarlyView.
The relationship between cannabinoids and mental health has become a major focus of scientific inquiry and public discourse. Cannabinoids are diverse chemical compounds from the Cannabis species that have been explored for their therapeutic applications in treating chronic pain, psychiatric and neurological conditions, such as depression, schizophrenia,
Paraskevi Papakyriakopoulou, Georgia Valsami, Georgios Ismailos   +2 more
wiley   +1 more source

S 47445 Produces Antidepressant- and Anxiolytic-Like Effects through Neurogenesis Dependent and Independent Mechanisms

Frontiers in Pharmacology, 2017
Glutamatergic dysfunctions are observed in the pathophysiology of depression. The glutamatergic synapse as well as the AMPA receptor’s (AMPAR) activation may represent new potential targets for therapeutic intervention in the context of major depressive ...
Indira Mendez-David, Jean-Philippe Guilloux, Mariusz Papp, Laurent Tritschler, Elisabeth Mocaer, Alain M. Gardier, Sylvie Bretin, Denis J. David   +7 more
doaj   +1 more source

Nicotinamide Phosphoribosyltransferase Positive Allosteric Modulators Attenuate Neuronal Oxidative Stress

ACS Medicinal Chemistry Letters
Evidence supports boosting nicotinamide adenine dinucleotide (NAD+) to counteract oxidative stress in aging and neurodegenerative disease. One approach is to enhance the activity of nicotinamide phosphoribosyltransferase (NAMPT). Novel NAMPT positive allosteric modulators (N-PAMs) were identified.
Jesse Gordon-Blake, Kiira Ratia, Victoria Weidig, Ganga Reddy Velma, Martha Ackerman-Berrier, Christopher Penton, Soumya Reddy Musku, Erick T.M. Alves, Tom Driver, Leon Tai, Gregory R. J. Thatcher   +10 more
openaire   +2 more sources

The molecular determinants of small-molecule ligand binding at P2X receptors [PDF]

, 2018
P2X receptors are trimeric eukaryotic ATP-gated cation channels. Extracellular ATP - their physiological ligand - is released as a neurotransmitter and in conditions of cell damage such as inflammation, and substantial evidence implicates P2X receptors ...
Brancale, Andrea, Pasqualetto, Gaia, Young, Mark T.   +2 more
core   +3 more sources

Zuranolone: A case study in (regulatory) rush to judgement?

British Journal of Clinical Pharmacology, EarlyView.
Abstract Sage, in collaboration with Biogen, submitted a new drug approval for zuranolone for postpartum depression (PPD) and major depressive disorder (MDD) in December 2022. In August 2023, the US Food and Drug Administration granted approval for PPD but denied approval for MDD.
Lisa Cosgrove, Milutin Kostic, Barbara Mintzes, Gianna D'Ambrozio, Allen Shaughnessy   +4 more
wiley   +1 more source

Positive allosteric modulation of mGluR5 accelerates extinction learning but not relearning following methamphetamine self-administration

Frontiers in Pharmacology, 2012
Recent studies have implicated glutamate neurotransmission as an important substrate for the extinction of conditioned behaviors, including responding for drug reinforcement.
Peter R Kufahl, Lauren E Hood, Natali E Nemirovsky, Piroska eBarabas, Casey eHalstengard, Angel eVilla, Elisabeth eMoore, Lucas R Watterson, M Foster eOlive   +8 more
doaj   +1 more source