Results 11 to 20 of about 13,221 (154)

Basmisanil, a highly selective GABAA-α5 negative allosteric modulator: preclinical pharmacology and demonstration of functional target engagement in man [PDF]

Scientific Reports, 2021
GABAA-α5 subunit-containing receptors have been shown to play a key modulatory role in cognition and represent a promising drug target for cognitive dysfunction, as well as other disorders.
Joerg F. Hipp, Frederic Knoflach, Robert Comley, Theresa M. Ballard, Michael Honer, Gerhard Trube, Rodolfo Gasser, Eric Prinssen, Tanya L. Wallace, Andreas Rothfuss, Henner Knust, Sian Lennon-Chrimes, Michael Derks, Darren Bentley, Lisa Squassante, Stephane Nave, Jana Nöldeke, Christoph Wandel, Andrew W. Thomas, Maria-Clemencia Hernandez   +19 more
doaj   +2 more sources

In Vitro Functional Characterization of GET73 as Possible Negative Allosteric Modulator of Metabotropic Glutamate Receptor 5 [PDF]

Frontiers in Pharmacology, 2018
The present study was aimed to further characterize the pharmacological profile of N-[4-(trifluoromethyl) benzyl]-4-methoxybutyramide (GET73), a putative negative allosteric modulator (NAM) of metabotropic glutamate subtype 5 receptor (mGluR5) under ...
Sarah Beggiato, Sarah Beggiato, Andrea C. Borelli, Andrea C. Borelli, Maria C. Tomasini, Maria C. Tomasini, M. Paola Castelli, M. Paola Castelli, Nicholas Pintori, Roberto Cacciaglia, Antonella Loche, Luca Ferraro, Luca Ferraro, Luca Ferraro   +13 more
doaj   +2 more sources

An NMDAR positive and negative allosteric modulator series share a binding site and are interconverted by methyl groups [PDF]

eLife, 2018
N-methyl-d-aspartate receptors (NMDARs) are an important receptor in the brain and have been implicated in multiple neurological disorders. Many non-selective NMDAR-targeting drugs are poorly tolerated, leading to efforts to target NMDAR subtypes to ...
Riley Perszyk, Brooke M Katzman, Hirofumi Kusumoto, Steven A Kell, Matthew P Epplin, Yesim A Tahirovic, Rhonda L Moore, David Menaldino, Pieter Burger, Dennis C Liotta, Stephen F Traynelis   +10 more
doaj   +2 more sources

Negative allosteric modulation of GluN1/GluN3 NMDA receptors [PDF]

Neuropharmacology, 2020
NMDA receptors are ligand-gated ion channels that mediate excitatory neurotransmission. Most native NMDA receptors are tetrameric assemblies of two glycine-binding GluN1 and two glutamate-binding GluN2 subunits. Co-assembly of the glycine-binding GluN1 with glycine-binding GluN3 subunits (GluN3A-B) creates glycine activated receptors that possess ...
Zongjian, Zhu, Feng, Yi, Matthew P, Epplin, Ding, Liu, Samantha L, Summer, Ruth, Mizu, Gil, Shaulsky, Wenshu, XiangWei, Weiting, Tang, Pieter B, Burger, David S, Menaldino, Scott J, Myers, Dennis C, Liotta, Kasper B, Hansen, Hongjie, Yuan, Stephen F, Traynelis   +15 more
openaire   +2 more sources

COR758, a negative allosteric modulator of GABAB receptors

Neuropharmacology, 2021
Allosteric modulators of G protein coupled receptors (GPCRs), including GABABRs (GABABRs), are promising therapeutic candidates. While several positive allosteric modulators (PAM) of GABABRs have been characterized, only recently the first negative allosteric modulator (NAM) has been described.
Porcu, Alessandra, Mostallino, Rafaela, Serra, Valeria, Melis, Miriam, Sogos, Valeria, Beggiato, Sarah, Ferraro, Luca, Manetti, Fabrizio, Gianibbi, Beatrice, Bettler, Bernhard, Corelli, Federico, Mugnaini, Claudia, Castelli, M. Paola   +12 more
openaire   +5 more sources

Recent Advances in the Discovery of Nicotinic Acetylcholine Receptor Allosteric Modulators

Molecules, 2023
Positive allosteric modulators (PAMs), negative allosteric modulators (NAMs), silent agonists, allosteric activating PAMs and neutral or silent allosteric modulators are compounds capable of modulating the nicotinic receptor by interacting at allosteric ...
Dina Manetti, Silvia Dei, Hugo R. Arias, Laura Braconi, Alessio Gabellini, Elisabetta Teodori, Maria Novella Romanelli   +6 more
doaj   +1 more source

Negative allosteric modulation of the glucagon receptor by RAMP2

Biophysical Journal, 2022
AbstractReceptor activity-modifying proteins (RAMPs) modulate the activity of many Family B heterotrimeric guanine nucleotide-binding protein (G protein)-coupled receptors (GPCRs). The glucagon receptor (GCGR), a Family B GPCR responsible for maintenance of proper blood sugar levels, interacts with RAMP2, though the purpose and consequence of this ...
Kaavya Krishna Kumar, Evan S. O’Brien, Chris H. Habrian, Naomi R. Latorraca, Haoqing Wang, Inga Tuneew, Elizabeth Montabana, Susan Marqusee, Daniel Hilger, Ehud Y. Isacoff, Jesper Mosolff Mathiesen, Brian K. Kobilka   +11 more
openaire   +4 more sources

Prospects for the use of allosteric drugs in real-world clinical practice

Реальная клиническая практика: данные и доказательства, 2023
While the clinical validity of the use of allosteric regulation is known, scientists are working on the discovery of new methods for the development of allosteric drugs that can modulate the functions of enzymes, depending on the desired therapeutic ...
I. R. Svechkareva, A. S. Kolbin
doaj   +1 more source

Sodium is a negative allosteric regulator of the ghrelin receptor

Cell Reports, 2023
Summary: The functional properties of G protein-coupled receptors (GPCRs) are intimately associated with the different components in their cellular environment.
Guillaume Ferré, Antoniel A.S. Gomes, Maxime Louet, Marjorie Damian, Paulo M. Bisch, Olivier Saurel, Nicolas Floquet, Alain Milon, Jean-Louis Banères   +8 more
doaj   +1 more source

Allosteric Modulators of G Protein-Coupled Dopamine and Serotonin Receptors: A New Class of Atypical Antipsychotics

Pharmaceuticals, 2020
Schizophrenia was first described by Emil Krapelin in the 19th century as one of the major mental illnesses causing disability worldwide. Since the introduction of chlorpromazine in 1952, strategies aimed at modifying the activity of dopamine receptors ...
Irene Fasciani, Francesco Petragnano, Gabriella Aloisi, Francesco Marampon, Marco Carli, Marco Scarselli, Roberto Maggio, Mario Rossi   +7 more
doaj   +1 more source