Results 31 to 40 of about 121,181 (303)

Negative effect of treatment with mGluR5 negative allosteric modulator AFQ056 on blood biomarkers in young individuals with Fragile X syndrome [PDF]

SAGE Open Medicine
Background: Fragile X syndrome, with an approximate incidence rate of 1 in 4000 males to 1 in 8000 females, is the most prevalent genetic cause of heritable intellectual disability and the most common monogenic cause of autism spectrum disorder. The full
Dragana Protic, Elizabeth Breeze, Guadalupe Mendoza, Marwa Zafarullah, Leonard Abbeduto, Randi Hagerman, Christopher Coffey, Merit Cudkowicz, Blythe Durbin-Johnson, Paul Ashwood, Elizabeth Berry-Kravis, Craig A Erickson, Robin Filipink, Andrea Gropman, Lenora Lehwald, Angela Maxwell-Horn, Stephanie Morris, Amanda Palladino Bennett, Lisa Prock, Amy Talboy, Nicole Tartaglia, Jeremy Veenstra-VanderWeele, Flora Tassone   +22 more
doaj   +2 more sources

The action of a negative allosteric modulator at the dopamine D₂ receptor is dependent upon sodium ions. [PDF]

Sci Rep, 2018
Sodium ions (Na+) allosterically modulate the binding of orthosteric agonists and antagonists to many class A G protein-coupled receptors, including the dopamine D2 receptor (D2R).
Draper-Joyce CJ, Verma RK, Michino M, Shonberg J, Kopinathan A, Klein Herenbrink C, Scammells PJ, Capuano B, Abramyan AM, Thal DM, Javitch JA, Christopoulos A, Shi L, Lane JR.   +13 more
europepmc   +2 more sources

The structural determinants of the bitopic binding mode of a negative allosteric modulator of the dopamine D₂ receptor. [PDF]

Biochem Pharmacol, 2018
Graphical abstract Figure. No caption available. ABSTRACT SB269652 is a negative allosteric modulator of the dopamine D2 receptor (D2R) yet possesses structural similarity to ligands with a competitive mode of interaction.
Draper-Joyce CJ, Michino M, Verma RK, Klein Herenbrink C, Shonberg J, Kopinathan A, Scammells PJ, Capuano B, Thal DM, Javitch JA, Christopoulos A, Shi L, Lane JR.   +12 more
europepmc   +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

A Phase I randomized clinical trial testing the safety, tolerability and preliminary pharmacokinetics of the mGluR5 negative allosteric modulator GET 73 following single and repeated doses in healthy volunteers

European Journal of Pharmaceutical Sciences, 2017
&NA; Preclinical work suggests that the metabotropic glutamate receptor subtype 5 (mGlu5) may represent a novel target to treat neuropsychiatric disorders, including alcohol use disorder and obesity.
Carolina L Haass-Koffler, Kimberly Goodyear, Antonella Loche   +2 more
exaly   +2 more sources

Negative allosteric modulation of the glucagon receptor by RAMP2

Biophysical Journal, 2022
Abstract Receptor 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 ...
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

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 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

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

A Thieno[2,3- d]pyrimidine Scaffold Is a Novel Negative Allosteric Modulator of the Dopamine D2 Receptor. [PDF]

Journal of Medicinal Chemistry, 2019
Recently, a novel negative allosteric modulator (NAM) of the D 2-like dopamine receptors 1 was identified through virtual ligand screening. This ligand comprises a thieno[2,3-d]pyrimidine scaffold that does not feature in known dopaminergic ligands ...
Tim J Fyfe, B. Zarzycka, H. Lim, B. Kellam, Shailesh N Mistry, V. Katrich, P. Scammells, J. R. Lane, B. Capuano   +8 more
semanticscholar   +2 more sources