COR758, a negative allosteric modulator of GABAB receptors [PDF]
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 +12 more
core +7 more sources
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 +8 more
doaj +2 more sources
A Negative Allosteric Modulator of WNT Receptor Frizzled 4 Switches into an Allosteric Agonist [PDF]
Biochemistry, 2018 The WNT pathway interconnects a network of signaling events involved in a huge plethora of cellular processes, from organogenesis to tissue homeostasis. Despite its importance, the exiguity of organic drugs directly targeting the members of the Frizzled family of WNT receptors has hampered progress across the whole spectrum of biological fields in ...
Gennaro Riccio +10 more
openaire +5 more sources
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 +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 +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 +10 more
doaj +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 +11 more
openaire +4 more sources
A negative allosteric modulator of PDE4D enhances learning after traumatic brain injury. [PDF]
Neurobiol Learn Mem, 2018 •A PDE4D negative allosteric modulator did not alter cognition in non-injured rats.•Cognition after TBI is improved with a PDE4D negative allosteric modulator.•A PDE4D negative allosteric modulator improves LTP in TBI animals. Traumatic brain injury (TBI)
Titus DJ +6 more
europepmc +2 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 +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 +15 more
openaire +2 more sources