Results 41 to 50 of about 4,995,094 (293)
Positive Allosteric Modulators of Nicotinic Acetylcholine Receptor [PDF]
ACS Medicinal Chemistry Letters, 2013 Priority Application: Priority date: July 8, 2011 Inventors: Eskildsen, J.; Sams, A. G.; Pueschl, A. Assignee Company: H. Lundbeck A/S, Den. Disease Area: autism, neurodegenerative diseases Biological Target: nicotinic acetylcholine receptor α7 (α7 nAChR) Summary: The patent application claims cyclopropylcarboxamide derivatives as positive allosteric ...
openaire +2 more sources
Positive Allosteric Modulation of TRPV1 as a Novel Analgesic Mechanism [PDF]
Molecular Pain, 2012 Background: The prevalence of long-term opiate use in treating chronic non-cancer pain is increasing, and prescription opioid abuse and dependence are a major public health concern. To explore alternatives to opioid-based analgesia, the present study investigates a novel allosteric pharmacological approach operating through the cation channel TRPV1 ...
Lebovitz Evan E +5 more
openaire +3 more sources
, 2023 International audienceThe α7 nicotinic acetylcholine receptor (nAChR), a potential drug target for treating cognitive disorders, mediates communication between neuronal and non- neuronal cells. Although many competitive antagonists, agonists, and partial-
Stéphanie Pons +21 more
core +1 more source
eLife, 2020 Pentameric ligand-gated ion channels (pLGICs) or Cys-loop receptors are involved in fast synaptic signaling in the nervous system. Allosteric modulators bind to sites that are remote from the neurotransmitter binding site, but modify coupling of ligand ...
Marijke Brams +12 more
doaj +1 more source
Pepcan-12 (RVD-hemopressin) is a CB2 receptor positive allosteric modulator constitutively secreted by adrenals and in liver upon tissue damage. [PDF]
, 2017 Pepcan-12 (RVD-hemopressin; RVDPVNFKLLSH) is the major peptide of a family of endogenous peptide endocannabinoids (pepcans) shown to act as negative allosteric modulators (NAM) of cannabinoid CB1 receptors.
Chicca, Andrea +13 more
core +2 more sources
Understanding the Allosteric Modulation of PTH1R by a Negative Allosteric Modulator
Cells, 2022 The parathyroid hormone type 1 receptor (PTH1R) acts as a canonical class B G protein-coupled receptor, regulating crucial functions including calcium homeostasis and bone formation.
Mengrong Li +5 more
doaj +1 more source
GABAA receptor: Positive and negative allosteric modulators [PDF]
Neuropharmacology, 2018 gamma-Aminobutyric acid (GABA)-mediated inhibitory neurotransmission and the gene products involved were discovered during the mid-twentieth century. Historically, myriad existing nervous system drugs act as positive and negative allosteric modulators of these proteins, making GABA a major component of modern neuropharmacology, and suggesting that many
openaire +2 more sources
An allosteric modulator binds to a conformational hub in the β2 adrenergic receptor [PDF]
, 2020 Most drugs acting on G-protein-coupled receptors target the orthosteric binding pocket where the native hormone or neurotransmitter binds. There is much interest in finding allosteric ligands for these targets because they modulate physiologic signaling ...
Hirata, Kunio +31 more
core +1 more source
Allo-network drugs: Extension of the allosteric drug concept to protein-protein interaction and signaling networks [PDF]
, 2013 Allosteric drugs are usually more specific and have fewer side effects than orthosteric drugs targeting the same protein. Here, we overview the current knowledge on allosteric signal transmission from the network point of view, and show that most ...
Csermely, Péter +3 more
core +2 more sources
, 2023 Structure-Activity Relationship Study of the High-Affinity Neuropeptide Y4 Receptor Positive Allosteric Modulator ...
Y Du (6951416) +10 more
core