The evolving small-molecule fluorescent-conjugate toolbox for Class A GPCRs [PDF]
, 2013 The past decade has witnessed fluorescently tagged drug molecules gaining significant attraction in their use as pharmacological tools with which to visualize and interrogate receptor targets at the single-cell level.
Hill, Stephen J. +2 more
core +2 more sources
Pitolisant protects mice chronically treated with corticosterone from some behavioral but not metabolic changes in corticosterone-induced depression model [PDF]
, 2020 Purpose: Histamine H3 receptor ligands may have antidepressant and anxiolytic effects. They can also compensate for metabolic disorders, which affect glucose or triglyceride levels.
Kieć-Kononowicz, Katarzyna +6 more
core +2 more sources
cccDNA-Targeted Drug Screen Reveals a Class of Antihistamines as Suppressors of HBV Genome Levels
Biomolecules, 2023 Chronic infection with hepatitis B virus (HBV) is incurable, as the current therapeutics cannot eliminate its persistent genomic material, cccDNA. Screening systems for cccDNA-targeting therapeutics are unavailable, as low copies of cccDNA in vitro ...
Ee Chee Ren +5 more
doaj +1 more source
Prader Willi locus Snord116 RNA regulates hypothalamic functions: sleep and temperature [PDF]
, 2020 Sleep is a complex behavior and it is hierarchically regulated involving several brain regions, neurotransmitters, and genes that co-operate in building modulatory mechanisms aimed at controlling and maintaining sleep.
FALAPPA, MATTEO
core +1 more source
Substituted Purines as High-Affinity Histamine H3 Receptor Ligands
Pharmaceuticals, 2022 Continuing with our program to obtain new histamine H3 receptor (H3R) ligands, in this work we present the synthesis, H3R affinity and in silico studies of a series of eight new synthetically accessible purine derivatives.
Christian Espinosa-Bustos +7 more
doaj +1 more source
Przekaźnictwo histaminergiczne w narkolepsji typu 1 – implikacje terapeutyczne
Aktualności Neurologiczne, 2018 Narkolepsja typu 1 (narkolepsja z katapleksją) jest chorobą objawiającą się nadmierną sennością dzienną, niekontrolowanym zasypianiem, epizodami katapleksji (nagłej utraty napięcia mięśniowego), halucynacjami hipnagogicznymi i hipnopompicznymi oraz ...
Mariusz Siemiński
doaj +1 more source
Sleep MedicinePURPOSE Obstructive sleep apnea (OSA) is typically treated with continuous positive airway pressure (CPAP) therapy. Some patients experience residual excessive daytime sleepiness (EDS) under CPAP. Pitolisant demonstrated effectiveness in reducing EDS. An
D. Testelmans +5 more
semanticscholar +1 more source
Development of a conformational histamine H(3) receptor biosensor for the synchronous screening of agonists and inverse agonists [PDF]
, 2020 The histamine H(3) receptor (H(3)R) represents a highly attractive drug target for the treatment of various central nervous system disorders, but the discovery of novel H(3)R targeting compounds relies on the assessment of highly amplified intracellular ...
Leurs, R. +7 more
core +2 more sources
European guideline and expert statements on the management of narcolepsy in adults and children [PDF]
, 2021 Background and purpose: Narcolepsy is an uncommon hypothalamic disorder of presumed autoimmune origin that usually requires lifelong treatment. This paper aims to provide evidence-based guidelines for the management of narcolepsy in both adults and ...
Baldin, Elisa +17 more
core +11 more sources
Nature and Science of Sleep, 2020 Jay T Guevarra, Robert Hiensch, Andrew W Varga, David M Rapoport Division of Pulmonary, Critical Care, and Sleep Medicine, Mount Sinai Integrative Sleep Center, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USACorrespondence: Jay T ...
Guevarra JT +3 more
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