Pharmaceutics, 2022 The clinical symptoms of Parkinson’s disease (PD) appear when dopamine (DA) concentrations in the striatum drops to around 20%. Simultaneous inhibitory effects on histamine H3 receptor (H3R) and MAO B can increase DA levels in the brain.
Dorota Łażewska +15 more
doaj +1 more source
Pharmacology Research & Perspectives, 2021 Several therapeutic options are currently available to treat excessive daytime sleepiness (EDS) in patients suffering from narcolepsy or obstructive sleep apnea.
Stéphane Krief +11 more
doaj +1 more source
Nonclinical cardiovascular safety of pitolisant: comparing International Conference on Harmonization S7B and Comprehensive in vitro Pro-arrhythmia Assay initiative studies [PDF]
, 2017 Background and purpose: We evaluated the concordance of results from two sets of nonclinical cardiovascular safety studies on pitolisant. Experimental approach: Nonclinical studies envisaged both in the ICH S7B guideline and Comprehensive in vitro ...
Alexander +51 more
core +3 more sources
Pitolisant in an Adolescent with Prader-Willi Syndrome
The Journal of Pediatric Pharmacology and Therapeutics, 2021 This case report evaluates the potential benefit of pitolisant in a 15-year-old female with Prader-Willi syndrome, obsessive-compulsive disorder, autism spectrum disorder, and mild intellectual disability. Due to its action on the H3 receptor, it enhances central activity of histaminergic neurons resulting in increased alertness, irrespective of the ...
Stephanie, Pennington +2 more
openaire +3 more sources
The UK myotonic dystrophy patient registry: facilitating and accelerating clinical research [PDF]
, 2017 Myotonic dystrophy type 1 (DM1) is the most frequent muscular dystrophy worldwide with complex, multi-systemic, and progressively worsening symptoms. There is currently no treatment for this inherited disorder and research can be challenging due to the ...
Atalaia, Antonio +18 more
core +4 more sources
Pitolisant for Daytime Sleepiness in Patients with Obstructive Sleep Apnea Who Refuse Continuous Positive Airway Pressure Treatment A Randomized Trial [PDF]
, 2020 Rationale: Excessive daytime sleepiness is a common disabling symptom in obstructive sleep apnea syndrome. Objectives: To evaluate the efficacy and safety of pitolisant, a selective histamine H3 receptor antagonist with wake-promoting effects, for the ...
Dauvilliers, Yves +4 more
core +1 more source
Medicines, 2020 Background: Besides its well-known role as a peripheral chemical mediator of immune, vascular, and cellular responses, histamine plays major roles in the central nervous system, particularly in the mediation of arousal and cognition-enhancement.
Victoria Harwell, Pius S. Fasinu
doaj +1 more source
Effects of an H3R Antagonist on the Animal Model of Autism Induced by Prenatal Exposure to Valproic Acid [PDF]
, 2015 Autism spectrum disorders (ASD) are a group of neurodevelopmental disorders primarily characterized by impaired social interaction and communication, and by restricted repetitive behaviors and interests.
A Burban +53 more
core +2 more sources
Computational design of syntheses leading to compound libraries or isotopically labelled targets [PDF]
, 2019 Although computer programs for retrosynthetic planning have shown improved and in some cases quite satisfactory performance in designing routes leading to specific, individual targets, no algorithms capable of planning syntheses of entire target ...
Abu-El-Haj +80 more
core +1 more source
Novel chalcone-based fluorescent human histamine H 3 receptor ligands as pharmacological tools [PDF]
, 2012 Novel fluorescent chalcone-based ligands at human histamine H(3) receptors (hH(3)R) have been designed, synthesized, and characterized. Compounds described are non-imidazole analogs of ciproxifan with a tetralone motif.
Tomasch, Miriam +3 more
core +1 more source