Search Results - "Łażewska, Dorota"
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Potent, Selective Agonists for the Cannabinoid-like Orphan G Protein-Coupled Receptor GPR18: A Promising Drug Target for Cancer and Immunity
Published in Journal of medicinal chemistry (27-06-2024)“…The human orphan G protein-coupled receptor GPR18, activated by Δ9-tetrahydrocannabinol (THC), constitutes a promising drug target in immunology and cancer…”
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The Dual-Active Histamine H3 Receptor Antagonist and Acetylcholine Esterase Inhibitor E100 Alleviates Autistic-Like Behaviors and Oxidative Stress in Valproic Acid Induced Autism in Mice
Published in International journal of molecular sciences (03-06-2020)“…The histamine H3 receptor (H3R) functions as auto- and hetero-receptors, regulating the release of brain histamine (HA) and acetylcholine (ACh), respectively…”
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Dual Piperidine-Based Histamine H3 and Sigma‑1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain
Published in Journal of medicinal chemistry (27-07-2023)“…In search of new dual-acting histamine H3/sigma-1 receptor ligands, we designed a series of compounds structurally based on highly active in vivo ligands…”
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Multitargeting Histamine H3 Receptor Ligands among Acetyl- and Propionyl-Phenoxyalkyl Derivatives
Published in Molecules (Basel, Switzerland) (03-03-2023)“…Alzheimer’s disease (AD) is a neurodegenerative disorder, for which there is no effective cure. Current drugs only slow down the course of the disease, and,…”
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New Triazine Derivatives as Serotonin 5-HT6 Receptor Ligands
Published in Molecules (Basel, Switzerland) (22-01-2023)“…Since the number of people with Alzheimer’s disease (AD) continues to rise, new and effective drugs are urgently needed to not only slow down the progression…”
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Structural and Molecular Insight into Piperazine and Piperidine Derivatives as Histamine H3 and Sigma‑1 Receptor Antagonists with Promising Antinociceptive Properties
Published in ACS chemical neuroscience (05-01-2022)“…In an attempt to extend recent studies showing that some clinically evaluated histamine H3 receptor (H3R) antagonists possess nanomolar affinity at sigma-1…”
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AR71, Histamine H3 Receptor Ligand—In Vitro and In Vivo Evaluation (Anti-Inflammatory Activity, Metabolic Stability, Toxicity, and Analgesic Action)
Published in International journal of molecular sciences (01-08-2024)“…The future of therapy for neurodegenerative diseases (NDs) relies on new strategies targeting multiple pharmacological pathways. Our research led to obtaining…”
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Anti-Inflammatory Activities of 8-Benzylaminoxanthines Showing High Adenosine A2A and Dual A1/A2A Receptor Affinity
Published in International journal of molecular sciences (05-09-2023)“…Chronic inflammation plays an important role in the development of neurodegenerative diseases, such as Parkinson’s disease (PD). In the present study, we…”
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Reproductive and fetal toxicity studies of histamine H3 receptor antagonist DL76 used in mice to prevent maximal electroshock-induced seizure
Published in Frontiers in pharmacology (05-06-2024)“…Brain histamine is considered an endogenous anticonvulsant and histamine H1 receptor. H1R antagonists have, in earlier studies, been found to induce…”
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Rational design of new multitarget histamine H 3 receptor ligands as potential candidates for treatment of Alzheimer's disease
Published in European journal of medicinal chemistry (01-12-2020)“…Design and development of multitarget-directed ligands (MTDLs) has become a very important approach in the search of new therapies for Alzheimer's disease…”
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Synthesis and computer-aided SAR studies for derivatives of phenoxyalkyl-1,3,5-triazine as the new potent ligands for serotonin receptors 5-HT6
Published in European journal of medicinal chemistry (15-09-2019)“…This research has provided the most active 5-HT6R agents among 1,3,5-triazine derivatives investigated to date and has also identified the world's first…”
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Trisubstituted 1,3,5-Triazines as Histamine H4 Receptor Antagonists with Promising Activity In Vivo
Published in Molecules (Basel, Switzerland) (19-05-2023)“…Pain is a very unpleasant experience that makes life extremely uncomfortable. The histamine H4 receptor (H4R) is a promising target for the treatment of…”
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Role of Histamine H₃ Receptor Antagonists on Intraocular Pressure Reduction in Rabbit Models of Transient Ocular Hypertension and Glaucoma
Published in International journal of molecular sciences (24-02-2019)“…Intraocular pressure (IOP) has a tendency to fluctuate throughout the day, reaching its peak in the early morning in healthy subjects or glaucoma patients…”
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Benzophenone Derivatives with Histamine H3 Receptor Affinity and Cholinesterase Inhibitory Potency as Multitarget-Directed Ligands for Possible Therapy of Alzheimer’s Disease
Published in Molecules (Basel, Switzerland) (28-12-2022)“…The multitarget-directed ligands demonstrating affinity to histamine H3 receptor and additional cholinesterase inhibitory potency represent a promising…”
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Biphenylalkoxyamine Derivatives–Histamine H3 Receptor Ligands with Butyrylcholinesterase Inhibitory Activity
Published in Molecules (Basel, Switzerland) (11-06-2021)“…Neurodegenerative diseases, e.g., Alzheimer’s disease (AD), are a key health problem in the aging population. The lack of effective therapy and diagnostics…”
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Dual Target Ligands with 4-tert-Butylphenoxy Scaffold as Histamine H3 Receptor Antagonists and Monoamine Oxidase B Inhibitors
Published in International journal of molecular sciences (12-05-2020)“…Dual target ligands are a promising concept for the treatment of Parkinson’s disease (PD). A combination of monoamine oxidase B (MAO B) inhibition with…”
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Benzophenone Derivatives with Histamine H 3 Receptor Affinity and Cholinesterase Inhibitory Potency as Multitarget-Directed Ligands for Possible Therapy of Alzheimer's Disease
Published in Molecules (Basel, Switzerland) (01-01-2023)“…The multitarget-directed ligands demonstrating affinity to histamine H receptor and additional cholinesterase inhibitory potency represent a promising strategy…”
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Law and Literature.The Places for Metaphysical Thinking
Published in Journal of Modern Science (23-07-2018)“…Objectives The aim of this study is to identify places of metaphysical thinking in law and in literature.As metaphysical thinking is the search for the causes…”
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Dual Targeting Ligands—Histamine H3 Receptor Ligands with Monoamine Oxidase B Inhibitory Activity—In Vitro and In Vivo Evaluation
Published in Pharmaceutics (13-10-2022)“…The clinical symptoms of Parkinson’s disease (PD) appear when dopamine (DA) concentrations in the striatum drops to around 20%. Simultaneous inhibitory effects…”
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Anticonvulsant and procognitive properties of the non-imidazole histamine H3 receptor antagonist DL77 in male adult rats
Published in Neuropharmacology (01-07-2016)“…It has become clear that histamine H3 receptors (H3Rs) are implicated in modulating epilepsy and memory in laboratory animals. The new non-imidazole H3R…”
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