A5045614575- Mast cells and histamine
- Receptor Mechanisms and Signaling
- Auction Theory and Applications
- Phenothiazines and Benzothiazines Synthesis and Activities
- Click Chemistry and Applications
- Neuropeptides and Animal Physiology
- Experimental Behavioral Economics Studies
- Consumer Market Behavior and Pricing
- Chemical Synthesis and Analysis
- Circadian rhythm and melatonin
- Free Radicals and Antioxidants
- Neuroinflammation and Neurodegeneration Mechanisms
- Blockchain Technology Applications and Security
- Game Theory and Applications
- Adenosine and Purinergic Signaling
- Synthesis and Characterization of Heterocyclic Compounds
- Computational Drug Discovery Methods
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Evolutionary Game Theory and Cooperation
- Pain Mechanisms and Treatments
- Synthesis and biological activity
- Cholinesterase and Neurodegenerative Diseases
- Olfactory and Sensory Function Studies
Heinrich Heine University Düsseldorf
2022-2025
Max Planck Institute for Human Development
2023
Alzheimer's disease (AD) is a multifactorial neurodegenerative with manifold underlying pathophysiological mechanisms. Therefore, multitarget-directed ligands potentially offer beneficial therapeutic effects compared classical therapies. Dual targeting of the histamine H3 receptor (H3R) and acetylcholinesterase (AChE) valid strategy for treatment AD. In this work, new series pyrrolo[2,3-d]pyrimidines fused to fluorobenzylpiperidine derivatives was designed, synthesized, pharmacologically...
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This study examines the properties of a novel series 4-oxypiperidines designed and synthesized as histamine H3R antagonists/inverse agonists based on structural modification two lead compounds, viz., ADS003 ADS009. The products are intended to maintain high affinity for while simultaneously inhibiting AChE or/and BuChE enzymes. Selected compounds were subjected hH3R radioligand displacement gpH3R functional assays. Some showed nanomolar affinity. most promising compound in naphthalene was...
This study examines the properties of novel guanidines, designed and synthesized as histamine H3R antagonists/inverse agonists with additional pharmacological targets. We evaluated their potential against two targets viz., inhibition MDA-MB-231, MCF-7 breast cancer cells viability AChE/BuChE. ADS10310 showed micromolar cytotoxicity cells, combined nanomolar affinity at hH3R, may represent a promising target for development an alternative method therapy. Some newly compounds moderate BuChE in...
Microglia play an important role in the neuroinflammation developed response to various pathologies. In this study, we examined anti-inflammatory effect of new human histamine H3 receptor (H3R) ligands with flavonoid structure murine microglial BV-2 cells.The affinity flavonoids (E243 -flavone and IIIa-IIIc-chalcones) for H3R was evaluated radioligand binding assay. The cytotoxicity on cell viability investigated MTS Preliminary evaluation properties screened by Griess assay vitro model...
Pain is a very unpleasant experience that makes life extremely uncomfortable. The histamine H4 receptor (H4R) promising target for the treatment of inflammatory and immune diseases, as well pain. H4R ligands have demonstrated analgesic effects in variety pain models, including Continuing search active among alkyl derivatives 1,3,5-triazine, we obtained 19 new compounds two series: acyclic (I) aliphatic (II). In vitro pharmacological evaluation showed their variable affinity H4R. majority...
This paper investigates the collusive and competitive effects of algorithmic price recommendations on market outcomes. These are often non-binding common in many markets, especially online platforms. We develop a theoretical framework derive two algorithms that recommend pricing strategies. Utilizing laboratory experiment, we find sellers condition their prices recommendation algorithms. The algorithm with soft punishment strategy lowers has pro-competitive effect. recommends subgame perfect...
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Neurodegenerative diseases are a major public health problem due to the aging population and multifaceted pathology; therefore, search for new therapeutic alternatives is of utmost importance. In this sense, series six 1-(3-phenoxypropyl)piperidines alkyl-linked triphenylphosphonium cation derivative were synthesized as H
Autism spectrum disorder is a complex neurodevelopmental disorder. The available medical treatment options for autism are very limited. While the etiology and pathophysiology of still not fully understood, recent studies have suggested that wide alterations in GABAergic, glutamatergic, cholinergic, serotonergic systems play key role its development progression. Histamine neurotransmission known to interactions with other neurotransmitters fit perfectly into this disease. Multitarget-directed...