Search Results - "Karcz, Tadeusz"
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1
UDP-glucose and P2Y14 receptor amplify allergen-induced airway eosinophilia
Published in The Journal of clinical investigation (01-04-2021)“…Airway eosinophilia is a hallmark of allergic asthma and is associated with mucus production, airway hyperresponsiveness, and shortness of breath. Although…”
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2
Thermal behavior and determination of physicochemical properties of novel candidates for antipsychotic drugs
Published in Journal of thermal analysis and calorimetry (01-09-2024)“…Treatment of schizophrenia with currently available drugs is often ineffective or results in several adverse reactions. In previous studies focusing on the…”
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3
Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y14R Antagonist
Published in Journal of medicinal chemistry (24-02-2022)“…High affinity phenyl-piperidine P2Y14R antagonist 1 (PPTN) was modified with piperidine bridging moieties to probe receptor affinity and hydrophobicity…”
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4
Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y 14 R Antagonist
Published in Journal of medicinal chemistry (24-02-2022)“…High affinity phenyl-piperidine P2Y R antagonist (PPTN) was modified with piperidine bridging moieties to probe receptor affinity and hydrophobicity. Various…”
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5
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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6
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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7
Structure-Activity Relationship of Heterocyclic P2Y 14 Receptor Antagonists: Removal of the Zwitterionic Character with Piperidine Bioisosteres
Published in Journal of medicinal chemistry (22-04-2021)“…A known zwitterionic, heterocyclic P2Y R antagonist was substituted with diverse groups on the central phenyl and terminal piperidine moieties, following a…”
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8
Structure–Activity Relationship of Heterocyclic P2Y14 Receptor Antagonists: Removal of the Zwitterionic Character with Piperidine Bioisosteres
Published in Journal of medicinal chemistry (22-04-2021)“…A known zwitterionic, heterocyclic P2Y14R antagonist 3a was substituted with diverse groups on the central phenyl and terminal piperidine moieties, following a…”
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9
Exploration of Alternative Scaffolds for P2Y14 Receptor Antagonists Containing a Biaryl Core
Published in Journal of medicinal chemistry (10-09-2020)“…Various heteroaryl and bicyclo-aliphatic analogues of zwitterionic biaryl P2Y14 receptor (P2Y14R) antagonists were synthesized, and affinity was measured in…”
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10
Exploration of Alternative Scaffolds for P2Y 14 Receptor Antagonists Containing a Biaryl Core
Published in Journal of medicinal chemistry (10-09-2020)“…Various heteroaryl and bicyclo-aliphatic analogues of zwitterionic biaryl P2Y receptor (P2Y R) antagonists were synthesized, and affinity was measured in P2Y…”
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11
Funnel metadynamics and behavioral studies reveal complex effect of D2AAK1 ligand on anxiety-like processes
Published in Scientific reports (07-12-2022)“…Anxiety is a troublesome symptom for many patients, especially those suffering from schizophrenia. Its regulation involves serotonin receptors, targeted e.g…”
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12
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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13
Adipocyte P2Y14 receptors play a key role in regulating whole-body glucose and lipid homeostasis
Published in JCI insight (24-05-2021)“…Obesity is the major driver of the worldwide epidemic in type 2 diabetes (T2D). In the obese state, chronically elevated plasma free fatty acid levels…”
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14
Xanthine-Dopamine Hybrid Molecules as Multitarget Drugs with Potential for the Treatment of Neurodegenerative Diseases
Published in Biomolecules (Basel, Switzerland) (01-07-2023)“…Multitarget drugs based on a hybrid dopamine-xanthine core were designed as potential drug candidates for the treatment of neurodegenerative diseases…”
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15
Magnolia Extract, Magnolol, and Metabolites: Activation of Cannabinoid CB2 Receptors and Blockade of the Related GPR55
Published in ACS medicinal chemistry letters (10-01-2013)“…The bark of Magnolia officinalis is used in Asian traditional medicine for the treatment of anxiety, sleeping disorders, and allergic diseases. We found that…”
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16
Effects of Purinergic Receptor Deletion or Pharmacologic Modulation on Pulmonary Inflammation in Mice
Published in ACS pharmacology & translational science (14-10-2022)“…COVID-19 disease is associated with progressive accumulation of SARS-CoV-2-specific mRNA, which is recognized by innate immune receptors, such as TLR3. This in…”
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17
Therapeutic suppression of pulmonary neutrophilia and allergic airway hyperresponsiveness by a RORγt inverse agonist
Published in JCI insight (25-07-2019)“…Airway neutrophilia occurs in approximately 50% of patients with asthma and is associated with particularly severe disease. Unfortunately, this form of asthma…”
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18
The P2Y purinoceptor, P2Y14R, promotes AHR in an animal model of asthma
Published in The Journal of immunology (1950) (01-05-2018)“…Abstract The initiation and propagation of immune responses in the lung are mediated in part by so-called ‘alarmins’ that include nucleotides and…”
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19
Trisubstituted 1,3,5-Triazines as Histamine H[sub.4] Receptor Antagonists with Promising Activity In Vivo
Published in Molecules (Basel, Switzerland) (01-05-2023)“…Pain is a very unpleasant experience that makes life extremely uncomfortable. The histamine H[sub.4] receptor (H[sub.4]R) is a promising target for the…”
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20
Endogenous UDP-Glc acts through the purinergic receptor P2RY14 to exacerbate eosinophilia and airway hyperresponsiveness in a protease model of allergic asthma
Published in The Journal of immunology (1950) (01-05-2019)“…Abstract Human asthma represents a wide spectrum of pathologies that likely arise through distinct molecular pathways, and a major therapeutic goal is to…”
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