Search
Filters
total: 441
filtered: 248
Search results for: receptory imidazolinowe
-
Intrinsic effects of AM4113, a putative neutral CB1 receptor selective antagonist, on open-field behaviors in rats
PublicationW pracy przedstawiono wyniki testów otartego pola na zachowanie szczurów po iniekcji zwierzętom WIN55,21-2 (WIN; 3 mg/kg) agonisty receptora kanabinoidowego CB1R, bądź AM4113 (0.3−5.6 mg/kg) przypuszczalnie neutralnego antagonisty receptora kanabinoidowego CB1R oraz mieszaniny obu związków. W badaniach pod uwagę brano następujące zachowania zwierząt; ilość kwadratów, którą szczury przechodziły na czterech nogach, częstotliwość...
-
Ambulatory Blood Pressure Adds to Explaining Benefits of AT‐1 Receptor Blockade in the Treatment of Left Ventricular Hypertrophy
Publication -
Docking is not enough: 17-trifluoromethylphenyl trinor PGF2α is only a very weak ligand of neurokinin-1 receptor
Publication -
Correcting a widespread error: Neuroprotectant N-acetyl-L-tryptophan does not bind to the neurokinin-1 receptor
Publication -
Phase 3 randomised study of avatrombopag, a novel thrombopoietin receptor agonist for the treatment of chronic immune thrombocytopenia
Publication -
Optimization of Chemical Functionalities of Indole-2-carboxamides To Improve Allosteric Parameters for the Cannabinoid Receptor 1 (CB1)
Publication5-Chloro-3-ethyl-N-(4-(piperidin-1-yl)phenethyl)-1H-indole-2-carboxamide (1; ORG27569) is a prototypical allosteric modulator for the cannabinoid type 1 receptor (CB1). Here, we reveal key structural requirements of indole-2-carboxamides for allosteric modulation of CB1: a critical chain length at the C3-position, an electron withdrawing group at the C5-position, the length of the linker between the amide bond and the phenyl ring...
-
Interactions of vasopressin and oxytocin receptors with vasopressin analogues substituted in position 2 with 3,3′-diphenylalanine - a molecular docking study
Publication -
O-substituted tetrahydroxamate derivatives of p-tert-butylcalix[4]arene as receptors for transition and heavy metal cations
PublicationTetrasubstituted O-hydroxamate derivatives of p-tert-butylcalix[4]arene were applied as active materials in ion-selective membrane electrodes and were tested towards Pb-selectivity. The electrodes gave near-Nernstian characteristics for Pb2+ cations. The selectivity coefficients were determined. The influence of plasticizer on the electrode behaviour was studied. The dependence of the chemical structure on selectivity coefficients...
-
An Influence of the Aromatic Side Chains Conformations in Positions 2 and 3 of Vasopressin Analogs on Interactions with Vasopressin and Oxytocin Receptors
Publication -
Effect of psoriasis activity and topical treatment on plasma epidermal growth factor (EGF) and its soluble receptor (sEGFR)
Publication -
XbaI and PvuII Polymorphisms of Estrogen Receptor 1 Gene in Females with Idiopathic Scoliosis: No Association with Occurrence or Clinical Form
Publication -
Methylation level of the regulatory regions of the estrogen receptor type 1 gene in paravertebral muscles of girls with idiopathic scoliosis
Publication -
Effect of psoriasis activity on epidermal growth factor (EGF) and the concentration of soluble EGF receptor in serum and plaque scales
Publication -
Methylation of Estrogen Receptor 1 Gene in the Paraspinal Muscles of Girls with Idiopathic Scoliosis and Its Association with Disease Severity
Publication -
N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H3 receptor and cancer resistance proteins
Publication -
Nephrotic syndrome unfavorable course correlates with downregulation of podocyte vascular endothelial growth factor receptor (VEGFR)-2
Publication -
Radiochemical Synthesis and Evaluation of Novel Radioconjugates of Neurokinin 1 Receptor Antagonist Aprepitant Dedicated for NK1R-Positive Tumors
Publication -
The Leaderless Bacteriocin Enterocin K1 Is Highly Potent against Enterococcus faecium: A Study on Structure, Target Spectrum and Receptor
Publication -
Vitamin D Receptor Gene Polymorphism and Vitamin D Status in Population of Patients with Cardiovascular Disease—A Preliminary Study
Publication -
New generation of analytical tests based on the assessment of enzymatic and nuclear receptor activity changes induced by environmental pollutants
PublicationAnalytical methods show great potential in biological tests. The analysis of biological response that results from environmental pollutant exposure allows: (i) prediction of the risk of toxic effects and (ii) provision of the background for the development of markers of the toxicants presence. Bioanalytical tests based on changes in enzymatic activity and nuclear receptor action provide extremely high specificity and sensitivity....
-
Polymorphism in the chemokine receptor 7 gene (CCR7) is associated with previous myocardial infarction in patients undergoing elective coronary angiography
Publication -
Synthesis, activity on NK-3 tachykinin receptor and conformational solution studies of scyliorhinin II analogs modified at position 16
Publication -
Does Porcine Oocytes Maturation in Vitro is Regulated by Genes Involved in Transforming Growth Factor Beta Receptor Signaling Pathway?
Publication -
Novel Potent Muscarinic Receptor Antagonists: Investigation on the Nature of Lipophilic Substituents in the 5- and/or 6-Positions of the 1,4-Dioxane Nucleus
Publication -
Molecular dynamics study of 4-OH-phenylacetyl- D -Y(Me)FQNRPR-NH 2 selectivity to V1a receptor
Publication -
Amberlyst-15 catalysed synthesis of novel indole derivatives under ultrasound irradiation: Their evaluation as serotonin 5‑HT2C receptor agonists
Publication -
Amberlyst-15 catalysed synthesis of novel indole derivatives under ultrasound irradiation: Their evaluation as serotonin 5‑HT2C receptor agonists
PublicationA series of indole based novel Schiff bases was designed as potential agonists of 5‑HT2C receptor that was supported by docking studies in silico. These compounds were synthesized via Amberlyst-15 catalysed condensation of an appropriate pyrazole based primary amine with the corresponding indole-3-aldehyde under ultrasound irradiation at ambient temperature. A number of target Schiff bases were obtained...
-
Naphthyl-vs. anthrylpyridine-2,6-dicarboxamides in cation binding studies. Synthesis and spectroscopic properties
PublicationPyridine-2,6-carboxamides bearing - or -naphthyl- and - or -anthryl- residues were prepared using simple method from pyridine-2,6-carboxylic acid dichloride and the respective aromatic amines. For the obtained receptors selective binding of lead(II), and copper(II) was found. Ion-receptor interactions were studied using UV-vis spectroscopy, spectrofluorimetry, 1H NMR, and FTIR spectroscopy. The reversible lead(II) and copper(II)...
-
Cannabinoid CB1 antagonists and dopamine antagonists produce different effects on a task involving response allocation and effort-related choice in food-seeking behavior
PublicationW przeprowadzonych badaniach iniekcja antagonistów dopaminy (DA) szczurom powoduje znaczny spadek użycia siły przez zwierzęta w poszukiwaniu żywności i jednoczesny wzrost spożycia jedzenia laboratoryjnego. Przeciwnie, iniekcja antagonisty AM4113 lub odwrotnego agonisty AM251 receptora CB1 powoduje zmniejszenie ilości jedzenia granulek, ale nie wpływa na zwiększenie konsumpcji jedzenia laboratoryjnego. Efekty wywierane na zwierzęta...
-
Phenylalanine derivatives with modulating effects on human α1-glycine receptors and anticonvulsant activity in strychnine-induced seizure model in male adult rats
Publication -
Pharmacophore models based studies on the affinity and selectivity toward 5-HT1A with reference to α1-adrenergic receptors among arylpiperazine derivatives of phenytoin
Publication -
Estrogen Receptor Type 1 and Type 2 Presence in Paravertebral Skeletal Muscles: Expression Level and Relation to Phenotype in Children with Idiopathic Scoliosis
Publication -
Expression of Estrogen Receptor Coactivator Proline-, Glutamic Acid- and Leucine-Rich Protein 1 within Paraspinal Muscles in Adolescents with Idiopathic Scoliosis
Publication -
Efficacy of high-dose corticosteroid-based treatment for chronic lymphocytic leukemia patients with p53 abnormalities in the era of B-cell receptor inhibitors
Publication -
A New Phenylalanine Derivative Acts as an Antagonist at the AMPA Receptor GluA2 and Introduces Partial Domain Closure: Synthesis, Resolution, Pharmacology, and Crystal Structure
Publication -
The effect of sunscreen 4‐methylbenzylidene camphor in different and reproductive models, its bioaccumulation and molecular effects on ligand‐receptor interaction, and protein expression
Publication4-Methylbenzylidene camphor (4-MBC) is a photo-absorbing UV filter prevalently used in cosmetics, which can be absorbed into circulation and cause systemic effects. 4-MBC is continued to be released in the environment despite the growing knowledge about its bioaccumulation and endocrine disrupting effects. Previous reviews have mentioned UV-filter together but this review considers 4-MBC alone, due to its prevalence and concerning...
-
Texture or Linker? Competitive Patterning of Receptor Assembly toward Ultra-Sensitive Impedimetric Detection of Viral Species at Gold-Nanotextured Titanium Surfaces
PublicationIn this work, we study the electrodes with a periodic matrix of gold particles pattered by titanium dimples and modified by 3-mercaptopropionic acid (MPA) followed by CD147 receptor grafting for specific impedimetric detection of SARS-CoV-2 viral spike proteins. The synergistic DFT and MM/MD modeling revealed that MPA adsorption geometries on the Au–Ti surface have preferential and stronger binding patterns through the carboxyl...
-
Agrimoniin up-regulates collagen biosynthesis through increase in expression of β1-integrin receptor and prolidase activity in cultured human skin fibroblasts
Publication -
Molecularly targeted nanoparticles: an emerging tool for evaluation of expression of the receptor for advanced glycation end products in a murine model of peripheral artery disease
PublicationAbstract Background: Molecular imaging with molecularly targeted probes is a powerful tool for studying the spatio-temporal interactions between complex biological processes. The pivotal role of the receptor for advanced glycation end products (RAGE) in numerous pathological processes, aroused the demand for RAGE targeted imaging in various diseases. In the study, we evaluated the use of a diagnostic imaging agent for RAGE quantification...
-
Can cornelian cherry mask bitter taste of probiotic chocolate? Human TAS2R receptors and a sensory study with comprehensive characterisation of new functional product
Publication -
Safety and efficacy of P2X3 receptor antagonist for the treatment of refractory or unexplained chronic cough: A systematic review and meta-analysis of 11 randomized controlled trials
Publication -
The novel cannabinoid CB1 receptor neutral antagonist AM4113 suppresses ood intake and food-reinforced behavior but does not induce signs of nausea in rats
PublicationPrzeprowadzone badania biochemiczne wykazują, że związek AM4113 wiąże się z receptorem kanabinoidowym CB1, ale nie wykazuje właściwości odwrotnego agonisty (między innymi nie wpływa na powstawanie cyklicznego AMP). W testach na swobodne przemieszczanie się szczurów i znieczulenie związek AM4113 osłabia wpływ agonisty AM411 na receptor CB1. AM4113 wpływa na zachowanie szczurów związane z karmieniem oraz powoduje spadek łaknienia...
-
Prenatal stress affects insulin-like growth factor-1 (IGF-1) level and IGF-1 receptor phosphorylation in the brain of adult rats
Publication -
Enhanced susceptibility of SARS-CoV-2 spike RBD protein assay targeted by cellular receptors ACE2 and CD147: Multivariate data analysis of multisine impedimetric response
PublicationSevere acute respiratory syndrome coronavirus 2 (SARS-CoV-2) enters the cells through the binding of spike protein to the host cell surface-expressing angiotensin-converting enzyme 2 (ACE2) or by endocytosis mediated by extracellular matrix metalloproteinase inducer (CD147). We present extended statistical studies of the multisine dynamic electrochemical impedance spectroscopy (DEIS) revealing interactions between Spike RBD and...
-
Serotonergic–Muscarinic Interaction within the Prefrontal Cortex as a Novel Target to Reverse Schizophrenia-Related Cognitive Symptoms
PublicationRecent studies revealed that the activation of serotonergic 5-HT1A and muscarinic M1, M4, or M5 receptors prevent MK-801-induced cognitive impairments in animal models. In the present study, the effectiveness of the simultaneous activation of 5-HT1A and muscarinic receptors at preventing MK-801-induced cognitive deficits in novel object recognition (NOR) or Y-maze tests was investigated. Activators of 5-HT1A (F15599), M1 (VU0357017),...
-
Phytochemical screening and effect of Viscum album L. on monoamine oxidase A and B activity and serotonin, dopamine and serotonin receptor 5-HTR1A levels in Galleria mellonealla (Lepidoptera)
Publication -
The PARAGON Heart Failure trial – ongoing investigation of the angiotensin receptor antagonist/neprilysin inhibitor sacubitril/valsartan in heart failure patients with hypertension and preserved ejection fraction
Publication -
Efficacy and safety of B-cell receptor signaling pathway inhibitors in relapsed/refractory chronic lymphocytic leukemia: a systematic review and meta-analysis of randomized clinical trials
Publication -
Molecular cloning and initial characterization of African green monkey (Cercopithecus aethiops) corticotropin releasing factor receptor type 1 (CRF1) from COS-7 cells
Publication -
Influence of Estradiol-17beta on Progesterone and Estrogen Receptor mRNA Expression in Porcine Follicular Granulosa Cells during Short-Term, In Vitro Real-Time Cell Proliferation
Publication