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Search results for: receptory imidazolinowe
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new analogues of agmatine with higher activity to imidazoline receptors
PublicationOpracowano syntezę nowych pochodnych imidazoliny, będących kompilacją struktury agmatyny i imidazoliny w wyniku zaprojektowanej przez nas drogi syntezy. Kluczowymi substratami w syntezie były pochodne 1,2,4 -triaminobutanu, otrzymane z chronionego kwasu glutaminowego. Otrzymane nowe pochodne imidazoliny wykazywały zróżnicowane powinowactwo do receptorów imidazolinowych I1, I2 oraz do receptorów alfa -adrenergicznych.
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New imidazoline/alpha2-adrenoceptors affecting compounds - 4(5)-(2-aminoethyl)imidazoline (dihydrohistamine) derivatives. synthesis and receptor affinity studies
Publicationpołączenie struktury agmatyny i imidazoliny pozwoliło na otrzymanie nowej grupy ligandów receptorów imidazolinowych i alfa2-adrenergicznych, pochodnych 4(5)-(2-aminoetylo)imidazoliny. otrzymano oraz zbadano oddziaływanie nowych pochodnycch jak i analogów znanych ligandów - klonidyny, rilmenidyny, idazoksanu i antazoliny w stosunku do receptorów imidazolinowych oraz alfa2-adrenergicznych.
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Structural and Pharmacological Characterization of Phenylalanine-Based AMPA Receptor Antagonists at Kainate Receptors
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Analysis of interactions responsible for vasopressin binding to human neurohypophyseal hormone receptors—molecular dynamics study of the activated receptor–vasopressin–Gα systems
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Imidazolium ionic liquids in mineral processing
PublicationImidazoliowe ciecze jonowe (ILs) stanowią nową klasę związków o szerokich możliwościach przemysłowego zastosowania. Z przeglądu dostępnej literatury wynika, że ILs mogłyby zostać wykorzystane do odzysku i oczyszczania metali ze środowiska wodnego oraz rud w procesach ługowania, ekstarkcji rozpuszczalnikowej oraz w procesach elektrochemicznych. Pochodne imidazoliowe mogą być wykorzystywane zarówno jako rozpuszczalniki jak i aktywne...
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Molecular Docking-Based Study of Vasopressin Analogues Modified at Positions 2 and 3 with N-Methylphenylalanine: Influence on Receptor-Bound Conformations and Interactions with Vasopressin and Oxytocin Receptors
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Investigation of mechanism of desmopressin binding in vasopressin V2 receptor versus vasopressin V1a and oxytocin receptors: Molecular dynamics simulation of the agonist-bound state in the membrane–aqueous system
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Study of New Oxytocin Antagonist Barusiban (Fe200 440) Affinity Toward Human Oxytocin Receptor Versus Vasopressin V1a and V2 Receptors - Molecular Dynamics Simulation in POPC Bilayer
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Activation of Metabotropic Glutamate Receptor (mGlu2) and Muscarinic Receptors (M1, M4, and M5), Alone or in Combination, and Its Impact on the Acquisition and Retention of Learning in the Morris Water Maze, NMDA Expression and cGMP Synthesis
PublicationThe Morris water maze (MWM) is regarded as one of the most popular tests for detecting spatial memory in rodents. Long-term potentiation and cGMP synthesis seem to be among the crucial factors involved in this type of learning. Muscarinic (M1, M4, and M5 receptors) and metabotropic glutamate (mGlu) receptors are important targets in the search for antipsychotic drugs with the potency to treat cognitive disabilities associated with...
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Quantitative chirality in the binding of androgens to their receptor
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Angiotensin receptor blockers and endpoint protection
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Vasopressin V2 receptor/bioligand interactions
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Pyridylmethylsilanes as dicarboxyacid receptors: Experimental and theoretical study
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Estrogen Receptors in Cell Membranes: Regulation and Signaling
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Evidence for sex steroid receptors in feline brainstem
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Affinity of fentanyl and its derivatives for the σ1-receptor
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Molecular Modeling of the Neurohypophyseal Receptor/Atosiban Complexes
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Estrogen receptor 2 polymorphism in idiopathic scoliosis
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Selective detection of F- by chromogenic tetrazole receptor
PublicationA chromogenic anion host 4, containing two amide functionalities linked to azo dye and tetrazole rings was synthesized and its complexes with various anions were investigated. The results show that receptor 4 can recognize selectively biologically important F- ion. The binding affinity for F- was investigated by naked-eye colour change, UV-Vis and 1H NMR spectroscopy. Addition F- ion in CH3CN and DMSO to receptor 4 cause a colour...
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Moving out of CF3‐Land: Synthesis, Receptor Affinity, and in silico Studies of NK1 Receptor Ligands Containing a Pentafluorosulfanyl (SF5) Group
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Expression of α and β Estrogen Receptors in the Chicken Ovary
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Expression of hCG and GnRHs and Their Receptors in Endometrial Carcinoma and Hyperplasia
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Fosfonowe pochodne kaliks[4]arenów jako receptory w środowisku wodnym
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Gαi-derived peptide binds the µ-opioid receptor
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Molecular dynamics of fentanyl bound to μ-opioid receptor
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Estrogen Receptor 2 Gene Polymorphism in Idiopathic Scoliosis
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Aryl- and heteroaryl-substituted phenylalanines as AMPA receptor ligands
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Targeting melanocortin receptor type 1 with small peptides
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Vitamin D receptor(s): In the nucleus but also at membranes?
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Trend research of vitamin D receptor: Bibliometric analysis
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Towards β-selectivity in functional estrogen receptor antagonists
PublicationBased on the benzo[b]naphtho[1,2-d]furan and benzo[b]naphtho[1,2-d]thiophene frameworks, a series of ligands with different basic side chains (BSCs) has been synthesized and pharmacologically evaluated. Also, their binding modes have been modelled using docking techniques. It was found that the introduction of a BSC in these systems brings about a decrease of affinity for both estrogen receptors α and β in an in vitro competitive...
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New clicked full agonists of the estrogen receptor β
PublicationA click chemistry approach was used to synthesize a series of 1,4-diaryl-substituted 1,2,3-triazoles designed to behave as estrogen receptor (ER) ligands. We studied their affinities for both receptors α and β, their agonist activities in a cell-based luciferase reporter assay and their effect on the proliferation of the hormone-dependent MCF-7 cell line. We found two compounds (3a and 3c) that behave as selective full agonists...
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A new pH/organic modifier gradient RP HPLC method for convenient determination of lipophilicity and acidity of drugs as applied to established imidazoline agents
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QSPR analysis of some agonists and antagonists of α-adrenergic receptors
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Molecular Modeling of Interaction of the Vasopressin Analogs with Vasopressin and Oxytocin Receptors
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Estrogen receptors genes polymorphisms and age at menarche in idiopathic scoliosis
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Neurotrophin serum concentrations and polymorphisms of neurotrophins and their receptors in children with asthma
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Chromogenic amides of pyridine-2,6-dicarboxylic acid as anion receptors
PublicationThe synthesis of simple, chromogenic pyridine-2,6-dicarboxylic acid amides, derivates of isomeric nitroanilines and aminonitrophenols, and their ion binding properties are described. The ligands' response to ionic species was examined by naked eye and was studied with the use of UV-Vis spectroscopy in DMSO and its mixture with water. The effect of the localisation and the type of the substituents in aromatic rings were discussed....
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Tuning the sumanene receptor structure towards the development of potentiometric sensors
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Vitamin D receptor gene polymorphisms in Alzheimer's disease patients
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The neuroprotective activity of new phenylalanine-based AMPA receptor antagonists
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3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands
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RORα is not a receptor for melatonin (response to DOI 10.1002/bies.201600018)
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Molecular Dynamics of a Vasopressin V2 Receptor in a Phospholipid Bilayer Membrane
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Molecular Dynamics Study of the Internal Water Molecules in Vasopressin and Oxytocin Receptors
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Estrogen receptors 1 and 2 genotypes and age at menarche in idiopathic scoliosis
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Rola polimorfizmu i zróżnicowanej ekspresji genów cytochromu P450 w metabolizmie ksenobiotyków.
PublicationZdolność do metabolizmu ksenobiotyków przez cytochromy P450 (CYP) określona jest przez polimorfizm i poziom ekspresji genów tych białek. Najwięcej, 40 odmian polimorficznych o zróżnicowanej aktywności enzymatycznej, poznano dla CYP2D6, natomiast tylko dwie w przypadku CYP2C9, których obecność powoduje zahamowanie metabolizmu wielu leków. Z kolei polimorfizm genu CYP3A4 nie miał istotnego wpływu na aktywność metaboliczną jego produktu...
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Evaluation of Receptor Affinity, Analgesic Activity and Cytotoxicity of a Hybrid Peptide, AWL3020
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The FMO analysis of the molecular interaction of fentanyl derivatives with the μ-opioid receptor
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Angiotensin II receptor blocker combinations: From guidelines to clinical practice
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