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Search results for: MUSCARINIC RECEPTORS
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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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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
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Structural and Pharmacological Characterization of Phenylalanine-Based AMPA Receptor Antagonists at Kainate Receptors
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RECEPTORS & CHANNELS
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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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Nuclear Receptor Signaling
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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),...
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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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Oxolane Ammonium Salts (Muscarine-Like)—Synthesis and Microbiological Activity
PublicationCommercially available 2-deoxy-D-ribose was used to synthesize the appropriate oxolane derivative—(2R,3S)-2-(hydroxymethyl)oxolan-3-ol—by reduction and dehydration/cyclization in an acidic aqueous solution. Its monotosyl derivative, as a result of the quaternization reaction, allowed us to obtain eight new muscarine-type derivatives containing a quaternary nitrogen atom and a hydroxyl group linked to the oxolane ring. Their structure...
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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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Classical Receptions Journal
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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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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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Journal of Receptor Ligand and Channel Research
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Expression of hCG and GnRHs and Their Receptors in Endometrial Carcinoma and Hyperplasia
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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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Angiotensin receptor blockers and endpoint protection
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Quantitative chirality in the binding of androgens to their receptor
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Vasopressin V2 receptor/bioligand interactions
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Neurotrophin serum concentrations and polymorphisms of neurotrophins and their receptors in children with asthma
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Estrogen receptors genes polymorphisms and age at menarche in idiopathic scoliosis
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Molecular Modeling of Interaction of the Vasopressin Analogs with Vasopressin and Oxytocin Receptors
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QSPR analysis of some agonists and antagonists of α-adrenergic receptors
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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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Estrogen receptor 2 polymorphism in idiopathic scoliosis
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Molecular Modeling of the Neurohypophyseal Receptor/Atosiban Complexes
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Affinity of fentanyl and its derivatives for the σ1-receptor
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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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Estrogen receptors 1 and 2 genotypes and age at menarche in idiopathic scoliosis
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Molecular Dynamics Study of the Internal Water Molecules in Vasopressin and Oxytocin Receptors
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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 estrogen receptors, PELP1, and SRC in human spermatozoa and their associations with semen quality
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Neurohypophyseal Receptors-Ligands: Where We Are After the Landmark Rhodopsin Structure Determination
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Molecular Dynamics of Complexes of Atosiban with Neurohypophyseal Receptors in the Fully Hydrated Phospholipid Bilayer
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Synthesis of Fentanyl Triazole Derivatives and their Affinity for Mu-Opioid and Sigma-1 Receptors
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Theoretical Study on Interactions of Bicyclic Vasopressin Analogues with Human Neurohypophyseal Hormone Receptors
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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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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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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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Trend research of vitamin D receptor: Bibliometric analysis
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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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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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Studies on Aryl-Substituted Phenylalanines: Synthesis, Activity, and Different Binding Modes at AMPA Receptors
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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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