Search results for "Pyran"

showing 4 items of 224 documents

Differential effects of potassium channel blockers on neurohypophysial release of oxytocin and vasopressin. Evidence for frequency-dependent interact…

1988

Isolated rat neurohypophyses were fixed by their stalks to a platinum wire electrode and superfused with Krebs-HEPES solution. Vasopressin and oxytocin released into the medium were determined by specific radioimmunoassays. Hormone secretion was increased by electrical stimulation of the pituitary stalk at different frequencies. The effects of several potassium channel blockers, tetraethylammonium (TEA) ions, 4-aminopyridine (4-AP) and 3,4-diaminopyridine (3,4-DAP) were tested. The release of vasopressin and oxytocin evoked by electrical stimulation with 900 pulses at 15 Hz (about 900 and 1,000 μU, respectively) was about 10 times higher than that evoked by 900 pulses at 3 Hz. Both 10 and 3…

medicine.medical_specialtyVasopressinCromakalimPotassium ChannelsVasopressinsRadioimmunoassayNeuropeptideAminopyridinesStimulation(+)-NaloxoneOxytocinPituitary Gland PosteriorInternal medicinemedicineAnimalsBenzopyransPyrroles4-AminopyridineEndogenous opioidPharmacologyChemistryNaloxoneTetraethylammoniumPotassium channel blockerRats Inbred StrainsGeneral MedicineTetraethylammonium CompoundsPotassium channelElectric StimulationRatsEndocrinologyOxytocinFemaleEndorphinsAmifampridinehormones hormone substitutes and hormone antagonistsmedicine.drugNaunyn-Schmiedeberg's archives of pharmacology
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Sequestration of biogenic amines by alginic and fulvic acids.

2006

The interaction of natural (alginic and fulvic acids) and synthetic (polyacrylic acid 2.0 kDa) polyelectrolytes with some protonated polyamines [diamines: ethylendiamine, 1,4-diaminobutane (or putrescine), 1,5-diaminopentane (or cadaverine); triamines: N-(3-aminopropyl)-1,4diaminobutane (or spermidine), diethylenetriamine; tetramine: N.N'-bis(3-aminopropyl)-1,4-diaminobutane (or spermine); pentamine: tetraethylene-pentamine; hexamine: pentaethylenehexamine] was studied at T=25 degrees C by potentiometry and calorimetry. Measurements were performed without supporting electrolyte, in order to avoid interference, and results were reported at I=0 mol L(-1). For all the systems, the formation of…

polyammonium-polycarboxylate interactionsAlginatesPolymersBiogenic aminesInorganic chemistryFulvic acidCarboxylic AcidsBiophysicsProtonationCalorimetryBiochemistryMedicinal chemistryElectrolyteschemistry.chemical_compoundbiogenic amineGlucuronic AcidPolyaminesBenzopyransAlginic acidPolyacrylic acidCadaverineChemistryHexuronic AcidsOrganic ChemistryPolyacrylic acidPentaminesequestrationPolyelectrolytesPolyelectrolyteQuaternary Ammonium CompoundsBiogenic amines; Fulvic acid; Alginic acid; Polyacrylic acid; sequestrationModels ChemicalDiethylenetriamineThermodynamicsAmine gas treatingProtonsMathematics
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Intramolecular Hydrogen Bond, Hirshfeld Analysis, AIM; DFT Studies of Pyran-2,4-dione Derivatives

2021

Intra and intermolecular interactions found in the developed crystals of the synthesized py-ron-2,4-dione derivatives play crucial rules in the molecular conformations and crystal stabili-ties, respectively. In this regard, Hirshfeld calculations were used to quantitatively analyze the different intermolecular interactions in the crystal structures of some functionalized py-ran-2,4-dione derivatives. The X-ray structure of pyran-2,4-dione derivative namely (3E,3′E)-3,3′-((ethane-1,2-diylbis(azanediyl))bis(phenylmethanylylidene))bis(6-phenyl-2H-pyran-2,4(3H)-dione) was determined. It crystallized in the monoclinic crystal system and C2/c space group with unit cell parameters: a = 14.0869(4) …

pyran-24-dioneGeneral Chemical Engineeringintramolecular hydrogen bondCrystal structure010402 general chemistryDFT01 natural sciencesInorganic Chemistrykemialliset sidoksetAIMMoleculeGeneral Materials Scienceorgaaniset yhdisteetCrystallography010405 organic chemistryHydrogen bondChemistryChemical shiftAtoms in moleculesIntermolecular forceHirshfeld analysiskiteetCondensed Matter Physics0104 chemical sciencesatomitCrystallographyQD901-999Intramolecular forceMonoclinic crystal systemCrystals
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Synthesis and Structure-Affinity Relationships of Spirocyclic Benzopyrans with Exocyclic Amino Moiety

2019

σ1 and/or σ2 receptors play a crucial role in pathological conditions such as pain, neurodegenerative disorders, and cancer. A set of spirocyclic cyclohexanes with diverse O-heterocycles and amino moieties (general structure III) was prepared and pharmacologically evaluated. In structure-activity relationships studies, the σ1 receptor affinity and σ1:σ2 selectivity were correlated with the stereochemistry, the kind and substitution pattern of the O-heterocycle, and the substituents at the exocyclic amino moiety. cis-configured 2-benzopyran cis-11b bearing a methoxy group and a tertiary cyclohexylmethylamino moiety showed the highest σ1 affinity ( Ki = 1.9 nM) of this series of compounds. In…

synthesisexocyclic amino moietyReceptors Opioid mudocking studieCrystallography X-RayLigands01 natural sciencesopioid receptorschemistry.chemical_compoundProtein structureDrug DiscoveryMoiety0303 health sciencesσ1 receptor ligandsstructure (σ1) affinity relationshipmolecular dynamicBenzyl groupMolecular MedicinesynthesiBenzopyransSelectivityHydrophobic and Hydrophilic Interactionsfree binding enthalpyStereochemistrychange of receptor profileMolecular Dynamics Simulation03 medical and health sciencesStructure-Activity Relationshipσ1 receptor ligands; spirocyclic compounds; benzopyrans; benzofurans; exocyclic amino moiety; synthesis; structure (σ1) affinity relationships; σ1 antagonistic activity; receptor selectivity; molecular dynamics; docking studies; free binding enthalpy; X-ray crystal structure; opioid receptors; MOR affinity; change of receptor profile; structure MOR affinity relationshipsstructure (σ1) affinity relationshipsStructure–activity relationshipHumansReceptors sigmaBenzopyransSpiro Compoundsspirocyclic compoundBinding siteMOR affinity030304 developmental biologybenzopyranbenzofuransσ1 receptor ligandBinding Sitesspirocyclic compoundsreceptor selectivitystructure MOR affinity relationshipsdocking studiesbenzofuranopioid receptorX-ray crystal structuremolecular dynamics0104 chemical sciencesProtein Structure Tertiary010404 medicinal & biomolecular chemistrychemistrySalt bridgeσ1 antagonistic activity
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