Search results for "Dihydropyridine"
showing 10 items of 70 documents
Spectroscopic and electrochemical study of interactions between DNA and different salts of 1,4-dihydropyridine AV-153
2020
1,4-dihydropyridines (1,4-DHP) possess important biochemical and pharmacological properties, including antimutagenic and DNA-binding activity. The latter activity was first described for water-soluble 1,4-DHP with carboxylic group in position 4, the sodium salt of the 1,4-DHP derivative AV-153 among others. Some data show the modification of physicochemical properties and biological activities of organic compounds by metal ions that form the salts. We demonstrated the different affinity to DNA and DNA-protecting capacity of AV-153 salts, depending on the salt-forming ion (Na, K, Li, Rb, Ca, Mg). This study aimed to use different approaches to collate data on the DNA-binding mode of AV-153-N…
Metal ions modify DNA-protecting and mutagen-scavenging capacities of the AV-153 1,4-dihydropyridine.
2019
Abstract 1,4-Dihydropyridines (1,4-DHP) possess important biochemical and pharmacological properties, including antioxidant and antimutagenic activities. AV-153-Na, an antimutagenic and DNA-repair enhancing compound was shown to interact with DNA by intercalation. Here we studied DNA binding of several AV-153 salts to evaluate the impact of AV-153 modifications on its DNA binding capacity, the ability to scavenge the peroxynitrite, to protect HeLa and B-cells cells against DNA damage. Affinity of the AV-153 salts to DNA measured by a fluorescence assay was dependent on the metal ion forming a salt in position 4 of the 1,4-DHP, and it decreased as follows: Mg > Na > Ca > Li > Rb > K. AV-153-…
DNA-binding studies of AV-153, an antimutagenic and DNA repair-stimulating derivative of 1,4-dihydropiridine.
2014
Abstract The ability to intercalate between DNA strands determines the cytotoxic activity of numerous anticancer drugs. Strikingly, intercalating activity was also reported for some compounds considered to be antimutagenic. The aim of this study was to determine the mode of interaction of DNA with the antimutagenic and DNA repair-stimulating dihydropyridine (DHP) AV-153. DNA and AV-153 interactions were studied by means of UV/VIS spectroscopy, fluorimetry and infrared spectroscopy. Compound AV-153 is a 1,4 dihydropyridine with ethoxycarbonyl groups in positions 3 and 5. Computer modeling of AV-153 and DNA interactions suggested an ability of the compound to dock between DNA strands at a sin…
Design of pharmacophoric group containing 1,4-dihydropyridine derivatives and determination of spectrum of pharmacological activities
2017
Vairākkārtīgi ir uzsvērts, ka 1,4-dihidropiridīna cikls ir viens no farmakoloģiski priviliģētām struktūrām, kas iedarbojas uz jonu kanāliem un dažādiem receptoriem, un kuru modificējot, sintezējot tās struktūras analogus, variējot aizvietotājus molekulā, būtu iespējams iegūt dažādus farmakoloģiski aktīvus savienojumus. Pētījumā ir sintezēti jauni, mērķtiecīgi dizainēti, farmakoforas grupas saturoši 1,4-dihidropiridīna atvasinājumi, sistemātiski mainot farmakoforās grupas (piridīniju un/vai propargil) un to atrašanās vietu molekulā. Izvērtēts sintezēto savienojumu farmakoloģiskās darbības spektrs (aktivitāte uz kalcija kanāliem, antiradikālā aktivitāte un reducējošā kapacitāte), veidots stru…
Evaluation of Physicochemical Properties of Amphiphilic 1,4-Dihydropyridines and Preparation of Magnetoliposomes
2021
This study was focused on the estimation of the targeted modification of 1,4-DHP core with (1) different alkyl chain lengths at 3,5-ester moieties of 1,4-DHP (C12, C14 and C16)
A Novel 1,4-Dihydropyridine Derivative Improves Spatial Learning and Memory and Modifies Brain Protein Expression in Wild Type and Transgenic APPSweD…
2015
Ca2+ blockers, particularly those capable of crossing the blood-brain barrier (BBB), have been suggested as a possible treatment or disease modifying agents for neurodegenerative disorders, e.g., Alzheimer's disease. The present study investigated the effects of a novel 4-(N-dodecyl) pyridinium group-containing 1,4-dihydropyridine derivative (AP-12) on cognition and synaptic protein expression in the brain. Treatment of AP-12 was investigated in wild type C57BL/6J mice and transgenic Alzheimer's disease model mice (Tg APPSweDI) using behavioral tests and immunohistochemistry, as well as mass spectrometry to assess the blood-brain barrier (BBB) penetration. The data demonstrated the ability …
1,5-Dimethyl-2-nitrimino-1,2-dihydropyridine
2006
Methylation of 5-methyl-2-nitraminopyridine provides the title compound, C7H9N3O2, as the only product. The molecule consists of two planar fragments, viz. an aromatic ring and a nitrimino substituent. The NNO2 group is twisted by 17 (2)° out of the plane of the pyridine ring. Despite a small torsion angle between these fragments, the geometry of the molecule indicates the participation of the π-electrons in the C—N bond. The hydrogen bonds in the crystal structure seem to be too weak to generate any deformations observed in the molecule.
Binding Sites for Ca2+‐Channel Effectors and Ryanodine inPeriplaneta americana—Possible Targets for New Insecticides
1996
The calcium channel and the 'calcium release channel' of muscle membrane of the cockroach Periplaneta americana have been characterized. Biological assays with calcium channel blockers and ryanodine on different insects and acari revealed pronounced insecticidal effects with ryanodine, but not with calcium channel blockers, at concentrations between 0.1 and 300 μg ml -1 . Skeletal muscle membranes derived either from the tubular network or from the sarcoplasmatic reticulum of P. americana were characterized with respect to the binding of the dihydropyridine (DHP) [ 3 H]isradipine (PN 200-110), the phenylalkylamine [ 3 H]verapamil and the alkaloid [ 3 H]ryanodine. Preliminary binding studies…
Studies of Preparation and Stability of Liposomes Formed by 1,1'-[(3,5-didodeciloxycarbonyl-4-phenyl-1,4-dihydropyridine-2,6-diil)-dimethylen]Bispyri…
2013
In this work we describe the studies of preparation and stability of liposomes formed by 1,1'-[(3,5-didodeciloxycarbonyl-4-phenyl-1,4-dihydropyridine-2,6-diil) dimethylebispyridinium dibromide, novel lipid-like compound. The influence of the amount of amphiphilic compound, solvent and sonication time was studied. Liposomes were prepared by dispersing of compound in the corresponding media at a selected concentration by sonication using a probe type sonicator and characterised by atomic force microscopy (AFM) and dynamic light scattering (DLS) methods.
Memory-enhancing and brain protein expression-stimulating effects of novel calcium antagonist in Alzheimer’s disease transgenic female mice
2016
The prevalence of Alzheimer's disease (AD) is higher in females than in males, and causes more severe cognitive, memory and behavioral impairments. Previously, in male transgenic (Tg) APPSweDI mice, we reported that the novel lipophilic 1,4-dihydropyridine (DHP) derivative AP-12 crossed the blood-brain barrier, blocked neuronal and vascular calcium channels, changed brain protein expression and improved behavior. In this study, we used female Tg APPSweDI mice to assess the effects of AP-12 on behavior, and brain protein expression, with a particular focus on those of the GABAergic system. The results showed that in female Tg mice, similar to male Tg mice, AP-12 improved spatial learning/mem…