Adamantane: A tricyclo bridged hydrocarbon.Rimantadine: An RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza.Influenza A Virus, H3N2 Subtype: A subtype of INFLUENZA A VIRUS comprised of the surface proteins hemagglutinin 3 and neuraminidase 2. The H3N2 subtype was responsible for the Hong Kong flu pandemic of 1968.Viral Matrix Proteins: Proteins associated with the inner surface of the lipid bilayer of the viral envelope. These proteins have been implicated in control of viral transcription and may possibly serve as the "glue" that binds the nucleocapsid to the appropriate membrane site during viral budding from the host cell.Drug Resistance, Viral: The ability of viruses to resist or to become tolerant to chemotherapeutic agents or antiviral agents. This resistance is acquired through gene mutation.Antiviral Agents: Agents used in the prophylaxis or therapy of VIRUS DISEASES. Some of the ways they may act include preventing viral replication by inhibiting viral DNA polymerase; binding to specific cell-surface receptors and inhibiting viral penetration or uncoating; inhibiting viral protein synthesis; or blocking late stages of virus assembly.Influenza, Human: An acute viral infection in humans involving the respiratory tract. It is marked by inflammation of the NASAL MUCOSA; the PHARYNX; and conjunctiva, and by headache and severe, often generalized, myalgia.Encyclopedias as Topic: Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)Crystallization: The formation of crystalline substances from solutions or melts. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)Volatilization: A phase transition from liquid state to gas state, which is affected by Raoult's law. It can be accomplished by fractional distillation.X-Ray Diffraction: The scattering of x-rays by matter, especially crystals, with accompanying variation in intensity due to interference effects. Analysis of the crystal structure of materials is performed by passing x-rays through them and registering the diffraction image of the rays (CRYSTALLOGRAPHY, X-RAY). (From McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)Nanotechnology: The development and use of techniques to study physical phenomena and construct structures in the nanoscale size range or smaller.Petroleum: Naturally occurring complex liquid hydrocarbons which, after distillation, yield combustible fuels, petrochemicals, and lubricants.Isomerism: The phenomenon whereby certain chemical compounds have structures that are different although the compounds possess the same elemental composition. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)Newspapers: Publications printed and distributed daily, weekly, or at some other regular and usually short interval, containing news, articles of opinion (as editorials and letters), features, advertising, and announcements of current interest. (Webster's 3d ed)Journalism, Medical: The collection, writing, and editing of current interest material on topics related to biomedicine for presentation through the mass media, including newspapers, magazines, radio, or television, usually for a public audience such as health care consumers.Research Report: Detailed account or statement or formal record of data resulting from empirical inquiry.Nanoparticles: Nanometer-sized particles that are nanoscale in three dimensions. They include nanocrystaline materials; NANOCAPSULES; METAL NANOPARTICLES; DENDRIMERS, and QUANTUM DOTS. The uses of nanoparticles include DRUG DELIVERY SYSTEMS and cancer targeting and imaging.Drug Carriers: Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers.VietnamAbstracting and Indexing as Topic: Activities performed to identify concepts and aspects of published information and research reports.Albumins: Water-soluble proteins found in egg whites, blood, lymph, and other tissues and fluids. They coagulate upon heating.Data Mining: Use of sophisticated analysis tools to sort through, organize, examine, and combine large sets of information.Serum Albumin: A major protein in the BLOOD. It is important in maintaining the colloidal osmotic pressure and transporting large organic molecules.Nanodiamonds: Diamond nanoparticles that exhibit unique biological, thermal, mechanical, and optoelectronic properties. They have important NANOMEDICINE applications including DRUG DELIVERY SYSTEMS; DIAGNOSTIC IMAGING; protein separation; and BIOSENSING TECHNIQUES.Diamond: Diamond. A crystalline form of carbon that occurs as hard, colorless or tinted isomeric crystals. It is used as a precious stone, for cutting glass, and as bearings for delicate mechanisms. (From Grant & Hackh's Chemical Dictionary, 5th ed)Chemistry, Physical: The study of CHEMICAL PHENOMENA and processes in terms of the underlying PHYSICAL PHENOMENA and processes.Physicochemical Phenomena: The physical phenomena describing the structure and properties of atoms and molecules, and their reaction and interaction processes.Physics: The study of those aspects of energy and matter in terms of elementary principles and laws. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)Spectrometry, Mass, Electrospray Ionization: A mass spectrometry technique used for analysis of nonvolatile compounds such as proteins and macromolecules. The technique involves preparing electrically charged droplets from analyte molecules dissolved in solvent. The electrically charged droplets enter a vacuum chamber where the solvent is evaporated. Evaporation of solvent reduces the droplet size, thereby increasing the coulombic repulsion within the droplet. As the charged droplets get smaller, the excess charge within them causes them to disintegrate and release analyte molecules. The volatilized analyte molecules are then analyzed by mass spectrometry.Influenza A virus: The type species of the genus INFLUENZAVIRUS A that causes influenza and other diseases in humans and animals. Antigenic variation occurs frequently between strains, allowing classification into subtypes and variants. Transmission is usually by aerosol (human and most non-aquatic hosts) or waterborne (ducks). Infected birds shed the virus in their saliva, nasal secretions, and feces.Influenza A Virus, H1N1 Subtype: A subtype of INFLUENZA A VIRUS with the surface proteins hemagglutinin 1 and neuraminidase 1. The H1N1 subtype was responsible for the Spanish flu pandemic of 1918.Influenza Vaccines: Vaccines used to prevent infection by viruses in the family ORTHOMYXOVIRIDAE. It includes both killed and attenuated vaccines. The composition of the vaccines is changed each year in response to antigenic shifts and changes in prevalence of influenza virus strains. The vaccine is usually bivalent or trivalent, containing one or two INFLUENZAVIRUS A strains and one INFLUENZAVIRUS B strain.Disease Outbreaks: Sudden increase in the incidence of a disease. The concept includes EPIDEMICS and PANDEMICS.Influenza in Birds: Infection of domestic and wild fowl and other BIRDS with INFLUENZA A VIRUS. Avian influenza usually does not sicken birds, but can be highly pathogenic and fatal in domestic POULTRY.Hydrogen Bonding: A low-energy attractive force between hydrogen and another element. It plays a major role in determining the properties of water, proteins, and other compounds.Cyclization: Changing an open-chain hydrocarbon to a closed ring. (McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)Computer Simulation: Computer-based representation of physical systems and phenomena such as chemical processes.Hydrogen: The first chemical element in the periodic table. It has the atomic symbol H, atomic number 1, and atomic weight [1.00784; 1.00811]. It exists, under normal conditions, as a colorless, odorless, tasteless, diatomic gas. Hydrogen ions are PROTONS. Besides the common H1 isotope, hydrogen exists as the stable isotope DEUTERIUM and the unstable, radioactive isotope TRITIUM.Models, Chemical: Theoretical representations that simulate the behavior or activity of chemical processes or phenomena; includes the use of mathematical equations, computers, and other electronic equipment.Nanowires: Nanometer-scale wires made of materials that conduct electricity. They can be coated with molecules such as antibodies that will bind to proteins and other substances.Silicon: A trace element that constitutes about 27.6% of the earth's crust in the form of SILICON DIOXIDE. It does not occur free in nature. Silicon has the atomic symbol Si, atomic number 14, and atomic weight [28.084; 28.086].Zinc Oxide: A mild astringent and topical protectant with some antiseptic action. It is also used in bandages, pastes, ointments, dental cements, and as a sunblock.Germanium: A rare metal element with a blue-gray appearance and atomic symbol Ge, atomic number 32, and atomic weight 72.63.Zinc Fingers: Motifs in DNA- and RNA-binding proteins whose amino acids are folded into a single structural unit around a zinc atom. In the classic zinc finger, one zinc atom is bound to two cysteines and two histidines. In between the cysteines and histidines are 12 residues which form a DNA binding fingertip. By variations in the composition of the sequences in the fingertip and the number and spacing of tandem repeats of the motif, zinc fingers can form a large number of different sequence specific binding sites.Solutions: The homogeneous mixtures formed by the mixing of a solid, liquid, or gaseous substance (solute) with a liquid (the solvent), from which the dissolved substances can be recovered by physical processes. (From Grant & Hackh's Chemical Dictionary, 5th ed)Animal Rights: The moral and ethical bases of the protection of animals from cruelty and abuse. The rights are extended to domestic animals, laboratory animals, and wild animals.Consumer Advocacy: The promotion and support of consumers' rights and interests.United StatesTetraodontiformes: A small order of primarily marine fish containing 340 species. Most have a rotund or box-like shape. TETRODOTOXIN is found in their liver and ovaries.Salamandridae: A family of Urodela consisting of 15 living genera and about 42 species and occurring in North America, Europe, Asia, and North Africa.Pseudoalteromonas: A genus of GRAM-NEGATIVE AEROBIC BACTERIA of marine origin. Many species were formerly classified under ALTEROMONAS.Moon: The natural satellite of the planet Earth. It includes the lunar cycles or phases, the lunar month, lunar landscapes, geography, and soil.Chemical Safety: Risk or hazard associated with the handling and use of chemicals.Fishes: A group of cold-blooded, aquatic vertebrates having gills, fins, a cartilaginous or bony endoskeleton, and elongated bodies covered with scales.Crotoxin: A specific complex of toxic proteins from the venom of Crotalus durissus terrificus (South American rattlesnake). It can be separated into a phospholipase A and crotapotin fragment; the latter consists of three different amino acid chains, potentiates the enzyme, and is specifically neurotoxic.

Identification of selective mechanism-based inactivators of cytochromes P-450 2B4 and 2B5, and determination of the molecular basis for differential susceptibility. (1/428)

Rabbit cytochromes P-450 (P-450) 2B4 and 2B5 differ by only 12 amino acid residues yet they exhibit unique steroid hydroxylation profiles. Previous studies have led to the identification of active site residues that are determinants of these specificities. In this study, mechanism-based inactivators were identified that discriminate between the closely related 2B4 and 2B5 enzymes. A previously characterized inhibitor, 2-ethynylnaphthalene (2EN), was found to be selective for 2B4 inactivation. As inhibitor metabolism and the partition ratio affect susceptibility, molecular dynamics simulations were performed to assess the stability of the productive binding orientation of 2EN within 2B4 and 2B5 three-dimensional models. Although 2EN was stable within the 2B4 model, it exhibited substantial movement away from the heme moiety in the 2B5 model. However, heterologously expressed 2B5 was found to catalyze the oxidation of 2EN to the stable product 2-naphthylacetic acid. Thus, the increased mobility of 2EN may result in reduced susceptibility of 2B5 by increasing the probability that the reactive ketene intermediate hydrolyzes with water instead of reacting with active site residues. Another compound, 1-adamantyl propargyl ether (1APE), selectively inactivated 2B5. The structural basis for 2EN and 1APE susceptibility was assessed using active site mutants. Interconversion of 2EN susceptibility was observed for 2B4 or 2B5 mutants containing a single alteration at residue 363. Single substitutions in 2B4 also conferred susceptibility to 1APE; however, multiple alterations were required to reduce the susceptibility of 2B5. These alterations may influence inhibitor susceptibility by affecting the stability of the productive binding orientation.  (+info)

Guest exchange in an encapsulation complex: a supramolecular substitution reaction. (2/428)

Encapsulation complexes are reversibly formed assemblies in which small molecule guests are completely surrounded by large molecule hosts. The assemblies are held together by weak intermolecular forces and are dynamic: they form and dissipate on time scales ranging from milliseconds to days-long enough for many interactions, even reactions, to take place within them. Little information is available on the exchange process, how guests get in and out of these complexes. Here we report that these events can be slow enough for conventional kinetic studies, and reactive intermediates can be detected. Guest exchange has much in common with familiar chemical substitution reactions, but differs in some respects: no covalent bonds are made or broken, the substrate is an assembly rather than a single molecule, and at least four molecules are involved in multiple rate-determining steps.  (+info)

Eukaliuric diuresis and natriuresis in response to the KATP channel blocker U37883A: micropuncture studies on the tubular site of action. (3/428)

1. Systemic application of U37883A, a blocker of ATP sensitive potassium (KATP) channels, elicits diuresis and natriuresis without significantly altering urinary potassium excretion. 2. To elucidate tubular sites of action upstream to the distal nephron, micropuncture experiments were performed in nephrons with superficial glomeruli of anaesthetized Munich-Wistar-Fromter rats during systemic application of U37883A (1, 5 or 15 mg kg-1 i.v.). 3. The observed eukaliuric diuresis and natriuresis in response to U37883A at 15 mg kg-1 was accompanied by an increase in early distal tubular flow rate (VED) from 10 - 18 nl min(-1) reflecting a reduction in fractional reabsorption of fluid up to this site (FR-fluid) of 13%. The latter proposed an effect on water-permeable segments such as the proximal tubule which could fully account for the observed reduction in fractional reabsorption of Na+ up to the early distal tubule (FR-Na+) of 8% and the increase in early distal tubular Na+ concentration ([Na+]ED) from 35 - 51 mM whereas [K+]ED was left unaltered. 4. In comparison, furosemide (3 mg kg-1 i.v.), which acts in the water-impermeable thick ascending limb, elicited diuresis, natriuresis and kaliuresis which were associated with a fall in FR-Na+ of 10% with no change in FR-fluid, and a rise in [Na+]ED from 42 - 117 mM and [K+]ED from 1.2 - 5.7 mM with no change in VED. 5. Direct late proximal tubular fluid collections confirmed a significant inhibition of fluid reabsorption in proximal convoluted tubule in response to systemic application of U37883A. 6. These findings suggest that the diuretic and natriuretic effect upstream to the distal tubule in response to systemic application of U37883A involves actions on water-permeable segments such as the proximal convoluted tubule.  (+info)

Analysis of vasoconstrictor responses to histamine in the hindlimb vascular bed of the rabbit. (4/428)

Hemodynamic responses to histamine were investigated in the anesthetized rabbit. Intravenous injections of histamine induced dose-dependent decreases in systemic arterial pressure that were blocked by the H(1)-receptor antagonist pyrilamine but not the H(2) antagonist cimetidine. Injections of histamine and the H(1) agonist 6-[2-(4-imidazolyl)ethylamine]-N-(4-trifuormethylphenyl)-heptan ecardo xamide dimaleate (HTMT) into the hindlimb perfusion circuit increased hindlimb perfusion pressure, whereas the H(2) agonist dimaprit decreased perfusion pressure and the H(3)-receptor agonist R-(-)-alpha-methylhistamine did not alter perfusion pressure. Pyrilamine reduced hindlimb vasoconstrictor responses to histamine and HTMT but did not alter vasodilator responses to dimaprit. Cimetidine reduced the response to dimaprit but did not alter vasoconstrictor responses to histamine or HTMT. The H(3)-receptor antagonist thioperamide was without effect on responses to the histamine agonists. These data suggest the presence of H(1) and H(2) receptors and that histamine for the most part acts by stimulating H(1) receptors to produce vasoconstriction in the hindlimb vascular bed of the rabbit. Responses to histamine, HTMT, and norepinephrine were significantly enhanced by a nitric oxide synthase inhibitor at a time when vasodilator responses to dimaprit were unaltered and responses to acetylcholine were significantly reduced. Responses to histamine and the H(1) and H(2) agonists were not affected by the cyclooxygenase inhibitor meclofenamate or by ATP-sensitive K(+) channel, alpha-adrenergic, or angiotensin AT(1) receptor antagonists. The present data suggest that H(1) receptors mediate both systemic vasodepressor and hindlimb vasoconstrictor responses to histamine.  (+info)

Block of human aorta Kir6.1 by the vascular KATP channel inhibitor U37883A. (5/428)

1. A human aorta cDNA library was screened at low stringency with a rat pancreatic Kir6.1 cDNA probe and a homologue of Kir6.1 (hKir6.1) was isolated and sequenced. 2. Metabolic poisoning of Xenopus laevis oocytes with sodium azide and application of the K+ channel opener drug diazoxide induced K+ channel currents in oocytes co-injected with cRNA for hKir6.1 and hamster sulphonylurea receptor (SUR1), but not in oocytes injected with water or cRNA for hKir6.1 or SUR1 alone. 3. K+ channel currents due to hKir6.1+SUR1 or mouse Kir6.2+SUR1 were strongly inhibited by 1 microM glibenclamide. K+-current carried by hKir6.1+SUR1 was inhibited by the putative vascular-selective KATP channel inhibitor U37883A (IC50 32 microM) whereas current carried by Kir6.2+SUR1 or Shaker K+ channels was unaffected. 4. The data support the hypothesis that hKir6.1 is a component of the vascular KATP channel, although the lower sensitivity of hKir6.1+SUR1 to U37883A compared with native vascular tissues suggests the need for another factor or subunit. Furthermore, the data suggest that pharmacology of KATP channels can be determined by the pore-forming subunit as well as the sulphonylurea receptor and point to a molecular basis for the pharmacological distinction between vascular and pancreatic/cardiac KATP channels.  (+info)

Inhibition of vascular K(ATP) channels by U-37883A: a comparison with cardiac and skeletal muscle. (6/428)

1 The aim of this study was to investigate the selectivity of the ATP-sensitive potassium (K(ATP)) channel inhibitor U-37883A (4-morpholinecarboximidine-N-1-adamantyl-N'-1-cyclohexyl). Membrane currents through K(ATP) channels were recorded in single muscle cells enzymatically isolated from rat mesenteric artery, cardiac ventricle and skeletal muscle (flexor digitorum brevis). K(ATP) currents were induced either by cell dialysis with 0.1 mM ATP and 0.1 mM ADP, or by application of synthetic potassium channel openers (levcromakalim or pinacidil). 2 U-37883A inhibited K(ATP) currents in smooth muscle cells from rat mesenteric artery. Half inhibition of 10 microM levcromakalim-induced currents occurred at a concentration of 3.5 microM. 3 Relaxations of rat mesenteric vessels caused by levcromakalim were reversed by U-37883A. 1 microM levcromakalim-induced relaxations were inhibited at a similar concentration of U-37883A (half inhibition, 1.1 microM) to levcromakalim-induced KATP currents. 4 K(ATP) currents activated by 100 microM pinacidil were also studied in single myocytes from rat mesenteric artery, skeletal muscle and cardiac ventricle. 10 microM U-37883A substantially inhibited K(ATP) currents in vascular cells, but had little effect in skeletal or cardiac myocytes. Higher concentrations of U-37883A (100 microM) caused a modest decrease in K(ATP) currents in skeletal and cardiac muscle. The sulphonylurea K(ATP) channel antagonist glibenclamide (10 microM) abolished currents in all muscle types. 5 The effect of U-37883A on vascular inward rectifier (KIR) and voltage-dependent potassium (KV) currents was also examined. While 10 microM U-37883A had little effect on these currents, some inhibition was apparent at higher concentrations (100 microM) of the compound. 6 We conclude that U-37883A inhibits K(ATP) channels in arterial smooth muscle more effectively than in cardiac and skeletal muscle. Furthermore, this compound is selective for K(ATP) channels over KV and KIR channels in smooth muscle cells.  (+info)

Early increases in renal kallikrein secretion on administration of potassium or ATP-sensitive potassium channel blockers in rats. (7/428)

1 This study aimed to examine whether administration of potassium or ATP-sensitive potassium channel (KATP channel) blockers caused early increases in renal kallikrein (KK) secretion. To clarify this mechanism, the effect on renal KK secretion of a KATP channel blocker was compared with the effect resulting from use of an osmotic diuretic or volume load. Furthermore, the effect on potassium-induced increases in renal KK secretion by an additional treatment using a KATP channel blocker was examined. Lastly, the effect of a KATP channel blocker on renal KK secretion was also examined in superfused slices of kidney cortex. 2 Intravenous infusion of potassium augmented renal KK secretion within 30 min while urine volume increased gradually in both the potassium loading and control groups. 3 Administration of the KATP channel blocker, 4-morpholinecarboximidine-N-1-adamantyl-N'-cyclohexylhydr ochloride (PNU-37883A) or glibenclamide, caused a dose-dependent increase in renal KK secretion. 4 The concentration of KK in urine was higher in the PNU-37883A group as compared to the osmotic-diuretic or volume-load group. 5 PNU-37883A had no additive effect on the potassium-induced increase in renal KK secretion. 6 Renal KK secretion increased in slices of kidney cortex incubated with PNU-37883A within 10 min of superfusion. 7 In conclusion, administration of both potassium and KATP channel blockers induced early increases in renal KK secretion in the absence of the washout phenomenon. Potassium loading may have increased renal KK secretion through the same mechanism as the KATP channel blocker.  (+info)

Effects of the bcr/abl kinase inhibitors AG957 and NSC 680410 on chronic myelogenous leukemia cells in vitro. (8/428)

The tyrphostin AG957 (NSC 654705) inhibits p210bcr/abl, the transforming kinase responsible for most cases of chronic myelogenous leukemia (CML). The present studies were performed to determine the fate of AG957-treated cells and assess the selectivity of AG957 for CML myeloid progenitors. When K562 cells (derived from a patient with blast crisis CML) were treated with AG957, dose- and time-dependent p210bc/abl down-regulation was followed by mitochondrial release of cytochrome c, activation of caspase-9 and caspase-3, and apoptotic morphological changes. These apoptotic changes were inhibited by transfection with cDNA encoding dominant negative caspase-9 but not dominant-negative FADD or blocking anti-Fas antibodies. In additional experiments, a 24-h AG957 exposure caused dose-dependent inhibition of K562 colony formation in soft agar. To extend these studies to clinical samples of CML, peripheral blood mononuclear cells from 10 chronic phase CML patients and normal controls were assayed for the growth of hematopoietic colonies in vitro in the presence of increasing concentrations of AG957. These assays demonstrated selectivity of AG957 for CML progenitors, with median IC50s (CML versus normal) of 7.3 versus >20 microM AG957 in granulocyte colony-forming cells (P < 0.001), 5.3 versus >20 microM in granulocyte/macrophage colony-forming cells (P < 0.05), and 15.5 versus > 20 microM in erythroid colony-forming cells (P > 0.05). The adamantyl ester of AG957 (NSC 680410) down-regulated p210bcr/abl in K562 cells and inhibited granulocyte colony formation in CML specimens at lower concentrations without enhanced toxicity in normal progenitors. These observations not only demonstrate that AG957-induced p210bcr/abl down-regulation is followed by activation of the cytochrome c/Apaf-1/caspase-9 pathway but also indicate that this class of kinase inhibitor exhibits selectivity worthy of further evaluation.  (+info)

All the above methods yield adamantane as a polycrystalline powder. Using this powder, single crystals can be grown from the melt, solution, or vapor phase (e.g. with the Bridgman-Stockbarger technique). Melt growth results in the worst crystalline quality with a mosaic spread in the X-ray reflection of about 1°. The best crystals are obtained from the liquid phase, but the growth is impracticably slow - several months for a 5-10 mm crystal. Growth from the vapor phase is a reasonable compromise in terms of speed and quality.[2] Adamantane is sublimed in a quartz tube placed in a furnace, which is equipped with several heaters maintaining a certain temperature gradient (about 10 °C/cm for adamantane) along the tube. Crystallization starts at one end of the tube, which is kept near the freezing point of adamantane. Slow cooling of the tube, while maintaining the temperature gradient, gradually shifts the melting zone (rate ~2 mm/hour) producing a single-crystal boule.[16]. ...
Background: The H9N2 subtype of influenza A viruses is considered to be widespread in poultry industry. Adamantane is a group of antiviral agents which is effective both in prevention and treatment of influenza A virus infections. These drugs inhibit M2 protein ion channel which has role on viral replication. OBJECTIVES: The main objective of this study is to evaluate M gene of avian influenza viruses (AIVs) of H9N2 subtype in order to find adamantane drug resistance mutations. METHODS: Over 100 suspected samples were collected from different geographical regions of Iran during 2012-2013. Samples were injected via allantoic sac of 9-11 day-old chicken embryos. A total of 11 out of 100 were AIV. The H9N2 subtype was confirmed by specific RT-PCR. The RT-PCR was conducted for full length M gene. PCR amplified products were purified and then conducted for commercial direct sequencing. Finally, sequences were checked for possible sites of adamantane resistance mutations. RESULTS: Overall, 8 out of 11 viruses
TY - JOUR. T1 - Specific binding of adamantane drugs and direction of their polar amines in the pore of the influenza M2 transmembrane domain in lipid bilayers and dodecylphosphocholine micelles determined by NMR spectroscopy. AU - Cady, Sarah D.. AU - Wang, Jun. AU - Wu, Yibing. AU - Degrado, William F.. AU - Hong, Mei. PY - 2011/3/30. Y1 - 2011/3/30. N2 - The transmembrane domain of the influenza M2 protein (M2TM) forms a tetrameric proton channel important for the virus lifecycle. The proton-channel activity is inhibited by amine-containing adamantyl drugs amantadine and rimantadine, which have been shown to bind specifically to the pore of M2TM near Ser31. However, whether the polar amine points to the N- or C-terminus of the channel has not yet been determined. Elucidating the polar group direction will shed light on the mechanism by which drug binding inhibits this proton channel and will facilitate rational design of new inhibitors. In this study, we determine the polar amine direction ...
In chemistry, diamondoids are variants of the carbon cage molecule known as adamantane (C10H16), the smallest unit cage structure of the diamond crystal lattice. Diamondoids also known as nanodiamonds or condensed adamantanes may include one or more cages (adamantane, diamantane, triamantane, and higher polymantanes) as well as numerous isomeric and structural variants of adamantanes and polymantanes. These diamondoids occur naturally in petroleum deposits and have been extracted and purified into large pure crystals of polymantane molecules having more than a dozen adamantane cages per molecule. These species are of interest as molecular approximations of the diamond cubic framework, terminated with C−H bonds. Cyclohexamantane may be thought of as a nanometer-sized diamond of approximately 6978560000000000000♠5.6×10−22 grams. Examples include: Adamantane (C10H16) Iceane (C12H18) BC-8 (C14H20) Diamantane (C14H20) also diadamantane, two face-fused cages Triamantane (C18H24), also ...
I first became interested in adamantane when I read about it in one of rays articles. According to Ray it seems to have a stabilizing and structurally...
394:764-766 20Aug98] describe encapsulation of guest molecules by specially synthesized container molecules. In the Science paper the capsule consists of four copies of a molecule with five fused rings, while in the Nature paper it consists of two copies of a molecule with seventeen fused rings. In both cases the rings lie on the surfaces of the capsules, and the monomers are joined to each other by hydrogen bonds from the edge of one ring to the edge of another.. In the Science paper, the guest molecules were adamantane and a number of hydroxyl and keto derivatives of adamantane. Equilibrium constants for the formation of the complexes were measured, showing that hydrogen bonds between the oxygenated guests and the capsule stabilized these complexes by 0.6-3.0 kcal/mol. Kinetically, the complexes were sufficiently stable that "The exchange of guests in and out of the capsule is slow on the NMR time scale." In the case of unmodified adamantane, the NMR signal shows a single sharp peak, ...
More data confirm DPP-4 inhibitor vildagliptin (Galvus) offers special advantages for elderly Type 2 diabetes patients : Pharmaceutical feature | PharmiWeb.com
(2-methyl-2-adamantyl) prop-2-enoate 249562-06-9 NMR spectrum, (2-methyl-2-adamantyl) prop-2-enoate H-NMR spectral analysis, (2-methyl-2-adamantyl) prop-2-enoate C-NMR spectral analysis ect.
1-adamantyl 2-(trifluoromethyl)prop-2-enoate 188739-82-4 NMR spectrum, 1-adamantyl 2-(trifluoromethyl)prop-2-enoate H-NMR spectral analysis, 1-adamantyl 2-(trifluoromethyl)prop-2-enoate C-NMR spectral analysis ect.
TY - JOUR. T1 - Cost-effectiveness of vildagliptin for people with type 2 diabetes mellitus in Brazil. T2 - findings and implications. AU - de Oliveira, Gustavo Laine Araujo. AU - Guerra Júnior, Augusto Afonso. AU - Godman, Brian. AU - de Assis Acúrcio, Francisco. PY - 2017/2/22. Y1 - 2017/2/22. N2 - Introduction: Vildagliptin is an inhibitor of the enzyme dipeptidyl peptidase 4, indicated for the treatment of type 2 diabetes mellitus, combined or not with metformin. This study aims to evaluate the cost-effectiveness of vildagliptin in the Brazilian context. Areas covered: Using MEDLINE, Cochrane Library, Lilacs and CRD, six studies were selected for the economic models. This study utilised cost data in the Brazilian health system to provide the context.Expert commentary: Type 2 diabetes mellitus is an epidemic disease and represents a challenge for all health care systems. Although guidelines clearly define first-line treatment, there are several other promising treatments. Vildagliptin is ...
Metformin + vildagliptin is used in the treatment of type 2 diabetes.get complete information about metformin + vildagliptin including usage, side effects, drug interaction, expert advice along with medicines associated with metformin + vildagliptin at 1mg.com
Seventy-two patients were enrolled (vildagliptin, n = 30; SU, n = 41; no treatment, n = 1), of whom 23 (76.7%) and 36 (87.8%), respectively, completed the study. With vildagliptin, there were no HEs or severe HEs, compared with 34 HEs (15 patients, 41.7%) and one severe (grade 2) HE with SU. The mean between-group difference in the proportion who experienced at least one HE was -41.7% (95%CI -57.8%, -25.6%), p = 0.0002. Vildagliptin lowered mean HbA(1c) from 7.6% (SD 0.9%) at baseline to 7.2% (SD 0.7%) post-Ramadan, whereas SU had no effect (7.2% [SD 0.6%] vs 7.3% [SD 0.7%]; mean between-group difference -0.5% [95% CI -0.9%, -0.1%], p = 0.0262). The mean number of missed doses was markedly lower with vildagliptin (0.2 [SD 0.8] vs 7.6 [SD 14.9]; mean between-group difference -7.4 [95% CI -13.7, -1.20] doses; p = 0.0204). Body weight remained unchanged in both groups.. ...
The general molecular formula of homologous diamondoid is C4n+6H4n+12. Diamondoids have one or more cages and are called diamantane, triamantane, and polymantanes. There are numerous structural isomers as well. Aadamantane itself is the simplest diamondoid. Some examples are; iceane (C12H18), diadamantane (C14H20), triadamantane (C18H24), isotetramantane (C22H28), cyclohexamantane (C26H30), superadamantane (C35H36). Natural diamondoids are extracted and purified from petroleum deposits. Diamondoids are being investigated in the new field of nanotechnoloy ...
On the left is adamantane with four hydrogen atoms abstracted. Previous simulations gave reason to suspect it would fail in mechanosynthesis due to internal cyclization. However I have misplaced those results. In order to overcome this problem a larger building block was chosen, penta-adamantane, rendered on the right also with four hydrogen atoms abstracted. I chose this because it has a similar shape as adamantane, and my collaborators decided we could run with it ...
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Tolerability and efficacy of glycemic control with saxagliptin in older patients (aged ≥ 65 years) with inadequately controlled type 2 diabetes mellitus Chetan S Karyekar, Shoba Ravichandran, Elsie Allen, Douglas Fleming, Robert Frederich Bristol-Myers Squibb, Princeton, NJ, USA Purpose: To assess safety and efficacy of saxagliptin in older patients with type 2 diabetes mellitus (T2DM). Patients and methods: This was a post hoc analysis of pooled data from older patients (≥65 years of age) from five 24-week phase III trials: three studies of saxagliptin versus placebo as an add-on therapy to metformin, glyburide, or a thiazolidinedione; and two studies of saxagliptin versus placebo as monotherapy in drug-naïve patients. Separate analyses were conducted on one study of initial combination therapy with saxagliptin plus metformin versus metformin monotherapy in drug-naïve patients. The safety analysis population for the five-study pool included 428 patients ≥ 65 years of age with
Serial blood samples for determination of study drug were collected predose (0 h), 6 h, 12 h, 18 h, 24 h, 30 h, 36 h, 42 h, 48 h, 54 h and 60 h postdose, relative to dosing on Day 1 in each cross over period. Saxagliptin is the parent drug and 5-OH saxagliptin is the metabolite. The molecular weights to be used for the molar ratios were 315.42 and 331.42 for saxagliptin and 5-OH, respectively. Plasma samples were analyzed for saxagliptin and for 5-OH by LC-MS/MS using a validated method (quantitation range of 0.100 ng/mL to 50.0 ng/mL and 0.200 ng/mL to 100.0 ng/mL for saxagliptin and 5-OH, respectively ...
Saxagliptin, sold under the brand name Onglyza, is an oral hypoglycemic (anti-diabetic drug) of the dipeptidyl peptidase-4 (DPP-4) inhibitor class. Early development was solely by Bristol-Myers Squibb; in 2007 AstraZeneca joined with Bristol-Myers Squibb to co-develop the final compound and collaborate on the marketing of the drug. In April 2016, the U.S. FDA added a warning about increased risk of heart failure. This was based on data in an article that concluded "DPP-4 inhibition with saxagliptin did not increase or decrease the rate of ischemic events, though the rate of hospitalization for heart failure was increased. Although saxagliptin improves glycemic control, other approaches are necessary to reduce cardiovascular risk in patients with diabetes." Saxagliptin is used as monotherapy or in combination with other drugs for the treatment of type 2 diabetes. It does not appear to decrease the risk of heart attacks or strokes. It increases the risk of hospitalization for heart failure by ...
Diabetes, Obesity and Metabolism has published the results of a long term study comparing vildagliptin to glimepiride.. The study recruited 2,789 patients who were inadequately controlled on metformin monotherapy. Participants were then randomised to vildagliptin 50mg twice daily or glimepiride titrated up to 6mg daily. These results are a prespecified interim analysis after 52 weeks to ensure that vildagliptin is non-inferior to glimepiride.. Baseline HbA1c was 7.3% in both groups. This fell by 0.44% in the vildagliptin arm and 0.53% in the glimepiride arm. The difference was not significant and therefore non-inferiority was proven.. Other notable differences reported include a lower incidence of hypoglycaemia in the patients receiving vildagliptin and beneficial effects on body weight. Patients treated with vildagliptin lost approximated 0.23kg compared to a weight gain of 1.56kg in the glimepiride cohort. Additionally, no major differences were noted in haematological or biochemical ...
Metformin + Vildagliptin in Malaysia: Metformin and Vildagliptin are combined in this medicine. This medicine is used on its own or together with other medicines to treat type 2 diabetes (gradual
23479-47-2 - JAPQLDFOGYVHMQ-UHFFFAOYSA-N - Ketone, 1-adamantyl piperidinomethyl, hydrochloride - Similar structures search, synonyms, formulas, resource links, and other chemical information.
4-(1-Adamantyl)phenyl acetate | C18H22O2 | CID 269932 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
This page contains information on the chemical Ethanethiol, 2-(1-adamantyl)amino-, hydrogen phosphate (ester), hydrate including: 3 synonyms/identifiers.
1-Adamantanecarboxylic acid, 2-adamantyl ester | C21H30O2 | CID 585141 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Sigma-1 receptors (S1Rs) are overexpressed in almost all human cancers, especially in breast cancers. 1-(4-Iodophenyl)-3-(2-adamantyl)guanidine (IPAG) is a
Blood pressure and fasting lipid changes after 24 weeks treatment with vildagliptin: a pooled analysis in |2,000 previously drug-naïve patients with type 2 diabetes mellitus Marc Evans,1 Anja Schweizer,2 James E Foley3 1Diabetes Resource Centre, Llandough Hospital, Cardiff, UK; 2Medical Affairs Cardio Metabolic, Novartis Pharma AG, Basel, Switzerland; 3Medical Affairs Cardio-Metabolic, Novartis Pharmaceuticals Corporation, East Hanover, NJ, USA Introduction: We have previously shown modest weight loss with vildagliptin treatment. Since body weight balance is associated with changes in blood pressure (BP) and fasting lipids, we have assessed these parameters following vildagliptin treatment. Methods: Data were pooled from all double-blind, randomized, controlled, vildagliptin monotherapy trials on previously drug-naïve patients with type 2 diabetes mellitus who received vildagliptin 50 mg once daily (qd) or twice daily (bid; n=2,108) and wherein BP and fasting lipid data were obtained. Results: Data
Last year, I wrote about a scientific controversy over the structure of the influenza M2 proton channel, particularly over the proteins binding site for adamantane type anti-flu drugs. The Schnell/Chou model, based on solution NMR, had the drug binding to the outside of the channel, within the membrane (at a 4:1 drug:protein ratio). On the…. ...
The crystal energy landscapes of two model pharmaceutically active chloride salts were used to rationalize the different hydration behaviour of the salts on the basis of the packing of the ions and calculated solvent-accessible volumes in the low-energy structures. The crystal structure of 1-(methylamino)adamantane was characterized and correctly predicted under blind test conditions as the second ranked structure in lattice energy, but the failure to predict the Z′ = 3 structure for the corresponding hydrochloride salt of this relatively simple base illustrates the limits of blind crystal structure prediction ...
In the framework of real structures, i.e. finite sized systems, the transition from a molecule (hydrocarbon) to a true allotrope is ill-defined. For hexagonal systems, it is universally accepted that benzene is a molecule and not a carbon allotrope. This also holds for coronene and higher oligoacenes and, in principle, as long as the fraction of heteroatoms (mainly hydrogen) does not reach zero. However, what we consider to be graphene and even graphite or other allotropes of carbon, still contain finite fractions of heteroatoms (e.g. nitrogen impurities in diamond).. The same scenario holds for systems with tetrahedrally coordinated carbon. When the size of a diamond crystal is so small that the fraction of hydrogen atoms saturating the dangling bonds of the surface carbon atoms cannot be neglected, we are prone to consider it as a molecule: a diamondoid. The smallest diamondoid is adamantane, formed by a carbon cage of ten carbon atoms (C10H16). Higher diamondoids have multiples of four ...
15b, as 92 of the cubane and adamantane com- pounds are mapped into common neurons. 3363 7. The flow phantom was pumped by the syringe pump at a constant sshowcomments for all of the setups.2000) or statr, whether MHC-I molecules play an active role by first binding precursor peptides and then recruiting a trimming aminopeptidase that is released when the appropriate length for binding is reached.
Efficacy and Safety of Vildagliptin as an Add-On Therapy in Inadequately Controlled Type 2 Diabetes Patients Treated With Basal Insulin
Objective: DPP4 inhibitors (DPP-4i) lower blood glucose in diabetic subjects however the mechanism of action through which these agents improve glucose homeostasis remains incompletely understood. Although GLP-1 and GIP represent important targets for DPP4 activity, whether additional substrates are important for the glucose-lowering actions of DPP4 inhibitors remains uncertain.. Research Design and Methods: We examined the efficacy of continuous vildagliptin administration in wildtype (WT) and dual incretin receptor knockout (DIRKO) mice after 8 weeks of a high fat (HF)-diet.. Results: Vildagliptin had no significant effect on food intake, energy expenditure, body composition, body weight gain or insulin sensitivity in WT or DIRKO mice. However glycemic excursion after oral glucose challenge was significantly reduced in WT but not in DIRKO mice after vildagliptin treatment. Moreover, vildagliptin increased levels of glucose-stimulated plasma insulin, and reduced levels of cholesterol and ...
5143 Here we describe a novel pharmacologically-induced death pathway in tumor cells involving c-Jun upregulation and caspase-dependent c-Abl cleavage using the tyrophostin adaphostin (NSC680410) as a tool compound.. Adaphostin has been previously studied as a bcr-abl inhibitor in CML. However its role in MM is unknown. After demonstrating its anti-myeloma cytotoxicity, expression profiling of adaphostin-treated MM cells was carried out to identify its molecular targets. Surprisingly, c-Jun was the most upregulated gene even at the earliest point of analysis (2 hours). Subsequently, adaphostin-induced c-Abl cleavage was observed in immunoblot analysis. Proteasome inhibitor bortezomib, but not melphalan or dexamethasone, induced similar effects, indicating unique agent-dependent mechanisms. Using caspase inhibitors as well as caspase-resistant mutants of c-Abl (TM-c-Abl and D565A-Abl), we then showed that c-Abl cleavage in MM cells requires caspase activity. Importantly, both overexpression of ...
This trial is investigating the efficacy and tolerability of vildagliptin + insulin in haemodialysis patients with type-2 diabetes mellitus that is inadequately
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Vildagliptin is an oral anti-diabetic agent. This 52-week clinical study is designed as an open label, long-term study aimed to evaluate the safety of
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The presented analyses of the SAVOR-TIMI 53 study were unsuitable for conclusions on positive or negative effects in comparison with the appropriate comparator therapies.
Saxagliptin (Onglyza), a drug prescribed for type 2 diabetes, can interact with some medications, including: antifungal medicationsmedications to trea
Saxagliptin or Onglyza is a new oral blood glucose lowering agent used in the treament of Type 2 diabetes; it was recently launched in the UK
Medscape - Type 2 diabetes mellitus dosing for Qtern (dapagliflozin/saxagliptin) dosing, frequency-based adverse effects, comprehensive interactions, contraindications, pregnancy & lactation schedules, and cost information.
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the contacts provided below. For general information, Learn About Clinical Studies. ...
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流行前にインフルエンザ治療を復習このまま流行せず春が来て欲しいです。以下UpToDate よりTarget groups for therapy●Given the concerning trends of increasing resistance with both the adamantanes and the …
A label change for AstraZenecas DPP-4 inhibitor Onglyza (saxagliptin) could be on the horizon after the US Food and Drug Administration cited concerns that it could be linked with a higher risk of death. - News - PharmaTimes
Onglyza (saxagliptin) is a type 2 diabetes medication that was approved by the FDA in 2009. It belongs to a class of drugs known as
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice. ...
Diamond nanoparticles, or nanodiamonds, are intriguing carbon-based materials which, maybe surprisingly, are the most abundant constituent of presolar grains. While the spectroscopic properties of even quite large diamondoids have already been explored, little is known about their unimolecular fragmentation process 2017 PCCP HOT Articles Theory, experiment, and simulations in laboratory astrochemistry
Press Release issued Dec 6, 2016: Diabetes is the chronic condition associated with abnormally high level of glucose in the blood. Insufficient or non production of insulin in pancreas causes diabetes. Globally, the incidence of diabetes is increasing significantly and it is becoming a major burden. According to World Health Organization (WHO), approximately 221 million people are suffering from diabetes. There are large numbers of blood glucose lowering drugs. Saxagliptin is an oral anti-diabetic agent known as DPP IV inhibitor. DDP IV inhibitor is an enzyme helps in suppressing the release of glucagon. Saxagliptin is used for medication of diabetes, as to boost the amount of insulin in the body produced after meal. Saxagliptin is marketed under the brand name Onglyza. Saxagliptin acts on natural hormone in the body known as incretins. Saxagliptin has various side effects such as headache, urinary tract infection, upper respiratory tract infection and nasopharyngitis. Saxagliptin can also cause
2016 Society for Endocrinology. Obesity and testosterone deprivation are associated with coronary artery disease. Testosterone and vildagliptin (dipeptidyl peptidase-4 inhibitors) exert cardioprotection during ischemic-reperfusion (I/R) injury. However, the effect of these drugs on I/R heart in a testosterone-deprived, obese, insulin-resistant model is unclear. This study investigated the effects of testosterone and vildagliptin on cardiac function, arrhythmias and the infarct size in I/R heart of testosterone-deprived rats with obese insulin resistance. Orchiectomized (O) or sham operated (S) male Wistar rats were divided into 2 groups to receive normal diet (ND) or high-fat diet (HFD) for 12 weeks. Orchiectomized rats in each diet were divided to receive testosterone (2 mg/kg), vildagliptin (3 mg/kg) or the vehicle daily for 4 weeks. Then, I/R was performed by a 30-min left anterior descending coronary artery ligation, followed by a 120-min reperfusion. LV function, arrhythmia scores, infarct ...
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice. ...
Literature References: Deriv of adamantane, q.v. Prepn: NL 6408505; W. W. Prichard, US 3352912 (1965, 1967 both to du Pont). Antiviral activity: A. Tsunoda et al., Antimicrob. Agents Chemother. 1965, 553. Effects on influenza in mice: J. W. McGahen et al., Ann. N.Y. Acad. Sci. 173, 557 (1970). Mechanism of action study: A. Bukrinskaya et al., Arch. Virol. 66, 275 (1980); eidem, J. Gen. Virol. 60, 49 (1982). Pharmacokinetics in humans: R. J. Wills et al., Antimicrob. Agents Chemother. 31, 826 (1987). Clinical trial in prophylaxis of influenza A infection: R. Dolin et al., N. Engl. J. Med. 307, 580 (1982). Comparative toxicity of rimantadine and amantadine in healthy adults: F. G. Hayden et al., Antimicrob. Agents Chemother. 19, 226 (1981). Controlled study of CNS effects: V. M. Millet et al., ibid. 21, 1 (1982). Review of studies in the USSR on exptl and clinical pharmacology: D. M. Zlydnikov et al., Rev. Infect. Dis. 3, 408-421 (1981). ...
Jalali, P and Hyde, C B and Gilroy, D W and Bishop-Bailey, D (2019) THE SOLUBLE EPOXIDE HYDROLASE INHIBITOR GSK2256294 DECREASES LPS- INDUCED CYTOKINE MRNA EXPRESSION IN HUMAN PERIPHERAL BLOOD MONONUCLEAR CELLS. Cardiovascular Drugs and Therapy, 33 (2). pp. 267-268. Full text not available from this repository ...
Page contains details about zinc(II) adamantane-1-thiolate nanowires . It has composition images, properties, Characterization methods, synthesis, applications and reference articles : nano.nature.com
The efficacy and safety of the dipeptidyl peptidase-4 inhibitor saxagliptin in treatment-naïve patients with type 2 diabetes mellitus: a randomized controlled trial. - Robert Frederich, Robert McNeill, Niklas Berglind, Douglas Fleming, Roland Chen
Disclosed are sulfone compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetes-related diseases.
The collision induced decompositions of 3-substituted adamantane carboxylate anions have been studied with a view to uncovering charge-remote fragmentations of the 3-substituent. The 3-substituent is chosen so that it cannot approach the anion site, and so any fragmentations of that substituent should proceed independently of the charged centre, viz. charge-remote reactions. The following systems have been studied (i) the 3-cyclohexenyl system shows no charge-remote retro Diels-Alder fragmentation (DeltaH = +157 kJ mol(-1)), instead, charge-remote loss of the cyclohexenyl radical is noted, (ii) the 3-isobutyl ketone system shows no Norrish II cleavage (loss of C(3)H(6), DeltaH = +18 kJ mol(-1)), instead, the competitive losses of CO(2) from the charged carboxyl centre, together with charge-remote radical loss of the 3-substituent are observed, and (iii) the corresponding 3-isopropyl ester does show the Norrish II loss of C(3)H(6), together with competitive losses of CO(2) and the ...
Generic for Galvus 50mg Tablet (Vildagliptin) is indicated in the treatment of type 2 diabetes. It belongs to a group of drugs known as dipeptidyl peptidase-4 (DPP-4) inhibitors.
Wear a self-contained breathing apparatus in pressure-demand, MSHA/NIOSH (approved or equivalent), and full protective gear. During a fire, irritating and highly toxic gases may be generated by thermal decomposition or combustion. Extinguishing media: Use agent most appropriate to extinguish fire. In case of fire use water spray, dry chemical, carbon dioxide, or appropriate foam ...
This eMedTV Web page provides a detailed list of common and serious side effects of saxagliptin/metformin ER. It also includes the percentages of people who experienced these reactions in clinical studies on the individual components.
ONGLYZA® (saxagliptin) achieves primary safety endpoint, demonstrating no increased risk for cardiovascular death, heart attack or stroke in SAVOR cardiovascular outcomes trial
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Its important to remember that individual cells do not last as long as people live. Cells naturally die and new cells grow within your body all the time. Research (mostly in animals) has suggested that Vildagliptin might have two separate effects on beta cells. On the one hand, it seems to cause beta cells to naturally divide and grow, and on the other hand, it seems to delay beta cells "natural death", so they live longer. Both of these effects may be important to curing type-1 diabetes, but it is not clear. This is why research is important. For example, even if Vildagliptin triggers a divide-and-grow reaction, it will only be effective if there are some beta cells to start with, and we just dont know if there are enough to get things started. On the cell death side, if the autoimmune attack directly kills beta cells, then stopping natural cell death may have little impact. Those cells will be killed by autoimmunity before they can die of "old age". However, if the autoimmune attack works ...
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TUPS | sEH inhibitor | CAS [950184-27-7] | Axon 3022 | Axon Ligand™ with >100% purity available from supplier Axon Medchem, prime source of life science reagents for your research
SAN DIEGO--(BUSINESS WIRE)-- Bristol-Myers Squibb Company (NYSE: BMY) and AstraZeneca (NYSE: AZN) today announced results from an investigational Phase 3b clinical study which reported that ONGLYZA™
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Generic Saxagliptin tablets are used for the management of the type 2 diabetes. Buy Onglyza to pose a control on the glycemic level. It is easily available on www.drugpillstore.net
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The soluble epoxide hydrolase (sEH) is an important enzyme chiefly involved in the metabolism of fatty acid signaling molecules termed epoxyeicosatrienoic acids (EETs). sEH inhibition (sEHI) has proven to be protective against experimental cerebral ischemia, and it is emerging as a therapeutic target for prevention and treatment of ischemic stroke. However, the role of sEH on synaptic function in the central nervous system is still largely unknown. This study aimed to test whether sEH C-terminal epoxide hydrolase inhibitor, 12-(3-adamantan-1-yl-ureido) dodecanoic acid (AUDA) affects basal synaptic transmission and synaptic plasticity in the prefrontal cortex area (PFC). Whole cell and extracellular recording examined the miniature excitatory postsynaptic currents (mEPSCs) and field excitatory postsynaptic potentials (fEPSPs); Western Blotting determined the protein levels of glutamate receptors and ERK phosphorylation in acute medial PFC slices. Application of the sEH C-terminal epoxide hydrolase
The mechanisms for amantadines antiviral and antiparkinsonian effects are unrelated. The mechanism of amantadines antiviral activity involves interference with the viral protein, M2, a proton channel.[14][15] After entry of the virus into cells via endocytosis, it is localized in acidic vacuoles; the M2 channel functions in transporting protons with the gradient from the vacuolar space into the interior of the virion. Acidification of the interior results in disassociation of ribonucleoproteins, and the initiation of viral replication. Amantadine and rimantadine function in a mechanistically identical fashion in entering the barrel of the tetrameric M2 channel, and blocking pore function (i.e., proton translocation). Resistance to the drug class is a consequence of mutations to the pore-lining residues of the channel, leading to the inability of the sterically bulky adamantane ring that both amantadine and rimantadine share, in entering in their usual way, into the channel.[citation ...
DPP-4 INHIBITORS, Dipeptidyl peptidase-4 inhibitor - Gliptins, Linagliptin , Tradjenta™,Saxagliptin , Onglyza™, Sitagliptin , Januvia®, KOMBIGLYZE XR (saxagliptin and metformin HCl ER), JANUMET® (sitagliptin and metformin HCl)
Manganese metal-organic framework (Mn-MOF) containing Mn2+ ions, benzenetricarboxylic acid (BTC) and N,N-dimethylformamid (DMF) was prepared and used as catalyst for oxidation of alkenes such as 1,1-diphenylethylene, trans-stilbene, cyclohexene, norbornene, styrene and cyclooctene to epoxides with 33-92% conversion and 75-100% selectivity and oxidation of alkanes such as fluorene, adamantane, ethylbenzene and diphenylmethane to alcohols or ketones with tert-butylhydroperoxide (TBHP) with 19-64% conversion and 80-100% selectivity. Study of the catalyst stability and reusability revealed that Mn-MOF behaves heterogeneously in the oxidation reactions.
A study was conducted to control thermoresponsivity with supramolecular self-assembly of pseudo-block copolymer based on star-shaped poly(N-isopropylacrylamide) with a β-cyclodextrin core and guest-bearing PEG. The study used a star polymer, synthesized with a β-CD core as molecular recognition moiety and multiple PNIPAAm arms as actuation moieties. Nuclear magnetic resonance (NMR) spectroscopy and X-ray photoelectron spectroscopy (XPS) were used to determine the degree of substitution (DS) of the purified macroinitiator. The study found that β-CD-core star polymer was obtained by synthesis of a β-CD-based macroinitiator. The study synthesized the macromolecular guests by coupling the molecular recognition moiety, adamantane with biocompatible hydrophilic poly(ehtylene glycol) (PEG ...
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2015 Society for Endocrinology. It is unclear whether the dipeptidyl peptidase 4 (DPP4) inhibitor can counteract brain insulin resistance, brain mitochondrial dysfunction, impairment of hippocampal synaptic plasticity and cognitive decline in testosterone-deprived obese rats. We hypothesized that DPP4 inhibitor vildagliptin improves cognitive function in testosterone-deprived obese rats by restoring brain insulin sensitivity, brain mitochondrial function and hippocampal synaptic plasticity. Thirty male Wistar rats received either a sham-operated (S, nZ6) or bilateral orchiectomy (ORX, nZ24). ORX rats were divided into two groups and fed with either a normal diet (ND (NDO)) or a high-fat diet (HFO) for 12 weeks. Then, ORX rats in each dietary group were divided into two subgroups (nZ6/subgroup) to receive either a vehicle or vildagliptin (3 mg/kg per day, p.o.) for 4 weeks. After treatment, cognitive function, metabolic parameters, brain insulin sensitivity, hippocampal synaptic plasticity and ...
Aims: Myocardial ischemia can result in marked mitochondrial damage leading to cardiac dysfunction, as such identifying novel mechanisms to limit mitochondrial injury is important. This study investigated the hypothesis that inhibiting soluble epoxide hydrolase (sEH), responsible for converting epoxyeicosatrienoic acids to dihydroxyeicosatrienoic acids protects mitochondrial from injury caused by myocardial infarction.Methods: sEH null and WT littermate mice were subjected to surgical occlusion of the left anterior descending artery or sham operation. A parallel group of WT mice received an sEH inhibitor, trans-4-[4-(3-adamantan-1-y1-ureido)-cyclohexyloxy]-benzoic acid (tAUCB; 10mg/L) or vehicle in the drinking water 4 days prior and 7 days post-MI. Cardiac function was assessed by echocardiography prior- and 7 days post surgery. Heart tissues were dissected into infarct, peri-infarct and non-infarct regions to assess ultrastructure by electron microscopy. Complexes I, II, IV, citrate synthase, PI3K
There is new medical research concerning pancreatic cancer linked to diabetes medicines in the DPP-4 inhibitor drug class.. In more detail, the use of dipeptidyl peptidase-4 inhibitors (DPP-4i) diabetes medicines may be associated with an increased risk for pancreatic cancer in patients with newly diagnosed type 2 diabetes. This finding comes from an August 20, 2019 article published online by the Diabetes Care medical journal.. Some of the more popular diabetes medicines in the dipeptidyl peptidase-4 (DPP-4) inhibitor drug class are Onglyza (saxagliptin), Nesina (alogliptin), and Tradjenta (linagliptin).. From the Abstract for this Diabetes Care article, "Nationwide Trends in Pancreatitis and Pancreatic Cancer Risk Among Patients With Newly Diagnosed Type 2 Diabetes Receiving Dipeptidyl Peptidase-4 Inhibitors", we get the following information:. ...
This selection from the eMedTV library explains why saxagliptin/metformin ER is used for type 2 diabetes in adults. It describes how this combination drug works, addresses possible off-label uses, and whether children can take it.
How much of 12:0 dodecanoic, lauric fatty acid is present in Veal, composite of trimmed retail cuts, separable fat, cooked in details, quantity how high or low 12:0 dodecanoic, lauric fatty acid nutrient content it has.
Chemical Entities of Biological Interest (ChEBI) is a freely available dictionary of molecular entities focused on small chemical compounds.
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Thank you for your interest in spreading the word about Diabetes Care.. NOTE: We only request your email address so that the person you are recommending the page to knows that you wanted them to see it, and that it is not junk mail. We do not capture any email address.. ...
Merck, known as MSD outside the United States and Canada, issued the following statement regarding the conclusion of the European Medicines Agency&#8217;s (EMA) Committee for Medicinal Products for Human Use&#160;(CHMP) ......MRK
The export option will allow you to export the current search results of the entered query to a file. Different formats are available for download. To export the items, click on the button corresponding with the preferred download format. By default, clicking on the export buttons will result in a download of the allowed maximum amount of items. To select a subset of the search results, click "Selective Export" button and make a selection of the items you want to export. The amount of items that can be exported at once is similarly restricted as the full export. After making a selection, click one of the export format buttons. The amount of items that will be exported is indicated in the bubble next to export format. ...
... causes arterial/arteriolar vasodilation leading to a decrease in blood pressure by activating peripheral D1 receptors.[5] It decreases afterload and also promotes sodium excretion via specific dopamine receptors along the nephron. The renal effect of fenoldopam and dopamine may involve physiological antagonism of the renin-angiotensin system in the kidney.[6] In contrast to dopamine, fenoldopam is a selective D1 receptor agonist with no effect on beta adrenoceptors, although there is evidence that it may have some alpha-1 [7] and alpha-2 adrenoceptor antagonist activity.[5] D1 receptor stimulation activates adenylyl cyclase and raises intracellular cyclic AMP, resulting in vasodilation of most arterial beds, including renal, mesenteric, and coronary arteries.[8] to cause a reduction in systemic vascular resistance. Fenoldopam has a rapid onset of action (4 minutes) and short duration of action (, 10 minutes) and a linear dose-response relationship at usual clinical doses.[9] ...
... (INN), also known as captodiamine, is an antihistamine sold under the trade names Covatine, Covatix, and Suvren which is used as a sedative and anxiolytic. The structure is related to diphenhydramine.[1] A 2004 study suggested captodiame may be helpful in preventing benzodiazepine withdrawal syndrome in people discontinuing benzodiazepine treatment.[1] In addition to its actions as an antihistamine, captodiamine has been found to act as a 5-HT2C receptor antagonist and σ1 receptor and D3 receptor agonist.[2] It produces antidepressant-like effects in rats.[2] However, captodiamine is unique among antidepressant-like drugs in that it increases brain-derived neurotrophic factor (BDNF) levels in the hypothalamus but not in the frontal cortex or hippocampus.[2] This unique action may be related to its ability to attenuate stress-induced anhedonia and corticotropin-releasing factor (CRF) signaling in the hypothalamus.[2] ...
The hormone prolactin stimulates lactation (production of breast milk). Dopamine, released by the hypothalamus stops the release of prolactin from the pituitary gland. Domperidone, by acting as an anti-dopaminergic agent, results in increased prolactin secretion, and thus promotes lactation (that is, it is a galactogogue). In some nations, including Australia, domperidone is used off-label, based on uncertain and anecdotal evidence of its usefulness, as a therapy for mothers who are having difficulty breastfeeding.[24][25] In the United States, domperidone is not approved for this or any other use.[26][27] A study called the EMPOWER trial was designed to assess the effectiveness and safety of domperidone in assisting mothers of preterm babies to supply breast milk for their infants.[28] The study randomized 90 mothers of preterm babies to receive either domperidone 10 mg orally three times daily for 28 days (Group A) or placebo 10 mg orally three times daily for 14 days followed by domperidone ...
InChI=1S/C18H22F2N4O/c19-15-5-3-14(4-6-15)17(25)2-1-7-23-8-10-24(11-9-23)18-21-12-16(20)13-22-18/h3-6,12-13,17,25H,1-2,7-11H2 ...
Djaldetti Ruth; Giladi Nir; Hassin-Baer Sharon; Shabtai Hertzel; Melamed Eldad (November-December 2003). "Pharmacokinetics of Etilevodopa Compared to Levodopa in Patient's With Parkinson's Disease: An Open-label, Randomized, Crossover Study". Clinical Neuropharmacology. 26 (6): 322-326. doi:10.1097/00002826-200311000-00012. PMID 14646613 ...
... has also been found to increase the analgesic effects of opioid drugs in a dose-dependent manner, in contrast to 5-HT1A agonists such as 8-OH-DPAT which were found to reduce opioid analgesia.[22][23] However, since 5-HT1A agonists were also found to reduce opioid-induced respiratory depression and WAY-100635 was found to block this effect,[24] it is likely that 5-HT1A antagonists might worsen this side effect of opioids. Paradoxically, chronic administration of the very high efficacy 5-HT1A agonist befiradol results in potent analgesia following an initial period of hyperalgesia, an effect most likely linked to desensitisation and/or downregulation of 5-HT1A receptors (i.e. analogous to a 5-HT1A antagonist-like effect).[25][26][27] As with other 5-HT1A silent antagonists such as UH-301 and robalzotan, WAY 100635 can also induce a head-twitch response in rodents.[28] ...
Melis MR, Succu S, Sanna F, Melis T, Mascia MS, Enguehard-Gueiffier C, Hubner H, Gmeiner P, Gueiffier A, Argiolas A (October 2006). "PIP3EA and PD-168077, two selective dopamine D4 receptor agonists, induce penile erection in male rats: site and mechanism of action in the brain". The European Journal of Neuroscience. 24 (7): 2021-30. doi:10.1111/j.1460-9568.2006.05043.x. PMID 17067298 ...
The present meta-analysis was conducted to estimate the magnitude of the effects of methylphenidate and amphetamine on cognitive functions central to academic and occupational functioning, including inhibitory control, working memory, short-term episodic memory, and delayed episodic memory. In addition, we examined the evidence for publication bias. Forty-eight studies (total of 1,409 participants) were included in the analyses. We found evidence for small but significant stimulant enhancement effects on inhibitory control and short-term episodic memory. Small effects on working memory reached significance, based on one of our two analytical approaches. Effects on delayed episodic memory were medium in size. However, because the effects on long-term and working memory were qualified by evidence for publication bias, we conclude that the effect of amphetamine and methylphenidate on the examined facets of healthy cognition is probably modest overall. In some situations, a small advantage may be ...
Most frequent side effects are nausea, orthostatic hypotension, headaches, and vomiting through stimulation of the brainstem vomiting centre.[9] Vasospasms with serious consequences such as myocardial infarction and stroke that have been reported in connection with the puerperium, appear to be extremely rare events.[10] Peripheral vasospasm (of the fingers or toes) can cause Raynaud's Phenomenon. Bromocriptine use has been anecdotally associated with causing or worsening psychotic symptoms (its mechanism is in opposition of most antipsychotics, whose mechanisms generally block dopamine).[11] Pulmonary fibrosis has been reported when bromocriptine was used in high doses for the treatment of Parkinson's disease.[12] Use to suppress milk production after childbirth was reviewed in 2014 and it was concluded that in this context a causal association with serious cardiovascular, neurological or psychiatric events could not be excluded with an overall incidence rate estimated to range between 0.005% ...
... (Serentil) is a piperidine neuroleptic drug belonging to the class of drugs called phenothiazines, used in the treatment of schizophrenia. It is a metabolite of thioridazine. The drug's name is derived from the methylsulfoxy and piperidine functional groups in its chemical structure. It has central antiadrenergic, antidopaminergic, antiserotonergic and weak muscarinic anticholinergic effects. Serious side effects include akathisia, tardive dyskinesia and the potentially fatal neuroleptic malignant syndrome. Mesoridazine was withdrawn from the United States market in 2004 due to dangerous side effects, namely irregular heart beat and QT-prolongation of the electrocardiogram.[1] It currently appears to be unavailable worldwide. ...
... is a synthetic compound that acts as a selective antagonist on D2 dopamine receptors.[1] Its selectivity to the cerebral D2 receptors is characterized by its respective Ki-values, which are as follows: 1.8, 3.5, 2400 and 18000 nM for D2, D3, D4 and D1 receptors respectively. It can be radiolabelled with radioisotopes, e.g. 3H or 11C and used as a tracer for in vitro imaging (autoradiography) as well as in vivo imaging positron emission tomography (PET). Images obtained by cerebral PET scanning (e.g. PET/CT or PET/MRI) allow the non-invasive assessment of the binding capacity of the cerebral D2 dopamine receptor, which can be useful for the diagnosis of movement disorders. In particular, cerebral D2 receptor binding as measured by carbon-11-raclopride (11C-raclopride) has shown to reflect disease severity of Huntington's disease, a genetical disease characterized by selective degeneration of cerebral D2 receptors.[2] Other studies have investigated the relationship of D2 receptor ...
InChI=1S/C20H33N3O3S/c1-4-10-22-14-17(21-27(25,26)23(5-2)6-3)11-16-12-18-15(13-19(16)22)8-7-9-20(18)24/h7-9,16-17,19,21,24H,4-6,10-14H2,1-3H3/t16-,17+,19-/m1/s1 ...
... crosses the protective blood-brain barrier, whereas dopamine itself cannot. Thus, L-DOPA is used to increase dopamine concentrations in the treatment of Parkinson's disease and dopamine-responsive dystonia. This treatment was made practical and proven clinically by George Cotzias and his coworkers, for which they won the 1969 Lasker Prize.[4][5] Once L-DOPA has entered the central nervous system, it is converted into dopamine by the enzyme aromatic L-amino acid decarboxylase, also known as DOPA decarboxylase. Pyridoxal phosphate (vitamin B6) is a required cofactor in this reaction, and may occasionally be administered along with L-DOPA, usually in the form of pyridoxine.. Besides the central nervous system, L-DOPA is also converted into dopamine from within the peripheral nervous system. Excessive peripheral dopamine signaling causes many of the adverse side effects seen with sole L-DOPA administration. To bypass these effects, it is standard clinical practice to coadminister (with ...
"Adamantane". Organic Syntheses. CS1 maint: Multiple names: authors list (link) ; Collective Volume, 5, p. 16 Li, Xiaofang; Hou ... endo-tetrahydrodicyclopentadiene which on reaction with aluminium chloride at elevated temperature rearranges to adamantane. ...
InChI=1S/C25H29N3O2/c1-27-14-18(13-26-25(29)30-16-17-7-4-3-5-8-17)11-21-20-9-6-10-22-24(20)19(12-23(21)27)15-28(22)2/h3-10,15,18,21,23H,11-14,16H2,1-2H3,(H,26,29)/t18-,21+,23+/m0/s1 ...
... (MDPPP) is a stimulant designer drug. It was sold in Germany in the late 1990s and early 2000s as an ingredient in imitation ecstasy (MDMA) pills.[1] It shares a similar chemical structure with α-PPP and MDPV,[2][3][4] and has been shown to have reinforcing effects in rats.[5] ...
In 1960 the Austrian biochemist Oleh Hornykiewicz, while at the University of Vienna, examined results of autopsies of patients who had died with Parkinson's disease. He suggested that the disease was associated with, or caused by, a reduction in the levels of dopamine in the basal ganglia of the brain. Since dopamine itself did not enter the brain, he tried treating twenty patients with a racemic mixture of dihydroxyphenylalanine (DOPA), which could enter the brain and be converted there to dopamine by the action of DOPA decarboxylase. His results were positive, as were those of another trial in Montreal run by André Barbeau. Unfortunately, other investigators were unable to replicate these early results, and the use of DOPA remained in question until 1967, when George Cotzias at the Brookhaven National Laboratories in Upton, New York, used megadoses of DOPA, up to 16 grams per day. Not long after these results became known, Curt Porter at Merck showed that L-DOPA was the active stereoisomer, ...
Other adamantane antivirals subsequently followed, such as rimantadine (1-(1-aminoethyl)adamantane) and adapromine (1-(1- ... Bromantane is an adamantane derivative. It is also known as adamantylbromphenylamine, from which its name was derived. In the ... Bromantane, sold under the brand name Ladasten, is an atypical psychostimulant and anxiolytic drug of the adamantane family ... These findings may also extend to the other adamantanes such as adapromine, rimantadine, and bromantane, and might potentially ...
Adamantanes: Amantadine • Memantine • Rimantadine Aminotetralins: 7-OH-DPAT • 8-OH-PBZI • Rotigotine • UH-232 Benzazepines: 6- ...
These findings might also extend to the other adamantanes such as adapromine, rimantadine, and bromantane and could explain the ... Morozov, I. S.; Ivanova, I. A.; Lukicheva, T. A. (2001). "Actoprotector and Adaptogen Properties of Adamantane Derivatives (A ... Tromantadine Spasov, A. A.; Khamidova, T. V.; Bugaeva, L. I.; Morozov, I. S. (2000). "Adamantane derivatives: Pharmacological ... Adapromine is an antiviral drug of the adamantane group related to amantadine (1-aminoadamantane), rimantadine (1-(1-aminoethyl ...
In 1941, while at Zagreb, Prelog developed the first synthesis of adamantane, a hydrocarbon with an unusual structure that was ...
It has a cage-like structure similar to adamantane. It is useful in the synthesis of other chemical compounds, e.g., plastics, ... Garcia, J. C.; Justo, J. F.; Machado, W. V. M.; Assali, L. V. C. (2009). "Functionalized adamantane: building blocks for ... The molecule has a symmetric tetrahedral cage-like structure, similar to adamantane, whose four "corners" are nitrogen atoms ...
Adamantane Twistane Propellane Hexanitrohexaazaisowurtzitane Fieser, L. F. (1965). "Extensions in the use of plastic ...
Highly reactive 1,3-dehydro derivative of adamantane". J. Am. Chem. Soc. 91 (16): 4593-4593. doi:10.1021/ja01044a072. ... This compound is formally derived from adamantane by removing two hydrogens and adding an internal bond. It can be viewed as [ ...
... s also known as nanodiamonds or condensed adamantanes may include one or more cages (adamantane, diamantane, ... Examples include: Adamantane (C10H16) Iceane (C12H18) BC-8 (C14H20) Diamantane (C14H20) also diadamantane, two face-fused cages ... Adamantane derivatives have been proposed as a functionalizing molecule for enhancing electron-tunneling-based DNA sequencing ... García, J. C.; Justo, J. F.; Machado, W. V. M.; Assali, L. V. C. (2009). "Functionalized adamantane: building blocks for ...
To be more precise, it is four fused cyclohexanes in chair form. To see this it is necessary to see the structure - sadly this is beyond my ASCII art sk...
... are resistant to adamantane, one of the antiviral drugs that can be used to treat influenza infections. ... The antiviral agents are not adamantane itself, but two amino derivatives of adamantane called amantadine and rimantadine. ... adamantane -â noun Chemistry. A white crystalline alicyclic hydrocarbon, C10H16, consisting of four fused cyclohexane rings, ... based on the chemical name 1-aminoadamantane; see amino-, adamantane. adamant. -â adjective. 1. utterly unyielding in attitude ...
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Hála, S.; Eyem, J.; Burkhard, J.; Landa, S., Retention indices of adamantanes, J. Chromatogr. Sci., 1970, 8, 4, 203-209, https ... Burkhard, J.; Vais, J.; Vodicka, L.; Landa, S., Adamantane and its derivatives. XVI. The gas chromatographic characterization ... Bayat, Z.; Abad M.F.Y., Computational approaches to the prediction of the Kovats retention index (RI) for adamantane ... study of Kovats retention indices of some of adamantane derivatives by the genetic algorithm amd nultiply linear regression (GA ...
Adamantane cationsEdit. The adamantane cation can be produced by reacting 1-fluoro-adamantane with SbF5 and it has high ... Fluorination of adamantane with gaseous fluorine has also been reported.[40]. CarboxylationEdit. Carboxylation of adamantane ... Adamantane analoguesEdit. Many molecules adopt adamantane-like cage structures. Those include phosphorus trioxide P4O6, arsenic ... Adamantane cages can be stacked together to produce higher diamondoids, such as diamantane (C14H20 - two fused adamantane cages ...
... all 13 were resistant to adamantane-based drugs (amantadine and rimantadine). Resistance to adamantane drugs (which were ... Adamantane-based drugs, however, bind to the outside of M2 and cause it to be locked in the closed state. This means that in ... I think that this issue in particular--the binding of adamantane-based drugs to the influenza M2 channel--is quite exciting, as ... This is actually a relatively common mutation found in flu viruses in general and the main source of all flu adamantane ...
... adamantane should be called tricyclo[3.3.1.13,7]decane. However, IUPAC recommends using the name "adamantane". The adamantane ... adamantane slowly sublimes even at room temperature. Adamantane can be distilled with water vapor. The adamantane molecule ... Today, adamantane is an affordable chemical compound with a cost of about $1 a gram. All the above methods yield adamantane as ... The adamantane cation can be produced by reacting 1-fluoro-adamantane with SbF5 and it has high stability compared with other ...
... has been prepared in adamantane and its EPR spectrum recorded from 4 to 170 K. It has three magnetically equivalent Na nuclei ... Howard J.A., Hampson C.A., Histed M., Morris H., Mile B. (1987) The EPR Spectrum of Na3 in Adamantane. In: Jena P., Rao B.K., ... The sodium trimer, Na3, has been prepared in adamantane and its EPR spectrum recorded from 4 to 170 K. It has three ... This suggests that the correlation time, τc, is faster in adamantane than it is in argon. ...
Phosphatrioxa-adamantane is an organophosphorus compound that is used as a precursor to bulky phosphine ligands. Abbreviated ... Paul G. Pringle, Martin B. Smith "Phosphatrioxa-adamantane Ligands" in Phosphorus(III) Ligands in Homogeneous Catalysis: Design ...
Adamantane is one of the main products of Jinxiang chemical factory. We will supply the best adamantane to every customer. ... Home , Press , Application of Adamantane. Abstract:. Adamantane consists of four cyclohexanes fused each other in chair ... Application of Adamantane. Nanjing, China , Posted on November 7th, 2012. Its systematical name is tricyclo[3.3.1.1(3,7)]decane ...
We demonstrate that the dissociation dynamics of adamantane dications takes place in a two-step process: barrierless cage ... This work presents a photodissociation study of the diamondoid adamantane using extreme ultraviolet femtosecond pulses. The ... Table 1 List of correlated singly charged fragments coming from the dissociation of adamantane dication observed experimentally ... Adamantane molecules, C10H16 (powder from Aldrich with ,99% purity), are produced in the gas phase by a pulsed Even-Lavie valve ...
Adamantane is mainly used for the synthesis of medicine to treat influenza, serve as NMDA receptor channel blockers. Also be ... Incidence of adamantane resistance among influenza A (H3N2) viruses isolated worldwide from 1994 to 2005: a cause for concern. ... Adamantane: Consequences of the Diamondoid Structure. Chem. Rev. 1964, 64 (3), 277-300. ...
7-dichloroquinolines was studied using adamantane-containing amines in which substituents at the nitrogen atom differ in ... Keywords: amines; adamantane; Pd catalysis; amination; quinoline amines; adamantane; Pd catalysis; amination; quinoline ... Pd-catalyzed amination of isomeric 2,6-, 2,8-, 4,8- and 4,7-dichloroquinolines was studied using adamantane-containing amines ... Palladium-Catalyzed Amination of Dichloroquinolines with Adamantane-Containing Amines. Anton S. Abel 1. ...
These findings of adamantane resistance pertain to human influenza A (H3N2) viruses and not to avian influenza A (H5N1) viruses ... High Levels of Adamantane Resistance Among Influenza A (H3N2) Viruses and Interim Guidelines for Use of Antiviral Agents --- ... Incidence of adamantane resistance among influenza A (H3N2) viruses isolated worldwide from 1994 to 2005: a cause for concern. ... Resistance of influenza A viruses to adamantanes can occur spontaneously or emerge rapidly during treatment (3). A single point ...
These NPs (GC-CD/HSA-ADA NPs) consisted of β-cyclodextrin-modified glycol chitosan (GC-CD) and adamantane-conjugated human ... In this article, we introduce a new albumin NPs prototype fabricated via a host (β-cyclodextrin)-guest (adamantane) ... A novel prototype of albumin nanoparticles fabricated by supramolecular cyclodextrin-adamantane association.. [Seunghyun Lee, ...
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Evaluation of adamantane hydroxamates as botulinum neurotoxin inhibitors: synthesis, crystallography, modeling, kinetic and ...
In this study, we synthesized new compounds in which the AhR ligands were replaced with a hydrophobic adamantane moiety to ... Adamantane-ATRA, with an amide bond (Ad-ATRA-2, 3) was also prepared via the condensation of 8 with 13, following a similar ... Targeted Protein Degradation by Chimeric Compounds using Hydrophobic E3 Ligands and Adamantane Moiety by Takuji Shoda 1,*,†, ... Adamantane-ATRA, with an ester bond (Ad-ATRA-1, 2), was obtained after the reduction of the azide group in 5, the condensation ...
We have found adamantane to dissociatively photoionise via several parallel channels of which H, C3H7 and C4H8 losses are the ... Dissociative ionisation of adamantane: a combined theoretical and experimental study A. Candian, J. Bouwman, P. Hemberger, A. ... In this paper we characterise the dissociative ionisation of adamantane (C10H16) - the smallest member of the diamondoid family ... which is located at 10.55 eV with respect to neutral adamantane. In addition, we found dissociation channels leading to small ...
We identified adamantane resistance in 47% of 152 influenza A virus (H3N2) isolates collected during 2005. Resistant and ... Adamantane-resistant influenza A is an emerging problem, but infections caused by resistant and susceptible viruses have not ... Bright RA, Medina MJ, Xu X, Perez-Oronoz G, Wallis TR, Davis XM, Incidence of adamantane resistance among influenza A (H3N2) ... Adamantane resistance among influenza A viruses isolated early during the 2005-2006 influenza season in the United States.JAMA ...
Adamantanes have been used by chronic care facilities for influenza A prophylaxis; however, genotypic resistance ha ... Adamantanes have been used by chronic care facilities for influenza A prophylaxis; however, genotypic resistance has altered ... Control of an Outbreak due to an Adamantane-Resistant Strain of Influenza A (H3N2) in a Chronic Care Facility. ... Enhanced infection control precautions and adamantane prophylaxis were used to control spread of influenza in a chronic care ...
... a Adamantane P1-Ligand with tetrahydropyrano-tetrahydrofuran in P2 and isobutylamine in P1) ... HIV-1 wild Type protease with GRL-031-14A (a Adamantane P1-Ligand with tetrahydropyrano-tetrahydrofuran in P2 and isobutylamine ... We have developed an enantioselective synthesis of adamantane-derived hydroxyethylamine isosteres utilizing Sharpless a ... ... We have developed an enantioselective synthesis of adamantane-derived hydroxyethylamine isosteres utilizing Sharpless ...
We identified adamantane resistance in 47% of 152 influenza A virus (H3N2) isolates collected during 2005. Resistant and ... Adamantane-resistant influenza A is an emerging problem, but infections caused by resistant and susceptible viruses have not ... Adamantane-Resistant Influenza Infection During the 2004-05 Season Mahbubur Rahman*1, Rick A. Bright†2, Burney A. Kieke*, James ... Adamantane-Resistant Influenza Infection During the 2004-05 Season. ...
We have described previously that N-(5-adamantane-1-yl-methoxy-pentyl)-deoxynojirimycin (AMP-DNM), an inhibitor of ... The Glucosylceramide Synthase Inhibitor N-(5-Adamantane-1-yl-methoxy-pentyl)-deoxynojirimycin Induces Sterol Regulatory Element ... The Glucosylceramide Synthase Inhibitor N-(5-Adamantane-1-yl-methoxy-pentyl)-deoxynojirimycin Induces Sterol Regulatory Element ... The Glucosylceramide Synthase Inhibitor N-(5-Adamantane-1-yl-methoxy-pentyl)-deoxynojirimycin Induces Sterol Regulatory Element ...
  • Adamantane molecules consists of three connected cyclohexane rings arranged in the "armchair" configuration. (wikipedia.org)
  • While this study was recently complemented by a first time-resolved study 10 , to date no results have been published on the dissociation dynamics of multiply charged adamantane molecules. (nature.com)
  • These diamondoids occur naturally in petroleum deposits and have been extracted and purified into large pure crystals of polymantane molecules having more than a dozen adamantane cages per molecule. (wikipedia.org)
  • The success of the drug therapy of the virus and Parkinson's diseases using abiotic polyhedral adamantane molecules suggests the pharmaceutical potential of other xenobiotics with rigid three-dimensional molecular structure. (wikipedia.org)
  • Molecules within the Td point group include methane, phosphorus pentoxide, and adamantane. (wikipedia.org)
  • In his research, Schleyer has made contributions in the area of synthesis of adamantane and other cage molecules by rearrangement mechanisms. (wikipedia.org)
  • Especially noted position in history of the Faculty is reserved to professor Vladimir Prelog, winner of Nobel prize in chemistry in 1975, who held a chair in organic chemistry from 1934 to 1941 and established strong bonds with local scientist and also with industry in production of medicines but also interesting new molecules like adamantane. (wikipedia.org)
  • This work presents a photodissociation study of the diamondoid adamantane using extreme ultraviolet femtosecond pulses. (nature.com)
  • Adamantane: Consequences of the Diamondoid Structure. (alfa.com)
  • In this paper we characterise the dissociative ionisation of adamantane (C 10 H 16 ) - the smallest member of the diamondoid family - utilising imaging Photoelectron Photoion Coincidence (iPEPICO) spectroscopy and Density Functional Theory (DFT) calculations. (rsc.org)
  • Adamantane is the simplest known diamondoid existing naturally. (raypeatforum.com)
  • Pentamantane has nine isomers with chemical formula C26H32 and one more pentamantane exists with chemical formula C25H30 Cyclohexamantane (C26H30) Super-adamantane (C30H36) One tetramantane isomer is the largest ever diamondoid prepared by organic synthesis using a keto-carbenoid reaction to attach cyclopentane rings. (wikipedia.org)
  • It is a cycloalkane and an isomer of the simplest diamondoid, adamantane, and like adamantane, is not very volatile. (wikipedia.org)
  • The structure of the P4O10 cage is reminiscent of adamantane with Td symmetry point group. (wikipedia.org)
  • Another way of visualising the structure is that it is the P4S10 adamantane (P4O10) structure with a PS3+ vertex removed. (wikipedia.org)
  • The isoelectronic anion [Ge4Se− which has the adamantane like P4O10 structure is known, an example is the sodium salt Na4Ge4Se10. (wikipedia.org)
  • Ga2S3 dissolves in aqueous solutions of potassium sulfide, K2S to form K8Ga4S10 containing the (Ga4S10)8− anion which has an adamantane, molecular P4O10 structure. (wikipedia.org)
  • On the left is adamantane with four hydrogen atoms abstracted. (blogspot.com)
  • In order to overcome this problem a larger building block was chosen, penta-adamantane, rendered on the right also with four hydrogen atoms abstracted. (blogspot.com)
  • 1,3-Dehydroadamantane, formally tetracyclo[3.3.1.13,7.01,ecane, is an organic compound with formula C10H14, which can be obtained from adamantane by removal of two hydrogen atoms to create an internal bond. (wikipedia.org)
  • The compound was characterized by computational and spectroscopic techniques and found to possess a cage-like structure similar to adamantane in which the four methanetriyl carbon bridgeheads are replaced by arsenic atoms and three of the six methylene bridges are replaced by oxygen atoms. (wikipedia.org)
  • Adamanzanes (abbreviated Adz) are compounds containing four nitrogen atoms linked by carbons (analogous to adamantane with nitrogen at the branched position). (wikipedia.org)
  • Cyclic and acyclic chloronium, bromonium and iodonium ions have been structurally characterised by X-ray crystallography, such as the adamantylideneadamantanebromonium cation, also known as dispiro[adamantane-2,3′-[1λromirane-3′,2″-adamantan]-1′-ylium, shown below. (wikipedia.org)
  • Additionally, functionalized diamondoids (adamantanes) have been proposed as molecular building blocks for self-assembled molecular crystals. (wikipedia.org)
  • Its tetrahedral molecular structure is similar to that of adamantane and almost identical to the structure of phosphorus pentoxide. (wikipedia.org)
  • The hexamethylenetetramine tetrahedral cage-like structure, similar to adamantane, serves as molecular building block to form a tridimensional polymeric network. (wikipedia.org)
  • Its molecular structure is uncommon for pharmacological compounds in that it has both a ozonide (trioxolane) group and an adamantane substituent. (wikipedia.org)
  • Paul G. Pringle, Martin B. Smith "Phosphatrioxa-adamantane Ligands" in Phosphorus(III) Ligands in Homogeneous Catalysis: Design and Synthesis, Edited by Paul C. J. Kamer and Piet W. N. M. van Leeuwen, 2012 John Wiley, New York. (wikipedia.org)
  • In this study, we synthesized new compounds in which the AhR ligands were replaced with a hydrophobic adamantane moiety to investigate the mechanisms of AhR-independent degradation. (mdpi.com)
  • Adamantane is the most stable among all the isomers with formula C10H16, which include the somewhat similar twistane. (wikipedia.org)
  • Examples include: Adamantane (C10H16) Iceane (C12H18) BC-8 (C14H20) Diamantane (C14H20) also diadamantane, two face-fused cages Triamantane (C18H24), also triadamantane. (wikipedia.org)
  • The process was still too complex, and a more convenient method was found in 1957 by Paul von Ragué Schleyer: dicyclopentadiene was first hydrogenated in the presence of a catalyst (e.g. platinum dioxide) and then transformed into adamantane using a Lewis acid (e.g. aluminium chloride) as another catalyst. (wikipedia.org)
  • It is the organic compound 1-adamantylamine or 1-aminoadamantane, meaning it consists of an adamantane backbone that has an amino group substituted at one of the four methyne positions. (wikipedia.org)
  • Continuing the trend seen in other cannabinoids of this generation, it contains a valine amino acid amide residue as part of its structure, where older cannabinoids contained a naphthyl or adamantane residue. (wikipedia.org)
  • We compared clinical and demographic characteristics of patients infected with either adamantane-susceptible or -resistant strains of influenza A during the 2004-05 season. (cdc.gov)
  • Due to the type of interaction that occurs between M2 and the adamantanes, the M2 proteins can undergo mutation, which makes it resistant to these drugs without losing its activity. (bvsalud.org)
  • Diamondoids also known as nanodiamonds or condensed adamantanes may include one or more cages (adamantane, diamantane, triamantane, and higher polymantanes) as well as numerous isomeric and structural variants of adamantanes and polymantanes. (wikipedia.org)
  • A-834,735 AB-005 AM-1248 APICA JWH-018 JWH-250 RCS-4 RCS-8 N-(S)-Fenchyl-1-(2-morpholinoethyl)-7-methoxyindole-3-carboxamide (1-Pentylindol-3-yl)-(2,2,3,3-tetramethylcyclopropyl)methanone Structural scheduling of synthetic cannabinoids Adamantane Jankovics, P. T. (wikipedia.org)
  • Adamantane was the first, and "Congressane", as diamantane came to be known, was only the second member of an entire family of compounds known as the diamandoids. (wikipedia.org)
  • 2 The barrier for rearrangement of the inverted adamantane into adamantane, which involved a cleave of a C-C bond, is 17 kcal mol -1 , which implies a half-life of 30 ms at 298K and and 2 days at 195 K. The perfluoro isomer has a higher barrier (32 kcal mol -1 ) and a longer half-life (110 years at 298K). (comporgchem.com)
  • We demonstrate that the dissociation dynamics of adamantane dications takes place in a two-step process: barrierless cage opening followed by Coulomb repulsion-driven fragmentation. (nature.com)
  • The study reveals, in addition to the expected hydrogen loss, dissociation via a number of parallel channels which all start with an opening of the carbon cage and hydrogen migration indicating that the low photostability of adamantane could explain its deficiency in astronomical observations. (nature.com)
  • Later, another German chemist D. Bottger tried to obtain adamantane using Meerwein's ester as precursor. (wikipedia.org)
  • In this work, a novel bridged organosilane precursor, adamantane-bridged organosilane (ADBO), was synthesized successfully which was employed to prepare adamantane-based (ADH-based) periodic mesoporous organosilica (PMO) thin film in the presence of porogen and acid catalyst via evaporation-induced self-assembly (EISA) after spin-coating procedure. (springer.com)
  • Univariate comparisons were performed, and crude and adjusted prevalence ratios were computed to evaluate the association between adamantane resistance and age, gender, vaccination status, date of clinical encounter, and presence of a high-risk medical condition. (cdc.gov)
  • dicyclopentadiene was first hydrogenated in the presence of a catalyst (e.g. platinum dioxide ) and then transformed into adamantane using a Lewis acid (e.g. aluminium chloride ) as another catalyst. (wikipedia.org)
  • Hydrogenation of dicyclopentadiene gives endo-tetrahydrodicyclopentadiene which on reaction with aluminium chloride at elevated temperature rearranges to adamantane. (wikipedia.org)
  • Adamantane susceptibility was assessed by conventional sequencing or pyrosequencing assay ( 2 ) with modifications ( 3 ), using viral RNA extracted from original clinical specimens and/or virus isolates. (cdc.gov)