A tricyclo bridged hydrocarbon.
An RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza.
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.
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.
The ability of viruses to resist or to become tolerant to chemotherapeutic agents or antiviral agents. This resistance is acquired through gene mutation.
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.
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.
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)
The formation of crystalline substances from solutions or melts. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
A phase transition from liquid state to gas state, which is affected by Raoult's law. It can be accomplished by fractional distillation.
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)
The development and use of techniques to study physical phenomena and construct structures in the nanoscale size range or smaller.
Naturally occurring complex liquid hydrocarbons which, after distillation, yield combustible fuels, petrochemicals, and lubricants.
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)
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)
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.
Detailed account or statement or formal record of data resulting from empirical inquiry.
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.
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.
Activities performed to identify concepts and aspects of published information and research reports.
Water-soluble proteins found in egg whites, blood, lymph, and other tissues and fluids. They coagulate upon heating.
Use of sophisticated analysis tools to sort through, organize, examine, and combine large sets of information.
A major protein in the BLOOD. It is important in maintaining the colloidal osmotic pressure and transporting large organic molecules.
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. 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)
The study of CHEMICAL PHENOMENA and processes in terms of the underlying PHYSICAL PHENOMENA and processes.
The physical phenomena describing the structure and properties of atoms and molecules, and their reaction and interaction processes.
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)
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.
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.
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.
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.
Sudden increase in the incidence of a disease. The concept includes EPIDEMICS and PANDEMICS.
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.

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
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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
Testing of 2009 influenza A (H1N1), influenza A (H3N2), and influenza B virus isolates for resistance to neuraminidase inhibitors (oseltamivir and zanamivir) is performed at CDC using a functional assay. Additional 2009 influenza A (H1N1) clinical samples are tested for a single mutation in the neuraminidase of the virus known to confer oseltamivir resistance (H275Y). The data summarized below combine the results of both testing methods. These samples are routinely obtained for surveillance purposes rather than for diagnostic testing of patients suspected to be infected with antiviral resistant virus.. High levels of resistance to the adamantanes (amantadine and rimantadine) persist among 2009 influenza A (H1N1) and A (H3N2) viruses (the adamantanes are not effective against influenza B viruses). As a result of the sustained high levels of resistance, data from adamantane resistance testing are not presented in the table below. ...
(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 ...
The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...
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 ...
Dipeptidyl peptidase-4 inhibitors, such as saxagliptin, have been reported to have beneficial effects on β-cell function, but the specific underlying mechanism remains unclear. Stromal cell-derived factor-1α (SDF-1α), a chemokine produced in multiple organs, has been considered as a crucial regulator in promoting β-cell survival. Here, we speculate that SDF-1α might mediate the effect of saxagliptin on improving β-cell function. After 12-week saxagliptin treatment in high-fat diet/streptozotocin-induced diabetic rats, significant improvement in pancreas insulin secretion capacity evaluated by hyperglycemia clamp and increased β-cell to α-cell areas ratio were observed. Saxagliptin significantly induced β-cell proliferation and upregulated the expression of proliferation-related factors including c-myc and cyclind D1 determined with western blotting from the isolated islets. The expression/activity of DPP-4 was significantly reduced and paralleled with the restoration of SDF-1α levels in the
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
Bismillah Assalamualaikum/Salam sejahtera,, Salam kini lepasi bulan syawal 2014 menanti detik seterusnya Temui nota ubat kali ini untuk sebuah perjalanan isu blog ini,, Kepada yang suka, jika suka teruskan layari bingkisan nota ubat.net Apa itu Saxagliptin ,5mg ? Secara ringkas tablet Saxagliptin 5mg merupakan ubat biji untuk di makan atas nama kimia ubat yang original…
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The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...
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.
AstraZeneca today announced that the US Food and Drug Administration (FDA) Endocrinologic and Metabolic Drugs Advisory Committee (EMDAC) voted 13 to 1 (1 abstained; 15 total votes) that the results...
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.
Malaria remains a major disease in the developing world and globally is the most important parasitic disease causing significant morbidity and mortality. Because of widespread resistance to conventional antimalarials, including chloroquine (CQ), new drugs are urgently needed. Here we report on the antimalarial efficacy, both in vitro and in vivo, of a series of aminoquinoline derivatives with adamantane or benzothiophene as a carrier. In vitro efficacy was evaluated by a lactate dehydrogenase (LDH) assay in cultures of a CQ-sensitive (3D7) and CQ-resistant (Dd2) strain of Plasmodium falcipanim. Of a series of 26 screened compounds, 12 that exerted a growth inhibition rate of ,= 5% were further examined in vitro to determine the 50% inhibitory concentration (IC50) values. Nine compounds shown in preliminary experiments to be non-toxic in vivo were evaluated in C57BL/6 mice infected with Plasmodium herghei ANKA strain using a modified Thompson test. All nine compounds examined in vivo pr...olonged ...
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.
For most adults, the recommended rimantadine dosage is 100 mg twice a day. This page from the eMedTV library also includes rimantadine dosing guidelines for other people, such as children, the elderly, and people with certain medical conditions.
Make sure your doctor knows if you have liver or kidney disease before using rimantadine. This eMedTV resource offers more precautions and warnings with rimantadine and lists other conditions you should tell your doctor about before starting the drug.
This is an open-label study of ZYC300 in the treatment of advanced stage malignancy of the kidney in patients who have not had previous immune-based therapies or treatment of advanced stage malignancies (cancerous growths) of the ovary, breast, colon, or hormone-refractory prostate in patients who have failed at least one but no more than two prior regimens of chemotherapy. Patients who meet all entry criteria will be administered 600 mg/m^2 cyclophosphamide intravenously 3 days before each dose of ZYC300. ZYC300 will be administered at 400 micrograms DNA/total dose every two weeks for a maximum of six doses (6 cycles).. ZYC300 is a plasmid DNA formulated within biodegradable microencapsulated particles. This is the first time that ZYC300 and Cyclophosphamide will be given together. Cyclophosphamide is a chemotherapy drug approved by the FDA that has been used for many years in many different kinds of cancer. In this trial the study drug will be used to boost the immune system. Sometimes the ...
The adamantanes are a class of compounds that have found use in the treatment of influenza A and Parkinsons disease, among others. The mode of action for influenza A is based on the adamantanes interaction with the transmembrane M2 channel, whereas the treatment of Parkinsons disease is thought to relate to a channel block of N-methyl-D-aspartate receptors. An understanding of how these compounds interact with the lipid bilayer is thus of great interest. We used molecular-dynamics simulations to calculate the potential of mean force of adamantanes in a lipid bilayer. Our results demonstrate a preference for the interfacial region of the lipid bilayer for both protonated and deprotonated species, with the protonated species proving significantly more favorable. However, the protonated species have a large free-energy barrier in the center of the membrane. In contrast, there is no barrier (compared with aqueous solution) at the center of the bilayer for deprotonated species, suggesting that the
TY - JOUR. T1 - Alkylation of pyridine-3,5-dicarboxamide and pyridine-3,5-dicarbonitriles by radical substitution. AU - Kanomata, Nobuhiro. AU - Nagahara, Hisashi. AU - Tada, Masaru. PY - 1992/10/1. Y1 - 1992/10/1. N2 - Structural modification of NAD(P) model compounds, N,N,N′,N′ tetramethylpyridine-3,5-dicarboxamide (1), pyridine-3,5-dicarbonitrile (2), and 4-methylpyridine-3,5-dicarbonitrile (3), have been explored by the reaction with alkyl radicals such as the 1-adamantyl, tert-butyi, and isopropyl radicals. The alkyl substitutions of compounds 1, 2, and 3 with the 1-adamantyl and the fert-butyl radical gave both 2-mono and 2,6-disubsti-tution products, whereas the reaction of compound 2 with the isopropyl radical gave 2-mono 6c, 2,4-di 7c, 2,6-di 8c, and 2,4,6-trisubstitution 9c products.. AB - Structural modification of NAD(P) model compounds, N,N,N′,N′ tetramethylpyridine-3,5-dicarboxamide (1), pyridine-3,5-dicarbonitrile (2), and 4-methylpyridine-3,5-dicarbonitrile (3), have been ...
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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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Schleyer, Paul von R.; Donaldson, M. M.; Nicholas, R. D.; Cupas, C. (1973). "Adamantane". Organic Syntheses.; Collective Volume ... On reaction with aluminium chloride at elevated temperature, this C10 hydrocarbon rearranges to adamantane. Dicyclopentadiene ... which undergoes acid-catalyzed rearrangement to adamantane. Merck Index, 11th Edition, 2744 NIOSH Pocket Guide to Chemical ...
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 ... Morozov, I. S.; Ivanova, I. A.; Lukicheva, T. A. (2001). "Actoprotector and Adaptogen Properties of Adamantane Derivatives (A ...
... 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 ...
Adamantanes: Amantadine • Memantine • Rimantadine Aminotetralins: 7-OH-DPAT • 8-OH-PBZI • Rotigotine • UH-232 Benzazepines: 6- ...
... is the ketone of adamantane. A white solid, it is prepared by oxidation of adamantane. It is a precursor to ... several adamantane derivatives. Adamantanone and some related polycyclic ketones, are reluctant to form enolates. This barrier ...
For example, it will oxidize adamantane to 1-adamantanol. Because it is such an aggressive oxidant, reaction conditions must be ... "Rigid Multivalent Scaffolds Based on Adamantane". The Journal of Organic Chemistry. 73 (3): 1056-1060. doi:10.1021/jo702310g. ...
It has a cage-like structure similar to adamantane. It is useful in the synthesis of other organic compounds, including ... 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. Tian, X; ... This compound is formally derived from adamantane by removing two hydrogens and adding an internal bond. It can be viewed as [ ...
Garcia, J. C.; Justo, J. F.; Machado, W. V. M.; Assali, L. V. C. (2009). "Functionalized adamantane: building blocks for ...
Detailed bibliography published by the web site Adamantane. ...
Garcia JC, Justo JF, Machado WV, Assali LV (2009). "Functionalized adamantane: building blocks for nanostructure self-assembly ...
This colorless solid is structurally related to adamantane. It is formally the anhydride of phosphorous acid, H3PO3, but cannot ...
Highly reactive 1,3-dehydro derivative of adamantane". J. Am. Chem. Soc. 91 (16): 4593-4593. doi:10.1021/ja01044a072. Matsuoka ... which can be obtained from adamantane by removal of two hydrogen atoms to create an internal bond. It is a polycyclic ...
Adamantane was the first, and "Congressane", as diamantane came to be known, was only the second member of an entire family of ... Olah, G. A; Ramaiah, P.; Rao, C. B.; Sandford, G.; Golam, R.; Trivedi, N. J.; Olah, J. A. (1993). "Nitration of adamantane and ... Diamantane then became as readily available as adamantane and its chemistry could be studied more easily. Diamantane can be ... Gordadze, G. N.; Giruts, M. V. (2008). "Synthesis of adamantane and diamantane hydrocarbons by high-temperature cracking of ...
http://www.adamantane.org/article-6172722.html "Robert Courrier. 6 October 1895-14 March 1986", Jamshed R. Tata, Biographical ...
They are the adamantanes and NAIs. The adamantanes only work on influenza A so since 2010 WHO recommended the usage of NAIs for ... In contrast to adamantanes, NAIs are less toxic and less prone to promote drug-resistant influenza. Moreover, they are ... Neuraminidase Neuraminidase inhibitors Influenza virus Adamantane Christopher W. Cairo. (2014) Inhibitors of the human ...
Adamantane is added to some dyes to prolong their life. Cycloheptatriene and cyclooctatetraene (COT) can be added as triplet ...
Currently, adamantane resistance is high among circulating influenza A viruses. Thus, they are no longer recommended for ... These findings may also extend to the other adamantanes such as adapromine, rimantadine, and bromantane, and could explain the ... Rimantadine is a closely related adamantane derivative with similar biological properties; both target the M2 proton channel of ... "Effects of the 1-amino-adamantanes at the MK-801-binding site of the NMDA-receptor-gated ion channel: a human postmortem brain ...
Hypothetical nanothread architectures built from the smallest diamondoids (adamantane) have been proposed to have higher ... Marutheeswaran, S.; Jemmis, Eluvathingal D. (15 March 2018). "Adamantane-Derived Carbon Nanothreads: High Structural Stability ...
This finding, reported by Scawab et al., was the beginning of medicinal chemistry of adamantane derivatives in the context of ... Before this finding, memantine, another adamantane derivative, had been synthesized by Eli Lilly and Company in 1963. The ... Wanka L, Iqbal K, Schreiner PR (May 2013). "The lipophilic bullet hits the targets: medicinal chemistry of adamantane ... two adamantane derivatives, the affinity for the binding site of NR1/NR2B subunit is much greater for memantine. In patch-clamp ...
"Synthesis and Single-Molecule Imaging of Highly Mobile Adamantane-Wheeled Nanocars". ACS Nano. 7 (1): 35-41. doi:10.1021/ ...
Like rimantadine, amantadine, and adapromine, tromantadine is a derivative of adamantane. Tromantadine inhibits the early and ...
Both rimantadine and the similar drug amantadine are derivates of adamantane. RImantadine is found to be more effective than ...
The adamantanes amantadine and rimantadine are orally administered drugs that block the influenza virus's M2 ion channel, ... Adamantane resistance first emerged in H3N2 in 2003, becoming worldwide by 2008. Oseltamivir resistance is no longer widespread ... because the 2009 pandemic H1N1 strain (H1N1 pdm09), which is resistant to adamantanes, seemingly replaced resistant strains in ...
Derivatives of adamantane have also been prepared using the Hofmann-Löffler-Freytag reaction. When N-chloroamine 56 was treated ... 6 adamantane such as 60 might be formed under standard Hofmann-Löffler-Freytag reaction conditions; however, the yields are ... 6 adamantane". Tetrahedron Lett. 14 (29): 2699-2701. doi:10.1016/S0040-4039(01)96116-7. Deshpande, R. P.; Nayak, U. R. (1979). ...
Adamantane Ethambutol (An older drug with a similar mechanism of action) Jia, L.; Tomaszewski, J. E.; Hanrahan, C.; Coward, L ...
AB-001 - one of the earliest adamantane derivatives discovered as a designer cannabinoid. AB-001 was unknown in the scientific ... "The Synthesis and Pharmacological Evaluation of Adamantane-Derived Indoles: Cannabimimetic Drugs of Abuse". ACS Chem Neurosci. ...
"The Genesis and Spread of Reassortment Human Influenza A/H3N2 Viruses Conferring Adamantane Resistance". Molecular Biology and ...
2007: Wanka/Schreiner, chiral peptidic adamantane-based thiourea, catalysis of Morita-Baylis-Hillman reactions. 2007: ...
Today, adamantane is an affordable chemical compound with a cost of about $1 a gram. All the above methods yield adamantane as ... Adamantane is the most stable isomer of C10H16. The spatial arrangement of carbon atoms in the adamantane molecule is the same ... Most reactions of adamantane occur via the 3-coordinated carbon sites. They are involved in the reaction of adamantane with ... Adamantane is an organic compound with a formula C10H16 or, more descriptively, (CH)4(CH2)6. Adamantane molecules can be ...
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 ...
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 ...
The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...
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 ...
... 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. ...
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 ...
... adamantane-1-carbohydrazide; CAS Number: ; find Princeton BioMolecular Research, Inc.-PRIH93ED8170 MSDS, related peer-reviewed ... Home > PRIH93ED8170 N-[(1Z)-3-amino-1H-isoindol-1-ylidene]adamantane-1-carbohydrazide ...
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 ...
A return to wide circulation of adamantane-sensitive A(H3N2) viruses would revive the option of using these drugs for treatment ... However, during the 2017 influenza season in Australia, 15/461 (3.3%) adamantane-sensitive A(H3N2) viruses encoding serine at ... influenza viruses have been resistant to the adamantane class of antivirals. ... The emergence of adamantane resistance in influenza A(H1) viruses in Australia and regionally in 2006. Antiviral Res. 2007;75(2 ...
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 ...
Optimized PM6_D3H4 data set: MERS=(1,1,1) GNORM=4 PM6-D3H4 THREADS=1 1,3-bis((Pyrid-2-ylamino)carbonyl)adamantane (RIZVOL) (PM6 ... Optimized PM7 data set: MERS=(1,1,1) GNORM=4 1,3-bis((Pyrid-2-ylamino)carbonyl)adamantane (RIZVOL) O 0.00548595 +1 0.0140174 +1 ... 111 1,3-bis((Pyrid-2-ylamino)carbonyl)adamantane (RIZVOL) (Previous) Nicotinamide (NICOAM01). (Back) Elements: O 1 N 2 C 11 H ...
Specific binding of adamantane drugs and direction of their polar amines in the pore of the influenza M2 transmembrane domain ...
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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-bridged organosilane (ADBO), was synthesized successfully which was employed to prepare adamantane-based (ADH-based ... Fort RC, Schleyer PV (1964) Adamantane: consequences of the diamondoid structure. Chem Rev 64:277-300CrossRefGoogle Scholar ... Novel adamantane-based periodic mesoporous organosilica film with ultralow dielectric constant and high mechanical strength. ... Prepare adamantane-based (ADH-based) periodic mesoporous organosilica (PMO) through evaporation-induced self-assembly (EISA) ...
2 The barrier for rearrangement of the inverted adamantane into adamantane, which involved a cleave of a C-C bond, is 17 kcal ... Archive for the adamantane Category. 1-Adamantyl cation - Predicting its NMR spectra. What is required in order to compute ... Inverted adamantane. There is a mystique surrounding chemical torture. Just how much strain can one subject a poor old carbon ... 1) Irikura, K. K., In-Adamantane, a Small Inside-Out Molecule, J. Org. Chem. 2008, 73, 7906-7908, DOI: 10.1021/jo801806w. ...
2 The barrier for rearrangement of the inverted adamantane into adamantane, which involved a cleave of a C-C bond, is 17 kcal ... Inverted adamantane. There is a mystique surrounding chemical torture. Just how much strain can one subject a poor old carbon ... 1) Irikura, K. K., In-Adamantane, a Small Inside-Out Molecule, J. Org. Chem. 2008, 73, 7906-7908, DOI: 10.1021/jo801806w. ... One Response to "Inverted adamantane". * syregnask. responded on 05 Mar 2009 at 4:24 am # ...
Our data raise concerns about the appropriate use of adamantanes and draw attention to the importance of tracking the emergence ... Incidence of Adamantane Resistance Among Influenza A (H3N2) Viruses Isolated Worldwide From 1994 to 2005: A Cause for Concern ... Incidence of Adamantane Resistance Among Influenza A (H3N2) Viruses Isolated Worldwide From 1994 to 2005: A Cause for Concern ... Adamantane Resistance Among Influenza A Viruses Isolated Early During the 2005-2006 Influenza Season in the United States RA ...
  • Adamantane derivatives have found practical application as drugs, polymeric materials, and thermally stable lubricants. (wikipedia.org)
  • Instead of adamantane, Meerwein obtained 1,3,5,7-tetracarbomethoxybicyclo[3.3.1]nonane-2,6-dione: this compound, later named Meerwein's ester, was used in the synthesis of adamantane and its derivatives. (wikipedia.org)
  • Other researchers attempted to synthesize adamantane using phloroglucinol and derivatives of cyclohexanone, but also failed. (wikipedia.org)
  • The method is used to synthesize certain derivatives of adamantane. (wikipedia.org)
  • Petroleum contains more than thirty of derivatives of adamantane. (wikipedia.org)
  • The most widely used drugs have been 2 adamantane derivatives (amantadine and rimantadine), which are effective for prophylaxis and reduce illness duration if started within 48 hours after symptom onset ( 3 , 4 ). (cdc.gov)
  • Those studies are mostly on adamantane derivatives but as you can see from the pictures on Wkipedia, these derivatives are most often nothing more than an addition of a simple group that makes the adamantane more water-soluble. (raypeatforum.com)
  • Many of the studies on those derivatives compared effects of adamantane to the new derivative and found them to be almost the same. (raypeatforum.com)
  • The list of studies is a little light because I wanted to post only the studies known to be directly relevant to adamantane and not its derivatives. (raypeatforum.com)
  • However, all 13 were resistant to adamantane-based drugs (amantadine and rimantadine). (scienceblogs.com)
  • Two classes of antiviral medications are available currently: adamantanes or M2 ion channel inhibitors (i.e., amantadine and rimantadine) and neuraminidase inhibitors (i.e., oseltamivir and zanamivir). (cdc.gov)
  • [13] These findings might also extend to the other adamantanes such as adapromine, rimantadine , and bromantane and could explain the psychostimulant-like effects of this family of compounds . (raypeatforum.com)
  • All the Influenza B are resistant to adamantanes, and in the case of influenza A (H1N1), which inherited an M2 from the swine virus circulating in Europe and Asia, amantadine and rimantadine also have no effect. (bvsalud.org)
  • Beginning in the 2005-2006 influenza season, most strains of influenza A (H3N2) circulating in the US were resistant to adamantanes (amantadine, rimantadine), 121 and resistance to these drugs among seasonal influenza A (H3N2) isolates has remained high during subsequent influenza seasons. (drugs.com)
  • Rimantadine , also called α-methyl-1-adamantane methylamine hydrochloride , drug used to treat infections caused by influenza type A virus , the most common cause of influenza epidemics . (britannica.com)
  • Alexander I Klimov, PhD. Incidence of adamantane resistance among influenza A (H3N2) viruses isolated worldwide from 1994 to 2005: a cause for concern. (alfa.com)
  • Detection of adamantane-sensitive influenza A(H3N2) viruses in Australia, 2017: a cause for hope? (eurosurveillance.org)
  • For over a decade virtually all A(H3N2) influenza viruses have been resistant to the adamantane class of antivirals. (eurosurveillance.org)
  • However, during the 2017 influenza season in Australia, 15/461 (3.3%) adamantane-sensitive A(H3N2) viruses encoding serine at residue 31 of the M2 protein were detected, more than the total number identified globally during the last 6 years. (eurosurveillance.org)
  • A return to wide circulation of adamantane-sensitive A(H3N2) viruses would revive the option of using these drugs for treatment and prophylaxis. (eurosurveillance.org)
  • We identified adamantane resistance in 47% of 152 influenza A virus (H3N2) isolates collected during 2005. (cdc.gov)
  • From 1997 through 2004, few influenza A (H3N2) isolates were resistant to adamantanes, although resistance among isolates from Asia increased substantially in 2003 ( 6 ). (cdc.gov)
  • In the United States, the proportion of influenza A (H3N2) isolates with adamantane resistance was 0.8%-2.2% during this period and 11% in the 2004-05 influenza seasons. (cdc.gov)
  • 90% of influenza A (H3N2) isolates from patients in 26 states contained a mutation conferring resistance to adamantane drugs ( 7 ). (cdc.gov)
  • Ferret models suggest that virulence is not increased by adamantane resistance in influenza A (H3N2) infections ( 8 ), although experimental studies with recombinant influenza (H1N1) in mice have suggested that the mortality rate is increased by a double mutation conferring adamantane resistance ( 9 ). (cdc.gov)
  • This study showed circulating A/ H3N2 viruses was resistant to adamantanes but susceptible to neuraminidase inhibitors. (bvsalud.org)
  • Adamantane molecules can be described as the fusion of three cyclohexane rings. (wikipedia.org)
  • 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)
  • This similarity led to the name adamantane, which is derived from the Greek adamantinos (relating to steel or diamond). (wikipedia.org)
  • Procedures for virus propagation, RNA extraction, and pyrosequencing for adamantane resistance have been described previously ( 4 ). (cdc.gov)
  • The spatial arrangement of carbon atoms in the adamantane molecule is the same as in the diamond crystal. (wikipedia.org)
  • All diamondoids are variants of the adamantane molecule, the most stable among all of the isomers with the formula C 10 H 16 , shown in Fig. 1 . (nature.com)
  • As is often the case in drug discovery and design, a generic molecule like adamantane is modified to be patentable and profitable, but the original molecule usually has the same beneficial effects as the patentable derivative and often without the side effects. (raypeatforum.com)
  • 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)
  • overview of why flu viruses (including the new A/H1N1 strain) are resistant to adamantane , one of the antiviral drugs that can be used to treat influenza infections. (scienceblogs.com)
  • Neither replication, transmission, nor virulence of adamantane-resistant influenza A viruses are impaired by the point mutations conferring resistance ( 5 ). (cdc.gov)
  • A recent report on the global prevalence of adamantane-resistant influenza A viruses indicated a significant increase of drug resistance, from 1.8% during the 2001--02 influenza season to 12.3% during the 2003--04 season ( 4 ). (cdc.gov)
  • Adamantane-resistant influenza A is an emerging problem, but infections caused by resistant and susceptible viruses have not been compared. (cdc.gov)
  • Little is known regarding clinical effects in humans infected with adamantane-resistant influenza viruses. (cdc.gov)
  • 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)
  • This outbreak demonstrates the importance of timely and consistent implementation of infection control measures in controlling influenza outbreaks in long term care facilities and raises questions about a possible role for adamantanes in preventing transmission of adamantane-resistant influenza A viruses. (springer.com)
  • Our data raise concerns about the appropriate use of adamantanes and draw attention to the importance of tracking the emergence and spread of drug-resistant influenza A viruses. (nih.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)
  • 94 Avian influenza A (H5N1) and avian influenza A (H7N9) generally have been resistant to adamantanes. (drugs.com)
  • Resistance to adamantane drugs (which were developed first) has actually become quite widespread among flu viruses in general, so oseltamivir and zanamivir are commonly the drugs of choice. (scienceblogs.com)
  • The adamantanes are active against only influenza A viruses and are used for both treatment and chemoprophylaxis of influenza A, whereas the neuraminidase inhibitors are active against both influenza A and B viruses. (cdc.gov)
  • This report describes new findings regarding the resistance to adamantanes of influenza A viruses currently circulating in the United States and provides interim recommendations that these drugs not be used during the remainder of the 2005--06 influenza season. (cdc.gov)
  • Resistance of influenza A viruses to adamantanes can occur spontaneously or emerge rapidly during treatment ( 3 ). (cdc.gov)
  • During October 1, 2005--January 14, 2006, a total of 123 influenza A viruses collected from 23 states were tested at CDC for adamantane resistance. (cdc.gov)
  • Adamantane resistance among influenza A viruses isolated early during the 2005-2006 influenza season in the United States. (eurosurveillance.org)
  • We sought to assess adamantane resistance among influenza A viruses isolated during the past decade from countries participating in WHO's global influenza surveillance network. (nih.gov)
  • 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. (ac.ir)
  • Overall, 8 out of 11 viruses harbored the adamantane resistance-associated mutations. (ac.ir)
  • In contrast to adamantane resistance, neuraminidase inhibitor resistance remains rare worldwide ( 6 ). (cdc.gov)
  • Adamantanes and neuraminidase inhibitors are influenza antiviral drugs . (bvsalud.org)
  • Pure adamantane is a colorless, crystalline solid with a characteristic camphor smell. (wikipedia.org)
  • Adamantane is a colorless, crystalline chemical compound with a camphor -like odor. (wikipedia.org)
  • The reason for the difference is that the adamantane drugs target different viral proteins from oseltamivir and zanamivir. (scienceblogs.com)
  • The simplest of these polycyclic diamondoids is adamantane followed by its homologues diamantanes, trimantanes, tetramantanes, pentamantanes, and hexamantanes [ 5 ]. (hindawi.com)
  • The discovery of adamantane in petroleum in 1933 launched a new field of chemistry dedicated to the synthesis and properties of polyhedral organic compounds. (wikipedia.org)
  • The adamantane synthesis yield was later increased to 60% and 98% by ultrasound and super acid catalysts. (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)
  • Adamantane is mainly used for the synthesis of medicine to treat influenza, serve as NMDA receptor channel blockers. (alfa.com)
  • 1-Adamantanemethanol is used as a reagent in the synthesis of adamantane and noradamantane based histone deacetylase (HDAC) inhibitors for the treatment of cancer. (hsppharma.com)
  • It is concluded for cases (ii) and (iii), that an adamantane carboxylate anion system with a carbonyl group directly attached at the 3-position is not a suitable model system for studying charge-remote reactions. (edu.au)
  • Adamantane is an organic compound with a formula C10H16 or, more descriptively, (CH)4(CH2)6. (wikipedia.org)
  • Adamantane is the most stable isomer of C10H16. (wikipedia.org)
  • Adamantane has an unusually high melting point for a hydrocarbon. (wikipedia.org)
  • At 270 °C, its melting point is much higher than other hydrocarbons with the same molecular weight, such as camphene (45 °C), limonene (−74 °C), ocimene (50 °C), terpinene (60 °C) or twistane (164 °C), or than a linear C10H22 hydrocarbon decane (−28 °C). However, adamantane slowly sublimes even at room temperature. (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)
  • The first adamantane derivative used as a drug was amantadine - first (1967) as an antiviral drug against various strains of flu[50] and then to treat Parkinson's disease. (raypeatforum.com)
  • 1 2 6 adamantane derivative. (drugs.com)
  • Pd-catalyzed amination of isomeric 2,6-, 2,8-, 4,8- and 4,7-dichloroquinolines was studied using adamantane-containing amines in which substituents at the nitrogen atom differ in bulkiness. (mdpi.com)
  • 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)
  • Amantadine is in a class of medications called adamantanes. (medlineplus.gov)
  • Today, adamantane is an affordable chemical compound with a cost of about $1 a gram. (wikipedia.org)
  • Because of the (assumed) similarity of its structure to that of diamond, the new compound was named adamantane. (wikipedia.org)
  • Phosphatrioxa-adamantane is an organophosphorus compound that is used as a precursor to bulky phosphine ligands. (wikipedia.org)
  • It is composed of an alicyclic compound called adamantane that contains a methyl group (CH 3 ) attached to an amine . (britannica.com)
  • However, following implementation of enhanced infection control practices and adamantane prophylaxis, only 10 (13%) of 79 case patients were identified on the second floor. (springer.com)
  • Enhanced infection control precautions and adamantane prophylaxis were used to control spread of influenza in a chronic care facility. (springer.com)
  • 3. The submitters have found that the absorption of adamantane on silica gel may also be accomplished by mixing the dry solids in a closed flask for a few hours. (orgsyn.org)
  • 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)
  • 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)
  • Electroencephalography (EEG) studies of animals suggest that adapromine and related adamantanes including amantadine, bromantane (1-amino-2-bromophenyladamantane), and memantine have psychostimulant -like and possibly antidepressant -like effects, and that these effects may be mediated via catecholaminergic processes . (raypeatforum.com)
  • Adamantane is the most stable among all the isomers with formula C 10 H 16 , which include the somewhat similar twistane . (wikipedia.org)
  • The adamantanes are a class of compounds that have found use in the treatment of influenza A and Parkinson's disease, among others. (ox.ac.uk)
  • 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)
  • 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)
  • We used molecular-dynamics simulations to calculate the potential of mean force of adamantanes in a lipid bilayer. (ox.ac.uk)
  • These outstanding properties of ADH-based PMO film can be ascribed to lower polarity, lower density, and rigid cavity structure of adamantane, which suggests its potential application as high-performance low- κ material in next-generation microelectronics. (springer.com)
  • In the United States, the frequency of adamantane resistance increased from 1.9% during the 2003--04 influenza season to 11% during the 2004--05 season (CDC, unpublished data, 2005). (cdc.gov)
  • Adamantane consists of four cyclohexanes fused each other in chair conformations. (nanotech-now.com)
  • In this work, we study the fragmentation dynamics of the adamantane dication after ionization by extreme ultraviolet (XUV) femtosecond pulses, the use of which ensures prompt and well-defined ionization. (nature.com)
  • Distribution and dynamics of adamantanes in a lipid bilayer. (ox.ac.uk)
  • Adelaide Research & Scholarship: The search for charge-remote reactions of even-electron anions derived from 1,3-disubstituted adamantanes in the gas phase. (edu.au)