OXAZINES with a fused BENZENE ring.
Six-membered heterocycles containing an oxygen and a nitrogen.
Compounds formed by the joining of smaller, usually repeating, units linked by covalent bonds. These compounds often form large macromolecules (e.g., BIOPOLYMERS; PLASTICS).
A trinitrobenzene derivative with antispasmodic properties that is used primarily as a laboratory reagent.
Toxic, volatile, flammable liquid hydrocarbon byproduct of coal distillation. It is used as an industrial solvent in paints, varnishes, lacquer thinners, gasoline, etc. Benzene causes central nervous system damage acutely and bone marrow damage chronically and is carcinogenic. It was formerly used as parasiticide.
Acrylic acids or acrylates which are substituted in the C-2 position with a methyl group.
Chemical reaction in which monomeric components are combined to form POLYMERS (e.g., POLYMETHYLMETHACRYLATE).
1,2-Dihydro-3,6-pyridazinedione. A herbicide and plant growth regulator; also used to control suckering of tobacco. Its residue in food and tobacco is highly toxic, causing CNS disturbances and liver damage.
Product of the oxidation of ethanol and of the destructive distillation of wood. It is used locally, occasionally internally, as a counterirritant and also as a reagent. (Stedman, 26th ed)
Extensive collections, reputedly complete, of facts and data garnered from material of a specialized subject area and made available for analysis and application. The collection can be automated by various contemporary methods for retrieval. The concept should be differentiated from DATABASES, BIBLIOGRAPHIC which is restricted to collections of bibliographic references.
An organothiophosphorus cholinesterase inhibitor that is used as an insecticide.
Sequential operating programs and data which instruct the functioning of a digital computer.
The major group of transplantation antigens in the mouse.
The study of natural phenomena by observation, measurement, and experimentation.
A nucleoside consisting of the base guanine and the sugar deoxyribose.
A species in the genus PARVOVIRUS that has the ability to replicate and kill tumor cells in culture.
The degree to which individuals are inhibited or facilitated in their ability to gain entry to and to receive care and services from the health care system. Factors influencing this ability include geographic, architectural, transportational, and financial considerations, among others.

Cannabinoid suppression of noxious heat-evoked activity in wide dynamic range neurons in the lumbar dorsal horn of the rat. (1/1038)

The effects of cannabinoid agonists on noxious heat-evoked firing of 62 spinal wide dynamic range (WDR) neurons were examined in urethan-anesthetized rats (1 cell/animal). Noxious thermal stimulation was applied with a Peltier device to the receptive fields in the ipsilateral hindpaw of isolated WDR neurons. To assess the site of action, cannabinoids were administered systemically in intact and spinally transected rats and intraventricularly. Both the aminoalkylindole cannabinoid WIN55,212-2 (125 microg/kg iv) and the bicyclic cannabinoid CP55,940 (125 microg/kg iv) suppressed noxious heat-evoked activity. Responses evoked by mild pressure in nonnociceptive neurons were not altered by CP55,940 (125 microg/kg iv), consistent with previous observations with another cannabinoid agonist, WIN55,212-2. The cannabinoid induced-suppression of noxious heat-evoked activity was blocked by pretreatment with SR141716A (1 mg/kg iv), a competitive antagonist for central cannabinoid CB1 receptors. By contrast, intravenous administration of either vehicle or the receptor-inactive enantiomer WIN55,212-3 (125 microg/kg) failed to alter noxious heat-evoked activity. The suppression of noxious heat-evoked activity induced by WIN55,212-2 in the lumbar dorsal horn of intact animals was markedly attenuated in spinal rats. Moreover, intraventricular administration of WIN55,212-2 suppressed noxious heat-evoked activity in spinal WDR neurons. By contrast, both vehicle and enantiomer were inactive. These findings suggest that cannabinoids selectively modulate the activity of nociceptive neurons in the spinal dorsal horn by actions at CB1 receptors. This modulation represents a suppression of pain neurotransmission because the inhibitory effects are selective for pain-sensitive neurons and are observed with different modalities of noxious stimulation. The data also provide converging lines of evidence for a role for descending antinociceptive mechanisms in cannabinoid modulation of spinal nociceptive processing.  (+info)

Role of a conserved lysine residue in the peripheral cannabinoid receptor (CB2): evidence for subtype specificity. (2/1038)

The human cannabinoid receptors, central cannabinoid receptor (CB1) and peripheral cannabinoid receptor (CB2), share only 44% amino acid identity overall, yet most ligands do not discriminate between receptor subtypes. Site-directed mutagenesis was employed as a means of mapping the ligand recognition site for the human CB2 cannabinoid receptor. A lysine residue in the third transmembrane domain of the CB2 receptor (K109), which is conserved between the CB1 and CB2 receptors, was mutated to alanine or arginine to determine the role of this charged amino acid in receptor function. The analogous mutation in the CB1 receptor (K192A) was found to be crucial for recognition of several cannabinoid compounds excluding (R)-(+)-[2, 3-dihydro-5-methyl-3-[(4-morpholinyl)methyl]pyrrolo[1,2,3-de]-1, 4-benzoxazin-6-yl](1-naphthalenyl)methanone (WIN 55,212-2). In contrast, in human embryonic kidney (HEK)-293 cells expressing the mutant or wild-type CB2 receptors, we found no significant differences in either the binding profile of several cannabinoid ligands nor in inhibition of cAMP accumulation. We identified a high-affinity site for (-)-3-[2-hydroxyl-4-(1, 1-dimethylheptyl)phenyl]-4-[3-hydroxyl propyl] cyclohexan-1-ol (CP-55,940) in the region of helices 3, 6, and 7, with S3.31(112), T3.35(116), and N7.49(295) in the K109A mutant using molecular modeling. The serine residue, unique to the CB2 receptor, was then mutated to glycine in the K109A mutant. This double mutant, K109AS112G, retains the ability to bind aminoalkylindoles but loses affinity for classical cannabinoids, as predicted by the molecular model. Distinct cellular localization of the mutant receptors observed with immunofluorescence also suggests differences in receptor function. In summary, we identified amino acid residues in the CB2 receptor that could lead to subtype specificity.  (+info)

Effect of the cannabinoid receptor agonist WIN55212-2 on sympathetic cardiovascular regulation. (3/1038)

1. The aim of the present study was to analyse the cardiovascular actions of the synthetic CB1/CB2 cannabinoid receptor agonist WIN55212-2, and specifically to determine its sites of action on sympathetic cardiovascular regulation. 2. Pithed rabbits in which the sympathetic outflow was continuously stimulated electrically or which received a pressor infusion of noradrenaline were used to study peripheral prejunctional and direct vascular effects, respectively. For studying effects on brain stem cardiovascular regulatory centres, drugs were administered into the cisterna cerebellomedullaris in conscious rabbits. Overall cardiovascular effects of the cannabinoid were studied in conscious rabbits with intravenous drug administration. 3. In pithed rabbits in which the sympathetic outflow was continuously electrically stimulated, intravenous injection of WIN55212-2 (5, 50 and 500 microg kg(-1)) markedly reduced blood pressure, the spillover of noradrenaline into plasma and the plasma noradrenaline concentration, and these effects were antagonized by the CB1 cannabinoid receptor-selective antagonist SR141716A. The hypotensive and the sympathoinhibitory effect of WIN55212-2 was shared by CP55940, another mixed CB1/CB2 cannabinoid receptor agonist, but not by WIN55212-3, the enantiomer of WIN55212-2, which lacks affinity for cannabinoid binding sites. WIN55212-2 had no effect on vascular tone established by infusion of noradrenaline in pithed rabbits. 4. Intracisternal application of WIN55212-2 (0.1, 1 and 10 microg kg(-1)) in conscious rabbits increased blood pressure and the plasma noradrenaline concentration and elicited bradycardia; this latter effect was antagonized by atropine. 5. In conscious animals, intravenous injection of WIN55212-2 (5 and 50 microg kg(-1)) caused bradycardia, slight hypotension, no change in the plasma noradrenaline concentration, and an increase in renal sympathetic nerve firing. The highest dose of WIN55212-2 (500 microg kg(-1)) elicited hypotension and tachycardia, and sympathetic nerve activity and the plasma noradrenaline concentration declined. 6. The results obtained in pithed rabbits indicate that activation of CB1 cannabinoid receptors leads to marked peripheral prejunctional inhibition of noradrenaline release from postganglionic sympathetic axons. Intracisternal application of WIN55212-2 uncovered two effects on brain stem cardiovascular centres: sympathoexcitation and activation of cardiac vagal fibres. The highest dose of systemically administered WIN55212-2 produced central sympathoinhibition; the primary site of this action is not known.  (+info)

Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656, and AM630. (4/1038)

We have tested our prediction that AM630 is a CB2 cannabinoid receptor ligand and also investigated whether L759633 and L759656, are CB2 receptor agonists. Binding assays with membranes from CHO cells stably transfected with human CB1 or CB2 receptors using [3H]-CP55940, confirmed the CB2-selectivity of L759633 and L759656 (CB2/CB1 affinity ratios = 163 and 414 respectively) and showed AM630 to have a Ki at CB2 receptors of 31.2 nM and a CB2/CB1 affinity ratio of 165. In CB2-transfected cells, L759633 and L759656 were potent inhibitors of forskolin-stimulated cyclic AMP production, with EC50 values of 8.1 and 3.1 nM respectively and CB1/CB2 EC50 ratios of > 1000 and > 3000 respectively. AM630 inhibited [35S]-GTPgammaS binding to CB2 receptor membranes (EC50 = 76.6 nM), enhanced forskolin-stimulated cyclic AMP production in CB2-transfected cells (5.2 fold by 1 microM), and antagonized the inhibition of forskolin-stimulated cyclic AMP production in this cell line induced by CP55940. In CB1-transfected cells, forskolin-stimulated cyclic AMP production was significantly inhibited by AM630 (22.6% at 1 microM and 45.9% at 10 microM) and by L759633 at 10 microM (48%) but not 1 microM. L759656 (10 microM) was not inhibitory. AM630 also produced a slight decrease in the mean inhibitory effect of CP55940 on cyclic AMP production which was not statistically significant. We conclude that AM630 is a CB2-selective ligand that behaves as an inverse agonist at CB2 receptors and as a weak partial agonist at CB1 receptors. L759633 and L759656 are both potent CB2-selective agonists.  (+info)

Cannabinoids and neuroprotection in global and focal cerebral ischemia and in neuronal cultures. (5/1038)

Marijuana and related drugs (cannabinoids) have been proposed as treatments for a widening spectrum of medical disorders. R(+)-[2, 3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1, 4-benzoxazin-yl]-(1-naphthalenyl)methanone mesylate (R(+)-WIN 55212-2), a synthetic cannabinoid agonist, decreased hippocampal neuronal loss after transient global cerebral ischemia and reduced infarct volume after permanent focal cerebral ischemia induced by middle cerebral artery occlusion in rats. The less active enantiomer S(-)-WIN 55212-3 was ineffective, and the protective effect of R(+)-WIN 55212-2 was blocked by the specific central cannabinoid (CB1) cannabinoid receptor antagonist N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2, 4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide-hydrochloride. R(+)-WIN 55212-2 also protected cultured cerebral cortical neurons from in vitro hypoxia and glucose deprivation, but in contrast to the receptor-mediated neuroprotection observed in vivo, this in vitro effect was not stereoselective and was insensitive to CB1 and CB2 receptor antagonists. Cannabinoids may have therapeutic potential in disorders resulting from cerebral ischemia, including stroke, and may protect neurons from injury through a variety of mechanisms.  (+info)

Involvement of CB1 cannabinoid receptors in the EDHF-dependent vasorelaxation in rabbits. (6/1038)

1. It was recently suggested that an endogenous cannabinoid could represent an endothelium-derived hyperpolarizing factor (EDHF). The aim of the present study was to clarify whether CB1 cannabinoid receptors are involved in the nitric oxide (NO)- and prostanoid-independent vasodilation produced by acetylcholine in rabbits. 2. Pithed rabbits received indomethacin. Noradrenaline was infused to raise blood pressure, and vasodilation was elicited by bolus injections of acetylcholine. The NO-synthase inhibitor Nomega-nitro-L-arginine methylester inhibited the acetylcholine-evoked vasodilation by about 40%. The remaining vasodilation was unaffected by the CB1 cannabinoid receptor antagonist SR141716A, but was inhibited by the potassium channel blocker tetraethylammonium. In addition, the mixed CB1/CB2 cannabinoid receptor agonist WIN55212-2 did not elicit vasodilation. 3. No CB1 cannabinoid receptors were involved in the prostanoid- and NO-independent vasodilation produced by acetylcholine. An exogenous cannabinoid also did not cause vasodilation. Therefore, it is unlikely that an endogenous cannabinoid serves as an EDHF acting at smooth muscle CB1 cannabinoid receptors in the rabbit.  (+info)

Distinct domains of the CB1 cannabinoid receptor mediate desensitization and internalization. (7/1038)

Desensitization of cannabinoid receptor signaling by a G-protein coupled receptor kinase (GRK) was examined using the Xenopus oocyte expression system. Application of a CB1 agonist, WIN 55,212-2, evoked a concentration-dependent increase in K+ conductance (Kir3) in oocytes coexpressing rat CB1 with the G-protein-gated, inwardly rectifying K+ channels Kir3.1 and Kir3.4. Desensitization was slight during continuous agonist application in the absence of GRK and arrestin. However, coexpression of GRK3 and beta-arrestin 2 (beta-arr2) caused profound homologous CB1 receptor desensitization, supporting the hypothesis that GRK3 and beta-arr2 effectively produce CB1 receptor desensitization. To identify the regions of the CB1 receptor responsible for GRK3- and beta-arr2-mediated desensitization, we constructed several CB1 receptor mutants. Truncation of the C-terminal tail of CB1 receptor at residue 418 (Delta418) almost completely abolished desensitization but did not affect agonist activation of Kir3. In contrast, truncation at residues 439 and 460 did not significantly affect GRK3- and beta-arr2-dependent desensitization. A deletion mutant (Delta418-439) did not desensitize, indicating that residues within this region are important for GRK3- and beta-arr2-mediated desensitization. Phosphorylation in this region was likely involved in desensitization, because mutation of either of two putative phosphorylation sites (S426A or S430A) significantly attenuated desensitization. CB1 receptors rapidly internalize after activation by agonist. Phosphorylation of S426 or S430 was not necessary for internalization, because the S426A/S430A CB1 mutant internalized when stably expressed in AtT20 cells. These studies establish that CB1 desensitization can be regulated by a GRK and that different receptor domains are involved in GRK- and beta-arrestin-dependent desensitization and CB1 internalization.  (+info)

Cannabinoid CB1 receptor of cat cerebral arterial muscle functions to inhibit L-type Ca2+ channel current. (8/1038)

The CB1 subtype of the cannabinoid receptor is present on neurons in the brain and mediates the perceptual effects of Delta9-tetrahydrocannabinol and other cannabinoids. We found that cat cerebral arterial smooth muscle cells (VSMC) contain the protein for the CB1 receptor and express a cDNA that has >98% amino acid homology to the CB1 cDNA expressed in rat and human neurons. Activation of the CB1 cannabinoid receptor has been shown to decrease the opening of N-type voltage-gated Ca2+ channels in neurons through a pertussis toxin-sensitive GTP-binding protein. In the present study we tested the hypothesis that activation of the cannabinoid CB1 receptor in cerebral VSMC inhibits voltage-gated Ca2+ channels and results in cerebral vasodilation. The predominant Ca2+ current identified in cat cerebral VSMC is a voltage-gated, dihydropyridine-sensitive, L-type Ca2+ current. The cannabimimetic drug WIN-55,212-2 (10-100 nM) induced concentration-dependent inhibition of peak L-type Ca2+ current, which reached a maximum of 82 +/- 4% at 100 nM (n = 14). This effect was mimicked by the putative endogenous CB1-receptor agonist anandamide, which produced a concentration-related reduction of peak L-type Ca2+ current with a maximum inhibition (at 300 nM) of 39 +/- 4% (n = 12). The inhibitory effects of both ligands on peak L-type Ca2+ currents were abolished by pertussis toxin pretreatment and application of the CB1-receptor antagonist SR-141716A (100 nM, n = 5). Both WIN-55,212-2 and anandamide produced concentration-dependent relaxation of preconstricted cerebral arterial segments that was abolished by SR-141716A. These results indicate that the CB1 receptor is expressed in cat cerebral VSMC and that the cerebral vasculature is one of the targets for endogenous cannabinoids. These findings suggest that the CB1 receptor and its endogenous ligand may play a fundamental role in the regulation of cerebral arterial tone and reactivity by modulating the influx of Ca2+ through L-type Ca2+ channels.  (+info)

ABSTRACT: to determine the effect of a rifampicin-containing tuberculosis regimen on efavirenz plasma concentrations and viral load in HIV/AIDS-Tuberculosis infection patients who received efavirenz-based antiretroviral therapy. Methods: plasma efavirenz concentrations and HIV viral load were measured in HIV/AIDS patients treated with 600 mg efavirenz-based antiretroviral for 3 to 6 months and in HIV/AIDS-Tuberculosis infection patients treated with similar antiretroviral regimen plus rifampicin-containing antituberculosis in Sulianti Saroso Infectious disease Hospital, Jakarta. Plasma efavirenz concentration in both groups were compared using Mann-Whitney test, while proportion of patients with viral load ,40 copy/mL were analyzed with chi-square test. Results: forty fve patients (27 with HIV/AIDS and 18 with HIV/AIDS-Tuberculosis infections) were recruited during the period of February to May 2015. The median efavirenz plasma concentration obtained from HIV/AIDS group was 0,680 mg/L(range 0,24 ...
McGee, KC, Shahmanesh, M, Boothby, M, Nightingale, P, Gathercole, LL, Tripathi, G, Harte, AL, Shojaee-Moradie, F, Umpleby, AM, Das, S et al, Al-Daghri, NM, McTernan, PG and Tomlinson, JW. (2012) Evidence for a shift to anaerobic metabolism in adipose tissue in efavirenz-containing regimens for HIV with different nucleoside backbones. ...
Efavirenz primary and secondary metabolism was investigated in vitro and in vivo. In human liver microsome (HLM) samples, 7- and 8-hydroxyefavirenz accounted for 22.5 and 77.5% of the overall efavirenz metabolism, respectively. Kinetic, inhibition, and correlation analyses in HLM samples and experiments in expressed cytochrome P450 show that CYP2A6 is the principal catalyst of efavirenz 7-hydroxylation. Although CYP2B6 was the main enzyme catalyzing efavirenz 8-hydroxylation, CYP2A6 also seems to contribute. Both 7- and 8-hydroxyefavirenz were further oxidized to novel dihydroxylated metabolite(s) primarily by CYP2B6. These dihydroxylated metabolite(s) were not the same as 8,14-dihydroxyefavirenz, a metabolite that has been suggested to be directly formed via 14-hydroxylation of 8-hydroxyefavirenz, because 8,14-dihydroxyefavirenz was not detected in vitro when efavirenz, 7-, or 8-hydroxyefavirenz were used as substrates. Efavirenz and its primary and secondary metabolites that were identified in ...
Primary Health Care Clinics). Health and Training Consultant. Session locum at Potchefstroom Provincial Hospital Pharmacogenetics and Pharmacokinetics of Antiretroviral drugs Pharmacogenetics and Pharmacokinetics of Antiretroviral drugs 6. Publications (List publications over the last three years) Viljoen, M. Loots, DT. Rheeders, M. Gous, HS. Routine drug level monitoring of first line ARV regimen in a South African paediatric HIV roll-out clinic. The Canadian Journal of Clinical Pharmacology, 2008 15 (3):e753. Viljoen M, Gous H, Kruger HS, Riddick A, Meyers TM, Rheeders M. Efavirenz Plasma Concentrations at 1, 3 and 6 Months Post Antiretroviral Therapy Initiation in HIV-1 Infected South African Children. Aids Research and Human Retroviruses, 2010 26(6): Viljoen, M. Meyer, CL. Lubbe, MS. The prevalence of side- effects: Ciprofloxacin 500 mg single dose prophylaxis against Neisseria Meningitidis outbreak in Potchefstroom during July 2003. Health SA Gesondheid: 2004 9 (3):42-54. 7. Papers ...
AIMS This study aimed to test whether a pharmacokinetic simulation model could extrapolate nonclinical drug data to predict human efavirenz exposure after single and continuous dosing as well as the effects of concomitant rifampicin and further to evaluate the weight-based dosage recommendations used to counteract the rifampicin-efavirenz interaction. METHODS Efavirenz pharmacokinetics were simulated using a physiologically based pharmacokinetic model implemented in the Simcyp™ population-based simulator. Physicochemical and metabolism data obtained from the literature were used as input for prediction of pharmacokinetic parameters. The model was used to simulate the effects of rifampicin on efavirenz pharmacokinetics in 400 virtual patients, taking into account bodyweight and CYP2B6 phenotype. RESULTS Apart from the absorption phase, the simulation model predicted efavirenz concentration-time profiles reasonably well, with close agreement with clinical data. The simulated effects of ...
The major new findings of the present study were that CYP2A6-mediated efavirenz 7-hydroxylation accounts for ∼23% of efavirenz metabolism; CYP2A6 is a partial contributor toward efavirenz 8-hydroxylation; efavirenz is metabolized sequentially to novel dihydroxylated metabolite(s), via CYP2B6-mediated 7- and 8-hydroxyefavirenz hydroxylation as intermediary; and 8,14-dihydroxyefavirenz is formed in vivo but not in vitro, suggesting novel metabolic reactions and challenging previous notion that it is formed through direct 14-hydroxylation of 8-hydroxyefavirenz (Mutlib et al., 1999b; Ward et al., 2003). The identification and quantification of all the efavirenz primary (7- and 8-hydroxyefavirenz) and secondary (8,14-dihydroxyefavirenz and a dihydroxylated) metabolites and the first demonstration of their full pharmacokinetics in plasma of healthy subject taking a single 600-mg oral dose of efavirenz confirm clinical relevance of the in vitro findings. Finally, the role CYP2B6 plays in efavirenz ...
In previously untreated patients, combinations that include efavirenz compare favorably with regimens that include either other nonnucleoside reverse transcriptase inhibitors or components from other antiretroviral classes.. Two parallel randomized, placebo-controlled Phase III studies in antiretroviral-naive adults compared efavirenz with rilpivirine, each in combination with 2 NRTIs (predominantly tenofovir + emtricitabine). By ITT analysis of pooled data from the 2 studies, 82% of efavirenz recipients and 84% of rilpivirine recipients had HIV RNA levels of ,50 copies/mL at 48 weeks; the difference was not statistically significant. In patients with HIV RNA ,100,000 copies/mL, the efavirenz regimen resulted in higher rates of virologic suppression. The mean increase in CD4 count was 176 cells/µL in the efavirenz group (compared with 192 cells/µL in the rilpivirine group).(13) A randomized trial comparing efavirenz with nevirapine, each given with lamivudine + stavudine in initial therapy, ...
The primary objective of this study is to compare the effectiveness of EFV-based regimens in HIV-1-infected patients who; (1) were previously allergic to NVP and stopped all ARV simultaneously; (2) were previously allergic to NVP and continued the other NRTIs for a period of time, i.e. staggered interruption; and (3) started EFV-based regimens as an initial regimen (as controlled group ...
Maraviroc (MVC) is a CCR5 antagonist that prevents virus entry blocking the binding of R5-tropic HIV to the cell surface CCR5 co-receptor. The MERIT Study compared MVC with EFV, each with a Combivir backbone, as initial therapy. Using a non-inferiority margin of 10% MVC was non-inferior to EFV using the ,400 copies/ml viral load cut-off but failed to reach non-inferiority when a ,50 copies/ml analysis was used. Since this study was performed a more sensitive tropism assay has become routinely available and a re-analysis of the MERIT results showed that some of the patients with apparent R5-tropic virus actually had non-R5 virus. When these patients were excluded from the analysis, MVC did achieve non-inferiority compared to efavirenz. Of note, a subanalysis in the original MERIT Study of individuals with a baseline viral load below 100,000 copies/ml demonstrated only a small numerical difference between MVC and EFV recipients with 69.6% and 71.6% respectively achieving a viral load less than 50 ...
Efavirenz is a synthetic non-nucleoside reverse transcriptase (RT) inhibitor with antiviral activity. Buy Reverse Transcriptase inhibitor Efavirenz (Sustiva, Stocrin, DMP-266, DMP 266) from AbMole BioScience.
TY - JOUR. T1 - A single-nucleotide polymorphism in CYP2B6 leads to ,3-fold increases in efavirenz concentrations in plasma and hair among HIV-infected women. AU - Gandhi, Monica. AU - Greenblatt, Ruth M.. AU - Bacchetti, Peter. AU - Jin, Chengshi. AU - Huang, Yong. AU - Anastos, Kathryn. AU - Cohen, Mardge. AU - Dehovitz, Jack A.. AU - Sharp, Gerald B.. AU - Gange, Stephen J.. AU - Liu, Chenglong. AU - Hanson, Susan C.. AU - Aouizerat, Bradley. PY - 2012/11/1. Y1 - 2012/11/1. N2 - Background. Efavirenz exhibits marked interindividual variability in plasma levels and toxicities. Prior pharmacogenetic studies usually measure exposure via single plasma levels, examine limited numbers of polymorphisms, and rarely model multiple contributors. We analyzed numerous genetic and nongenetic factors impacting short-term and long-term exposure in a large heterogeneous population of human immunodeficiency virus (HIV)-infected women. Methods. We performed 24-hour intensive pharmacokinetic studies in 111 ...
Authors: Lotfi, L. , Javadpour, J. , Naimi-Jamal, M.R. Article Type: Research Article Abstract: Introduction: The biological and mechanical properties of substances are relevant to their application as biomaterials and there are many efforts to enhance biocompatibility and mechanical properties of bio-medical materials. Objectives: In this study, to achieve a low rate of shrinkage during polymerization, good mechanical properties, and excellent biocompatibility, benzoxazine based composites were synthesized. Methods: Benzoxazine monomer was synthesized using a solventless method. FTIR and DSC analysis were carried out to determine the appropriate polymerization temperature. The low viscosity of the benzoxazine monomer at 70°C attract us to use in situ polymerization after high speed ball milling …of the benzoxazine and it mixture with different weight fractions of zirconia particles. Dispersion and adhesion between the ceramic and polymer components were evaluate by SEM. To evaluate the ...
Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI). It works by lowering the amount of HIV in the blood. Efavirenz will not cure or prevent HIV infection or AIDS, however, it helps keep HIV from reproducing and appears to slow down the destruction of the immune system. This may help delay the development of problems that usually result from AIDS or HIV disease. Efavirenz will not keep you from spreading HIV to other people. People who receive this medicine may continue to have some of the problems usually related to AIDS or HIV disease. This medicine is available only with your doctors prescription. This product is available in the following dosage forms:. ...
Buy Efavirenz Online! Efavirenz is available in capsule and tablet formulations. For pediatric patients and adults who cannot swallow pills, the contents of Efavirenz capsules may be sprinkled on a small amount of food (1-2 teaspoons) or infant formula.
For patients with HIV-1 RNA concentrations of fewer than 100 000 copies per mL at baseline, of those receiving cabotegravir, 43 (88%) of 49 in the 60 mg group, 40 (75%) of 53 in the 30 mg group, and 37 (71%) of 52 in the 10 mg group had sustained viral suppression after 72 weeks of maintenance therapy (week 96), compared with 32 (59%) of 54 patients receiving efavirenz. For patients who had a high viral load (HIV-1 RNA of at least 100 000 copies per mL) at baseline, of those receiving cabotegravir, eight (67%) of 12 in the 60 mg group, five (71%) of seven in the 30 mg group, and four (50%) of eight in the 10 mg group had sustained viral suppression at 72 weeks, compared with seven (88%) of eight patients in the efavirenz group. Patients in the cabotegravir groups with a high viral load were discontinued for both viral and non-viral reasons. Two of the patients discontinued had viral loads of greater than 2 million copies per mL at baseline and were not eligible to enter the maintenance phase at ...
To understand how structurally distinct ligands regulate CB1 receptor interactions with Gi1, Gi2, and Gi3, we quantified the Gαi and βγ proteins that coimmunoprecipitate with the CB1 receptor from a detergent extract of N18TG2 membranes in the presence of ligands. A mixture of A, R, GGDP (or G_), and ARGGDP (or ARG_) complexes was observed in the presence of aminoalkylindole (R)-(+)-[2,3-dihydro-5-methyl-3-(4-morpholinylmethyl)pyrrolo[1,2,3-de]-1,4-benzoxazin-6-yl]-1-naphthalenylmethanone (WIN 55,212-2) for all three RGαi complexes, cannabinoid desacetyllevonantradol for Gαi1 and Gαi2, and eicosanoid (R)-methanandamide for Gαi3. Desacetyllevonantradol maintained RGαi3 complexes and (R)-methanandamide maintained RGαi1 and RGαi2 complexes even in the presence of a nonhydrolyzable GTP analog. The biaryl pyrazole antagonist N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboximide hydrochloride (SR141716) maintained all three RGαi complexes. Gβ ...
Efavirenz (zaščiteni imeni Sustiva in Stocrin) je protivirusna učinkovina iz skupine nenukleozidnih zaviralcev reverzne transkriptaze (NNRTI), ki se uporablja kot del visokoaktivnega protiretrovirusnega zdravljenja (HAART) pri okužbah z virusom HIV (tipa 1). Efavirenz se v kombinaciji z drugimi protiretrovirusnimi zdravili uporablja tudi pri zaščiti po izpostavljenosti za zmanjšanje tveganja za okužbo pri posameznikih, ki so bili izpostavljeni visokemu tveganju za okužbo z virusom HIV (npr. vbod z injekcijsko iglo, nekatere oblike nezaščitenega spolnega odnosa ...). Na trgu je tudi kombinirana tableta, ki vsebuje poleg efavirenza še emtricitabin in tenofovir (zaščiteno ime je Atripla) in predstavlja celotno HAART-zdravljenje v obliki ene tablete, ki se jemlje enkrat dnevno. FDA je zdravilo odobrila julija 2006. ...
Thanks for your post. Efavirenz (one of the medications in Atripla) can be taken with or without food without impact to effectiveness. When taken with food, efavirenz levels can increase in some...
You are viewing an interactive 3D depiction of the molecule (2s)-2,4-dihydroxy-7-methoxy-2h-1,4-benzoxazin-3(4h)-one (C9H9NO5) from the PQR.
This study investigated changes in lipid profile, efficacy, safety and tolerability when switching from Efavirenz based regimen to Rilpivirine based regimen in
DuPont Pharmaceuticals new drug efavirenz (Sustiva) has enjoyed a favored position among treatment activists, offering both high levels of antiviral ...
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PubMed Central Canada (PMC Canada) provides free access to a stable and permanent online digital archive of full-text, peer-reviewed health and life sciences research publications. It builds on PubMed Central (PMC), the U.S. National Institutes of Health (NIH) free digital archive of biomedical and life sciences journal literature and is a member of the broader PMC International (PMCI) network of e-repositories.
In pregnancies with prospectively reported exposure to efavirenz-based regimens in the Antiretroviral Pregnancy Registry through January 2017 birth defects were observed in 22 of 978 live births with first-trimester exposure (2.2%, 95% CI, 1.4% to 3.4%).10 Although these data provide sufficient numbers of first-trimester exposures to rule out a 2-fold or greater increase in the risk of overall birth defects, the low incidence of neural tube defects in the general population means that a larger number of exposures are still needed to be able to definitively rule out an increased risk of this specific defect. Prospective reports to the Antiretroviral Pregnancy Registry of defects after first-trimester efavirenz exposure have documented one neural tube defect case (sacral aplasia, myelomeningocele, and hydrocephalus with fetal alcohol syndrome) and one case of bilateral facial clefts, anophthalmia, and amniotic band. An undefined abnormality of the cerebral vermis was seen on ultrasound and ...
Efavirenz causes central nervous system adverse effects (CNS AEs) including sleep disturbance, somnolence, vivid dreams and others. The relation between efavirenz clearance and CNS AEs has been unclear, particularly when stratified by race. P450 (CYP) isoenzyme 2B6 G516T confers slower metabolism and is more common with African origin. We hypothesized that this allele and additional CYP polymorphisms that affect efavirenz clearance mediate CNS AEs.. We included 842 HIV infected adults initiating efavirenz + 2 nucleoside analog reverse transcriptase inhibitors in a cohort study in Botswana. DNA was genotyped for 21 variants in CYP 2B6, 2A6, 3A4, and 3A5 genes and mid-dose EFV plasma samples were collected at 1 month of therapy. AEs were measured using 21 CNS symptoms in the ACTG Subject Experience Questionnaire. We used a one-compartment population PK model with nonlinear mixed effect modeling in NONMEM 7 to estimate EFV clearance, including the fixed covariates of allometrically scaled weight, ...
A research collaboration between the Desmond Tutu HIV Centre and Harvard University (Orrell, abstract 0113) reported resistance patterns among 230 patients (120 treatment na ve; 110 treatment experienced) receiving care in Cape Town, South Africa. Among the treatment naive individuals transmission of drug resistance was low (estimated at 2.5%). Among those failing first line ART treatment, rates of resistance were high. Failure was defined as HIV RNA > 1000 copies on two successive occasions. Seventy-three percent of patients were receiving an efavirenz-based regimen, and 89% were taking stavudine. Treatment limiting NNRTI mutations (K103N, Y181C, and V106M) were noted in 83%. Most had 2 or fewer NNRTI mutations. NRTI resistance mutations were frequent, with M184V being present in 78%. Surprisingly, and of great concern, the K65R mutation was noted in 9.5% of those failing first line therapy. All had received stavudine, and none had received tenofovir as part of their ART regimen. The selection ...
Researchers in the College of Arts and Sciences have determined that cannabinoid drugs do not appear to reduce the intensity of experimental pain, but, instead, may make pain feel less unpleasant and more tolerable.
Efavirenz (EFV) 600mg is currently recommended by WHO as a first-line antiretroviral agent in HIV infected adults. A dose reduction to 400mg EFV has been proposed because of concerns regarding toxicitity. EFV is widely used during pregnancy in those countries where HIV infection is most common. Pregnancy can reduce exposure to antiretroviral agents with a corresponding risk of poor maternal virologic control and PMTCT. Pharmacokinetics (PK) of EFV 600 mg have been previously studied in pregnancy with contradictory results. The aim of this multinetwork study was to further investigate the PK of EFV 600 mg in pregnant women.. HIV-infected pregnant women treated with EFV 600 mg once daily were recruited by the P1026s network (N=10) and PANNA network (N=13). Intensive PK profiles were obtained during 2nd (2T) and 3rd trimester (3T) and at least two weeks postpartum (PP). 2T and 3T PK parameters were compared with PP. Where possible cord blood and maternal delivery blood samples were ...
Synthetic cannabinoids - drugs that mimic the psychoactive effect of cannabis - have been linked to injuries and deaths. When one is banned, another rises to take its place.
Patients with a history of psychiatric disorders may be at increased risk of developing these psychiatric-type adverse events with a range of frequencies ranging from 0.3% for manic reactions to 2.0% for both depression and depression. severe and suicidal ideation. Post-marketing surveillance of suicide deaths, delusions and psychotic-type behavior has also been reported.. Symptoms affecting the nervous system : In controlled clinical trials, commonly reported adverse reactions include, but are not limited to, dizziness, insomnia, drowsiness, impaired concentration, and dream disturbance. Nervous systemic symptoms of moderate to severe intensity were observed in 19% (2% of whom were severe) of patients receiving efavirenz compared to 9% (1% of whom were severe) of patients receiving control regimens. In clinical studies, 2% of patients treated with efavirenz discontinued treatment due to such symptoms.. These usually appear during the first two days of treatment and often disappear after 2 to 4 ...
Die Diagnose wird durch Refraktions- bestimmung gestellt. Allen PM, Rodhakrishnan H, OвLeary DJ Repeatability and validity of the PowerRefractor and the Nidek AR600-A in efavirenz rifampicina adult population with healthy eyes, Optom Vis Sci 80245-51, Efavirenz rifampicina. Citalopram A 70-year-old woman, who had been taking citalopram 10 mgday for 3 years for depression, began taking tramadol 50 mgday) for pain relief and rapidly devel- efaavirenz tremor, restlessness, fever, and confusion (121). J.
This handbook provides a wide overview of the field, fundamental understanding of the synthetic methods and structure/property correlation, as well as studies related to applications in a wide range of subjects.
This handbook provides a wide overview of the field, fundamental understanding of the synthetic methods and structure/property correlation, as well as studies related to applications in a wide range of subjects.
2-(dibutylamino)-4H-3,1-benzoxazin-4-one - chemical structural formula, chemical names, chemical properties, synthesis references
Structure, properties, spectra, suppliers and links for: 2-(3-Hydroxyphenyl)-3-(4-morpholinylmethyl)-2H-thieno[3,2-e][1,2]thiazine-6-sulfonamide 1,1-diox.
This study will evaluate the effects of genetics on metabolism of the anti-HIV medicine efavirenz (Sustiva) and will see if Efavirenz interacts with bupropion (Zyban or Wellbutrin), a drug commonly used to treat depression and to help people quit smoking. Efavirenz is metabolized by an enzyme called CYP2B6, which is thought to be more active in some people than in others, depending on their genetic makeup. The rate of metabolism of the drug can affect how the body responds it and perhaps the ability of the HIV virus to develop resistance to it. Healthy volunteers between 18 and 55 years of age who are non-smokers and HIV-infected men and women 18 years of age and older who are taking efavirenz along with two or three nucleoside reverse transcriptase inhibitors may be eligible for this study. Candidates are screened with a medical history and physical examination and blood tests, including tests to determine which genes they have for four different proteins or enzymes (CYP2B6, CYP3A4, CYP3A5, and ...
The possibility for neurologic conditions in children more than doubles when the mothers antiretroviral regimen includes efavirenz, suggests a new study flagging the teratogenicity of the drug.
This study assessed the pharmacokinetics, efficacy and safety of maraviroc administered to HIV-infected individuals switching from efavirenz -containing
Easy to read patient leaflet for Sustiva (Efavirenz Tablets). Includes indications, proper use, special instructions, precautions, and possible side effects.
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Background: Consistent long-term viral suppression has been difficult to achieve in children with human immunodeficiency virus type 1 (HIV-1) infection. We tested the safety and antiviral efficacy of a novel combination consisting of efavirenz, nelfinavir, and one or more nucleoside reverse-transcriptase inhibitors in 57 children previously treated with only nucleoside reverse-transcriptase inhibitors. Methods: The children were monitored for 48 weeks after the initiation of therapy. We assessed plasma concentrations of efavirenz and nelfinavir, plasma HIV-1 RNA levels, and lymphocyte subpopulations. Results: At base line, the 57 HIV-1â€infected children (age range, 3.8 to 16.8 years) had a median of 699 CD4 cells per cubic millimeter and 10,000 copies of HIV-1 RNA per milliliter of plasma. The most common treatment-related effects of at least moderate severity were rash (in 30 percent of children), diarrhea (in 18 percent), neutropenia (in 12 percent), and biochemical abnormalities (in 12 ...
Information on antiretroviral dosing errors among health care providers for outpatient human immunodeficiency virus (HIV)-infected patients is lacking. We evaluated factors associated with nucleoside reverse-transcriptase inhibitor dosing errors in a university-based HIV clinic using an electronic medical record. Overall, older age, minority race or ethnicity, and didanosine use were related to such errors. Impaired renal function was more common in older patients and racial or ethnic minorities and, in conjunction with fixed-dose combination drugs, contributed to the higher rates of errors in nucleoside reverse-transcriptase inhibitor dosing. Understanding the factors related to nucleoside reverse-transcriptase inhibitor dosing errors is an important step in the building of preventive tools.
With this in mind, investigators in Spain designed an open-label, multicentre, randomised study to assess the impact on liver steatosis over 48 weeks of switching from efavirenz to raltegravir while maintaining a stable nucleoside reverse transcriptase inhibitor (NRTI) backbone (emtricitabine/tenofovir or lamivudine/abacavir).. The study population consisted of 39 individuals with hepatic steatosis, all with a suppressed viral load and evidence of significant liver steatosis. A total of 19 were randomised to switch to raltegravir, the other 20 remaining on efavirenz. Approximately three-quarters of the participants taking raltegravir and two-thirds of those treated with efavirenz had detectable HCV viral load. People with active drug/alcohol abuse were excluded from participation.. Changes in liver steatosis were assessed by transient elastography (Fibroscan), which measures liver stiffness and fat accumulation in the liver. Liver fat is calculated by measuring the controlled attenuation ...
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BioAssay record AID 541841 submitted by ChEMBL: Inhibition of CYP2B6 in human liver microsomes assessed as 8-hydroxyefavirenz 14-hydroxylation after 10 mins.
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efavirenz-containing regimens, most of which were In March 2005, Bristol-Myers Squibb and the FDA first-trimester exposures. Birth defects occurred in notified healthcare professionals of revisions of the five of 188 live births with first-trimester exposure, prescribing information for efavirenz. The pregnancy and in zero of 13 live births with second- or third- category for the drug has changed from category C trimester exposure. None of these prospectively re- (risk of fetal harm cannot be ruled out) to category ported defects were neural tube defects. However, D (positive evidence of fetal risk). This change is a there have been four retrospective reports (i.e. after result of four retrospective reports of neural tube the results of the pregnancy were known) of findings defects in infants born to women with first-trimester consistent with neural tube defects, including three exposure to efavirenz, including three cases of me- cases of meningomyelocele. Al four mothers were ningomyelocele and ...
The organic/inorganic hybrid materials from polyhedral oligomeric silsesquioxane (POSS, inorganic nanoparticles) and polybenzoxazine (PBZ) have received much interesting recently due to their excellent thermal and mechanical properties, flame retardance, low dielectric constant, well-defined inorganic framework at nanosized scale level, and higher performance relative to those of non-hybrid PBZs. This review describes the synthesis, dielectric constants, and thermal, rheological, and mechanical properties of covalently bonded mono- and multifunctionalized benzoxazine POSS hybrids, other functionalized benzoxazine POSS derivatives, and non-covalently (hydrogen) bonded benzoxazine POSS composites.
Concomitant amiodarone: not recommended; if no alternatives, monitor cardiac function (see full labeling). Concomitant certain immunosuppressants or chemotherapeutic agents: may increase risk of HBV reactivation. May potentiate P-gp, BCRP, OATP1B1, OATP1B3, or OATP2B1 substrates. Concomitant BCRP substrates (eg, methotrexate, mitoxantrone, imatinib, irinotecan, lapatinib, rosuvastatin, sulfasalazine, topotecan): not recommended. Concomitant P-gp and/or moderate to potent CYP2B6, CYP2C8, CYP3A4 inducers (eg, St. Johns wort, carbamazepine), anticonvulsants (eg, phenytoin, phenobarbital, oxcarbazepine), rifabutin, rifapentine, tipranavir/ritonavir, atazanavir-, lopinavir-, or efavirenz-containing regimens, OATP inhibitors (eg, cyclosporine): not recommended. Separate dosing of antacids by 4hrs. May give H2-antagonists simultaneously or staggered from Vosevi (at a dose that does not exceed doses comparable with famotidine 40mg twice daily). May coadminister with omeprazole 20mg. May potentiate ...
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The spectrum of anti-HIV drugs was recently extended by a new class of drugs, the integrase inhibitors. The first drug of this class that received FDA approval is Raltegravir. Clinical data show that when previously untreated patients start treatment on Raltegravir, their viral load declines more rapidly than it does in patients who take instead the reverse-transcriptase inhibitor Efavirenz. This spring, Antiviral Therapy published a modeling study by [http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2980788/ Sedaghat et al.] that discusses the possible mechanisms responsible for this accelerated decline in viral load. The study argues that the accelerated decline is likely not caused by greater antiviral efficiency of Raltegravir compared to Efavirenz. Instead, because Raltegravir acts later in the viral life cycle than Efavirenz, at the beginning of Raltegravir therapy fewer cells have progressed to a state where the drug can not inhibit virus production, and hence the viral load declines faster. ...
The spectrum of anti-HIV drugs was recently extended by a new class of drugs, the integrase inhibitors. The first drug of this class that received FDA approval is Raltegravir. Clinical data show that when previously untreated patients start treatment on Raltegravir, their viral load declines more rapidly than it does in patients who take instead the reverse-transcriptase inhibitor Efavirenz. This spring, Antiviral Therapy published a modeling study by [http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2980788/ Sedaghat et al.] that discusses the possible mechanisms responsible for this accelerated decline in viral load. The study argues that the accelerated decline is likely not caused by greater antiviral efficiency of Raltegravir compared to Efavirenz. Instead, because Raltegravir acts later in the viral life cycle than Efavirenz, at the beginning of Raltegravir therapy fewer cells have progressed to a state where the drug can not inhibit virus production, and hence the viral load declines faster. ...
Atripla tablets contain three active ingredients, efavirenz, emtricitabine and tenofovir. These three medicines are used in the treatment of HIV infection.
This page contains information on the chemical 3-Pyridinecarboxylic acid, 2-(2H-1,4-benzoxazin-3-yl)hydrazide including: 2 synonyms/identifiers.
A general protocol for the synthesis of 3,1-benzoxazin-2-ones 18 from 3-hydroxyoxindoles 16 in a two steps sequence through phenylsuccinates or phenylpropionates 17 is described. Best reaction conditions for ring opening of 16 to succinates or propionates17 were achieved using alcohol/silica gel, while cyclization of 17 to benzoxazinones 18 was easily done with HCl/alcohol. It was also found that 17 and 18 can be transesterified using HCl/alcohol. Most transformations were carried out by traditional heating and by microwave (MW) irradiation to accelerate reaction rates. ...
Tanaproget (NSP-989) is a novel nonsteroidal progesterone receptor agonist which can bind to the PR from various species with a higher relative affinity than reference steroidal progestins. - Mechanism of Action & Protocol.
Camber Pharmaceuticals, Inc.: Efavirenz tablets in combination with other antiretroviral agents is indicated for the treatment of human immunodeficiency virus...
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Advisors to the US Food and Drug Administration has recommended approval of Boehringer Ingelheims chronic obstructive pulmonary disease drug olodaterol. - News - PharmaTimes
Johns Hopkins study suggests the commonly prescribed anti-retroviral drug efavirenz attacks brain cells The way the body metabolizes a commonly prescribed anti-retroviral drug that is used long term by patients infected with HIV may contribute to cognitive impairment by damaging nerve cells, a new Johns Hopkins research suggests. Nearly 50 percent of people infected with HIV will eventually develop some form of brain damage that, while mild, can affect the ability to drive, work or participate in many daily activities. It has long been assumed that the disease was causing the damage, but Hopkins researchers say the drug efavirenz may play a key role. People infected with HIV typically take a cocktail of medications to suppress the virus, and many will take the drugs for decades. Efavirenz is known to be very good at controlling the virus and is one of the few that crosses the blood-brain barrier and can target potential reservoirs of virus in the brain. Doctors have long believed that it might ...
(4-Methyl-1-naphthalenyl)(2-methyl-1-pentyl-1H-indol-3-yl)methanone | C26H27NO | CID 45267820 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
XLR-12 is an indole-based synthetic cannabinoid drug that was invented by Abbott Laboratories in 2006.[1] It is an analogue of XLR-11 where the 5-fluoropentyl chain has been replaced with a 4,4,4-trifluorobutyl chain. XLR-12 is relatively highly selective for the CB2 receptor, with a Ki of 0.09 nM and 167x selectivity over the related CB1 receptor, however it still retains appreciable affinity for CB1 with a Ki of 15 nM.[2] ...
... s, also called benzoxazine resins, are cured polymerization products derived from benzoxazine monomers. ... The systematic IUPAC name of the prototypical unsubstituted monomer is 3,4-dihydro-3-phenyl-2H-1,3-benzoxazine. Benzoxazines ... Benzoxazines can be prepared by a one-pot process by heating an aromatic amine, a phenol and formaldehyde. Alternatively, they ... Handbook of Benzoxazine Resins, ed. Hatsuo Ishida And Tarek Agag, Elsevier B.V., 2011, ISBN 978-0-444-53790-4 Free Polymer ...
Bernardi L, Coda S, Bonsignori A, Pegrassi L, Suchowsky GK (August 1969). "Central depressant properties of 3,1-benzoxazine ... 3-benzoxazine". Experientia. 24 (8): 774-5. doi:10.1007/bf02144859. PMID 5683159. S2CID 30917127. ...
3-benzoxazine-1,4-dione, II), and N-hydroxyphthalimide (III). It was not until the 1950s that Cohn's product was definitely ...
5-methyl-3-(4-methylpiperazin-1-yl)pyridazino[3,4-b][1,4]benzoxazine ...
Starr KR, Price GW, Watson JM, Atkinson PJ, Arban R, Melotto S, Dawson LA, Hagan JJ, Upton N, Duxon MS (2007). "SB-649915-B, a novel 5-HT1A/B autoreceptor antagonist and serotonin reuptake inhibitor, is anxiolytic and displays fast onset activity in the rat high light social interaction test". Neuropsychopharmacology. 32 (10): 2163-2172. doi:10.1038/sj.npp.1301341. PMID 17356576 ...
... benzoxazine based composites were synthesized. Methods: Benzoxazine monomer was synthesized using a solventless method. FTIR ... The low viscosity of the benzoxazine monomer at 70°C attract us to use in situ polymerization after high speed ball milling …of ... the benzoxazine and it mixture with different weight fractions of zirconia particles. Dispersion and adhesion between the ...
There are several benzoxazine derivatives depending on the position of the oxygen and nitrogen in the ring. Benzoxazine is used ... Benzoxazine is composed of an oxazine ring, a heterocyclic aromatic six-membered ring with oxygen and nitrogen, attached to a ... There are several benzoxazine derivatives depending on the position of the oxygen and nitrogen in the ring. Benzoxazine is used ... benzoxazine-. 7-. sulfonyl chloride AldrichCPR C8H5Cl2NO4S * pricing ...
Aside from the synthesis and characterization of such multifunctional benzoxazines, reactivity and polymerization behavior is ... Comparing the polymerization processes and resulting structures, the trifunctional benzoxazine derivative enter new ... 3-benzoxazines derived from phenol-, resorcinol-, and phloroglucinol give monomers with one, two, and three oxazine units at a ... at the benzene ring yielding the lowest polymerization temperature for the trifunctional phloroglucinol-based benzoxazine. ...
... Wu Ke,1 Wang Rumin,1 and Zeng ... Wu Ke, Wang Rumin, and Zeng Jinfang, "Curing Kinetics of Hybrid Networks Composed of Benzoxazine and Multifunctional Novolac ...
... which is attributed to the benzoxazine-benzoxazine reaction and epoxy-benzoxazine system reaction takes place at nearly the ... On the other hand, the reaction time of epoxy-benzoxazine system is higher than that of benzoxazine homopolymer; the difference ... Epoxy-benzoxazine system ratio is 1 : 1, and there was only one peak in the plot. The reactive mechanism of the F-51/BZ mixture ... Curing Kinetics of Hybrid Networks Composed of Benzoxazine and Multifunctional Novolac Epoxy. Wu Ke,1 Wang Rumin,1 and Zeng ...
Use of this information is subject to copyright laws and may require the permission of the owner of the information, as described in the ECHA Legal Notice.. ...
A novel benzoxazine/epoxy blend with multiphase structure†. Pei Zhao , Qian Zhou , Yuyuan Deng , Rongqi Zhu and Yi Gu * College ... C. Jubsilp, T. Takeichi and S. Rimdusit, in Handbook of Benzoxazine Resins, ed. H. Ishida and T. Agag, Elsevier, Amsterdam, 1nd ... A novel benzoxazine (BOZ)/epoxy resin (ER) blend with multiphase structure was successfully prepared under the catalysis of ... Due to their prominent processability and excellent thermal and mechanical properties, epoxy (ER) modified benzoxazine (BOZ) ...
... which is quite different from that of normal benzoxazine. The theoretical calculations matched reasonably well with the ... A multifunctional benzoxazine monomer (BZCN) was synthesized, which has several outstanding properties, such as high thermal ... measurements were used to determine the kinetic parameters and the kinetic models of the curing processes of benzoxazine ... A multifunctional benzoxazine monomer (BZCN) was synthesized, which has several outstanding properties, such as high thermal ...
Benzoxazines are reported to exhibit antiinflammatory [1,2], analgesic [3], antibacterial [4,5], neuroprotective [6], D2 ... Benzoxazine and benzoxazinone based compounds (fig. 1) forms an important class of benzfuzed heterocyles with wide spectrum of ... Waisser K, Perina M, Kunes J, Klimesova V, Kaustova J. 3-Benzyl-2H-1,3-benzoxazine-2,4(3H)-diones, a new group of ... Antiinflammatory, antimicrobial, oxazines, 1,3- benzoxazine. Research and development of potent and effective antimicrobial ...
"Benzoxazines" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH (Medical Subject ... This graph shows the total number of publications written about "Benzoxazines" by people in this website by year, and whether " ... Below are the most recent publications written about "Benzoxazines" by people in Profiles. ...
A new RTM system based on a novel benzoxazine/epoxy chemistry has been developed and is in the final phase of commercial ... This is supported by the fact that benzoxazine chemistry has very low moisture absorption characteristics. The overall ... Huntsman Presents New RTM System Based on Benzoxazine Chemistry. 11 June 2004 ...
8,8-Methylene bis-(6-chloro-3,4-dihydro-3-phenyl-2h, 1,3-benzoxazine). *Formula: C29H24Cl2N2O2 ...
3-Benzoxazine-3(4H)-acetic acid, 2-oxo-, hydrazide including: 3 synonyms/identifiers. ... 2-Oxo-2H-1,3-benzoxazine-3(4H)-acetic acid hydrazide*2H-1,3-Benzoxazine-3(4H)-acetic acid, 2-oxo-, hydrazide Related Resources ... 2H-1,3-Benzoxazine-3(4H)-acetic acid, 2-oxo-, hydrazide. Identifications. *CAS Number: 18464-44-3*Synonyms/Related:* ... Chemical Database - 2H-1,3-Benzoxazine-3(4H)-acetic acid, 2-oxo-, hydrazide. EnvironmentalChemistry.com. 1995 - 2018. Accessed ...
... benzoxazine imide), NDOPoda Bz, through the reaction of a difunctional naphthalene dianhydride ortho-phenol (ND-ortho-phenol), ... This new poly(benzoxazine imide) underwent cross-linking polymerization to form a highly cross-linked poly(benzoxazine imide), ... Direct synthesis of poly(benzoxazine imide) from an ortho-benzoxazine: its thermal conversion to highly cross-linked ... Direct synthesis of poly(benzoxazine imide) from an ortho-benzoxazine: its thermal conversion to highly cross-linked ...
1-benzoxazine-1(4H)-acetate , C18H16ClNO4 , CID 215291 - structure, chemical names, physical and chemical properties, ...
Susceptible to nucleophilic attack, normally at the "acid" 4-carbon. More hindered nucleophiles attack at the "carbamate" 2-carbon. In the presence of DMAP, attack is directed to C-4, giving anthranilic acid derivatives: Synthesis, 266 (1982). For reviews of the chemistry of isatoic anhydrides, including reactions with a wide range of nucleophiles and the formation of a variety of heterocyclic systems, see: Synthesis, 505 (1980); Adv. Heterocycl Chem., 28, 127 (1981). /n. ...
... benzoxazine]-2-one; trifluoroacetic acid; CAS Number: 2361643-55-0; find Enamine-ENAH5802F400 MSDS, related peer-reviewed ... Home > ENAH5802F400 6-methyl-1,2-dihydrospiro[azetidine-3,4-[3,1]benzoxazine]-2-one; trifluoroacetic acid ... 6-methyl-1,2-dihydrospiro[azetidine-3,4-[3,1]benzoxazine]-2-one; trifluoroacetic acid. ...
H27198 6-Methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazine-4-propionitrile, 97% ...
Physical and Chemical Properties of Benzoxazine Resins. 2. Synthesis of benzoxazines in solutions and melt (H. Ishida, and Jin- ... Study of a cardanol-based benzoxazine as reactive diluent and toughening agent of conventional benzoxazines (P. Campaner, D. ... 8. Electrochemical polymerization of benzoxazines (Wei Chen). 9. Light Induced Reactions of Benzoxazines (M.At. Tasdelen, B. ... Handbook of Benzoxazine Resins. Author: Edited By Hatsuo Ishida & Tarek Agag ISBN 978-0-444-53790-4. Published: 2011 712 pages ...
Suraj R, Radhamani S, Meehan-Andrews T, Bradley C (2017) Role of a novel benzoxazine derivative in the chemosensitization of ... Inhibition of AKT signalling by benzoxazine derivative LTUR6 through the modulation of downstream kinases. ...
关键字:Full bio-based benzoxazine, Synthesis, Low-temperature curing performance, Thermal stability. 论文来源:期刊. 具体来源:Polymer, 2020.5 ... Novel full bio-based phloroglucin benzoxazine resin: Synthesis, curing reaction and thermal stability ... aniline benzoxazine (BA-a), P-fa and P-paba monomers showed a different curing reaction process and excellent low temperature ... as amine source and paraformaldehyde were selected to synthesize two novel full bio-based benzoxazine resin (3,7,11-tris(furan- ...
Study of the Complexation of a New Crown-containing Benzoxazine Spiropyran with Metal Cations. ...
3-benzoxazine - C15H16N2O, synthesis, structure, density, melting point, boiling point ...
Polybenzoxazines, also called benzoxazine resins, are cured polymerization products derived from benzoxazine monomers. ... The systematic IUPAC name of the prototypical unsubstituted monomer is 3,4-dihydro-3-phenyl-2H-1,3-benzoxazine. Benzoxazines ... Benzoxazines can be prepared by a one-pot process by heating an aromatic amine, a phenol and formaldehyde. Alternatively, they ... Handbook of Benzoxazine Resins, ed. Hatsuo Ishida And Tarek Agag, Elsevier B.V., 2011, ISBN 978-0-444-53790-4 Free Polymer ...
Bernardi L, Coda S, Bonsignori A, Pegrassi L, Suchowsky GK (August 1969). "Central depressant properties of 3,1-benzoxazine ... 3-benzoxazine". Experientia. 24 (8): 774-5. doi:10.1007/bf02144859. PMID 5683159. S2CID 30917127. ...
... benzoxazine-7-sulfonamide, 1-(4-methyl-1-piperazinyl)-N,N,10-trimethyl- - Similar structures search, synonyms, formulas, ... Substance Name: 1OH-Pyridazino(4,5-b)(1,4)benzoxazine-7-sulfonamide, 1-(4-methyl-1-piperazinyl)-N,N,10-trimethyl-. RN: 64610-60 ... 1OH-Pyridazino(4,5-b)(1,4)benzoxazine-7-sulfonamide, 1-(4-methyl-1-piperazinyl)-N,N,10-trimethyl- ...
0075] Preferred N-alkyl benzoxazine compounds and/or preferred N-alkenyl benzoxazine compounds are embraced by benzoxazine ... benzoxazine nitrogen atom. [0073] The term "N-alkenyl benzoxazine compound" as used herein refers to any benzoxazine compound ... and/or N-alkenyl benzoxazine compounds. [0072] The term "N-alkyl benzoxazine compound" as used herein refers to any benzoxazine ... benzoxazines and monofunctional benzoxazines, or combinations of one or more multifunctional benzoxazines or one or more ...
Prediction : 6-methoxy-1h-31-benzoxazine-24-quinone - albumin. Your feedback has been submited, thank you! ...
Prediction : 44-diethyl-2-2-pyridyl-12-dihydro-31-benzoxazine - albumin. Your feedback has been submited, thank you! ...
3-Benzoxazine-3(4H)-acetic acid, 2-oxo-, hydrazide - Similar structures search, synonyms, formulas, resource links, and other ... Substance Name: 2H-1,3-Benzoxazine-3(4H)-acetic acid, 2-oxo-, hydrazide. RN: 18464-44-3. InChIKey: WPLZQLUEIFERRQ-UHFFFAOYSA-N ...
  • 3,4-dihydro-3-phenyl-2H-1,3-benzoxazines derived from phenol-, resorcinol-, and phloroglucinol give monomers with one, two, and three oxazine units at a single benzene ring, respectively. (mdpi.com)
  • Polybenzoxazines, also called benzoxazine resins, are cured polymerization products derived from benzoxazine monomers. (wikipedia.org)
  • Benzoxazines can be homopolymerized to yield rigid materials, or can be copolymerized with other monomers to tune properties. (wikipedia.org)
  • The result of heating up benzoxazine monomers is a high molecular weight thermoset polymer matrix. (wikipedia.org)
  • The development of polybenzoxazines has always been linked to petro-based feedstocks, but for the last 5 years, the number of studies related to bio-based benzoxazines is exploding as a consequence of the versatility of the design of the chemical structure of their monomers. (intechopen.com)
  • Benzoxazine (Bz) monomers are subjected to cationic ring-opening polymerization (ROP), activated by a thermal treatment in the range of 160-250°C. In addition, Bz synthesis promotes the use of naturally occurring phenolic compounds instead of petroleum-based ones to develop high-performance materials from renewable resources and to fit to REACH restrictions. (intechopen.com)
  • In this chapter, the synthesis and the properties of di-functional benzoxazine monomers prepared from naturally occurring phenolic compounds are reviewed. (intechopen.com)
  • Aside from the synthesis and characterization of such multifunctional benzoxazines, reactivity and polymerization behavior is studied in dependence of the oxazine functionality. (mdpi.com)
  • This paper describes a facile one-pot synthesis of a poly(benzoxazine imide), NDOPoda Bz, through the reaction of a difunctional naphthalene dianhydride ortho -phenol (ND- ortho -phenol), paraformaldehyde, and 4,4′-oxydianiline in 1,4-dioxane, without the need for either the preparation of an amino-functionalized benzoxazine or subsequent thermal treatment. (rsc.org)
  • Benzoxazine is used in polymers, resins, and cross-linking agents due to its favorable thermal and chemical resistance, electrical properties, and design flexibility. (sigmaaldrich.com)
  • Benzoxazines are products of condensation between an amine, a phenol and formaldehyde, used to produce thermoset resins or thermosetting polymer. (wikipedia.org)
  • Advanced and Emerging Polybenzoxazine Science and Technology introduces advanced topics of benzoxazine resins and polybenzoxazines as presented through the collaboration of leading experts in the benzoxazine community, representing the authoritative introduction to the subjects. (researchandmarkets.com)
  • The last part of the chapter is dedicated to the use of bio-phenols to functionalize polymers and to provide benzoxazine functional groups. (intechopen.com)
  • A novel hybrid network composed of benzoxazines (BZ) and novolac epoxy resin (F-51) was prepared successfully. (hindawi.com)
  • Recently, many authors have investigated the copolymerization of benzoxazine resin with epoxy resin to increase the cross-linking density and glass-transition temperature and through this have gained plentiful and substantial achievements [ 8 , 20 - 22 ]. (hindawi.com)
  • 23 ]. However, the curing kinetic of benzoxazine-novolac epoxy resin hybrid networks by isothermal differential scanning calorimetry is scarce. (hindawi.com)
  • A novel benzoxazine (BOZ)/epoxy resin (ER) blend with multiphase structure was successfully prepared under the catalysis of imidazole (MZ) via reaction-induced phase separation. (rsc.org)
  • Aromatic diamine-phenol-based benzoxazine (BOZ) resin based on 4,4′-diaminodiphenyl methane (DDM), phenol and paraformaldehyde was synthesized and characterized as previous reports. (rsc.org)
  • Benzoxazine precursors were synthesized using 4-hydroxybenzaldehyde as phenolic component, paraformaldehyde, and two different functional polyetheramines. (aiche.org)
  • Benzoxazine and benzoxazinone based compounds ( fig. 1 ) forms an important class of benzfuzed heterocyles with wide spectrum of biological activities and are in the development phase as potential new drugs. (ijpsonline.com)
  • Benzoxazines are bicyclic heterocyclic compounds containing one oxygen and one nitrogen atom in a doubly unsaturated six-member ring, specifically a 1,3-oxazine ring, fused with a benzene ring. (wikipedia.org)
  • The present invention relates to a curable composition, comprising specific meta-substituted aromatic compounds and at least one benzoxazine compound. (patentsencyclopedia.com)
  • In particular, the invention relates to the use of said meta-substituted aromatic compounds as curatives/catalysts for benzoxazine-containing compositions. (patentsencyclopedia.com)
  • 7. The curable composition of claim 1, wherein the benzoxazine compound is selected from the group consisting of N-alkyl and/or N-alkenyl benzoxazine compounds. (patentsencyclopedia.com)
  • b) subjecting the polymerizable composition to conditions appropriate to polymerize the polymerizable composition, wherein the polymerizable composition comprises at least one benzoxazine compound, preferably selected from the group consisting of N-alkyl and N-alkenyl benzoxazine compounds. (patentsencyclopedia.com)
  • 16. Use of at least one meta-substituted aromatic compound a) as defined in claim 1 as a curative for polymerizable compositions, comprising at least one benzoxazine compound, preferably selected from the group consisting of N-alkyl and/or N-alkenyl benzoxazine compounds. (patentsencyclopedia.com)
  • The curing kinetic of benzoxazine-epoxy hybrid networks by nonisothermal differential scanning calorimetry was noted by Jubsilp et al. (hindawi.com)
  • To better understand the curing kinetics of BZCN, isothermal differential scanning calorimetry measurements were used to determine the kinetic parameters and the kinetic models of the curing processes of benzoxazine monomer with cyano functionality. (scientific.net)
  • The effect of graphene oxide on the ring-opening polymerization of benzoxazine was also evaluated using differential scanning calorimetry (DSC). (aiche.org)
  • There are several benzoxazine derivatives depending on the position of the oxygen and nitrogen in the ring. (sigmaaldrich.com)
  • Benzoxazine derivatives of phytophenols show anti-plasmodial activity via sodium homeostasis disruption. (nih.gov)
  • W. J. Chen and X. B. Liu, "Curing Kinetics of Cyano Functionalized Benzoxazine", Advanced Materials Research, Vols. (scientific.net)
  • No volatile release during cure Viscosities as low as 1000 cP at processing temperatures Near zero shrinkage Room temperature storage stability Gel times of as short as 17 minutes at 155 °C Good hydrophobicity Gel temperature Tg at 140 - 250 °C or higher Excellent electrical properties (low dielectric constant and dissipation factors) Good chemical resistance Thermosetting polymer Thermoset polymer matrix Plastic "Huntsman benzoxazine brochure, "High-Performance Materials for Extreme Environments"" (PDF). (wikipedia.org)
  • Comparing the polymerization processes and resulting structures, the trifunctional benzoxazine derivative enter new polymerization pathways, which include methylene linkages bridging aniline units, as well as the formation of carbonyl-derived structures. (mdpi.com)
  • Background: In this study, antimicrobial effect of total extract of Tribulus terrestris L. and its fraction containing Benzoxazine derivative ( Terresoxazine ) was studied for the first time in Iran. (sid.ir)
  • Liquid chromatography-mass spectrometry (LC/MS) system proved the existence of Benzoxazine derivative in the water and the third fractions. (sid.ir)
  • Conclusion: Because of antibacterial effects of Tribulus terrestris L. against both Gram negative and positive bacteria, and no antibacterial effect of the fraction containing Benzoxazine derivative, it can be concluded that antibacterial effects of the total extract is due to other active ingredients or it is because of the cumulating of different components in total extract. (sid.ir)
  • Benzoxazine is composed of an oxazine ring, a heterocyclic aromatic six-membered ring with oxygen and nitrogen, attached to a benzene ring. (sigmaaldrich.com)
  • Benzoxazines can be prepared by a one-pot process by heating an aromatic amine, a phenol and formaldehyde. (wikipedia.org)
  • The present invention provides a crosslinking agent having reactive benzoxazine groups that is the ungelled reaction product of (a) at least one mono-hydroxy aromatic compound and (b) at least one aminotriazine compound having one or les. (sumobrain.com)
  • This is supported by the fact that benzoxazine chemistry has very low moisture absorption characteristics. (netcomposites.com)
  • Broad topics covered include the recent development and improved understanding of the subjects, including low temperature cure, aerogels and carbon aerogels, smart chemistry in fire retarding materials and coatings, metal containing benzoxazines, rational design of advanced properties, and materials from natural renew. (researchandmarkets.com)
  • Monomer reactivities are directly related to the number of oxazine functionalities present at the benzene ring yielding the lowest polymerization temperature for the trifunctional phloroglucinol-based benzoxazine. (mdpi.com)
  • A multifunctional benzoxazine monomer (BZCN) was synthesized, which has several outstanding properties, such as high thermal stability and high glass transition. (scientific.net)
  • The systematic IUPAC name of the prototypical unsubstituted monomer is 3,4-dihydro-3-phenyl-2H-1,3-benzoxazine. (wikipedia.org)
  • Koschek, K. Multifunctional Benzoxazines Feature Low Polymerization Temperature and Diverse Polymer Structures. (mdpi.com)
  • Low-Dissipation Thermosets Derived from Oligo(2,6-Dimethyl Phenylene Oxide)-Containing Benzoxazines. (nih.gov)
  • Additional tables on key NMR and FTIR frequencies unique to benzoxazine, heat of polymerization, Tg, and char yield will greatly aid in the choice of proper benzoxazine for a specific application. (chemtec.org)
  • Abstract In this article, a new synthetic approach for the modification of partial glycerides (PG) obtained from sunflower oil with thermally curable benzoxazine units and its potential use as a coating material are described. (thefreedictionary.com)
  • A crosslinking agent having reactive benzoxazine groups is provided. (sumobrain.com)
  • The chemical structures of the benzoxazine precursors were confirmed by nuclear magnetic resonance spectroscopy ( 1 H-NMR) and (FT-IR).The morphological, surface, and thermal properties of the aerogels obtained were examined and compared with the neat polybenzoxazine aerogels. (aiche.org)
  • Benzoxazine film formation by thermally induced destabilization of benzoxazine nanodroplets. (mpg.de)
  • Benzoxazines (BZ) can be prepared by the Mannich-like condensation of different types of phenol, formaldehyde, and an amine, by employing either solution or solventless methods, so the molecular structure of BZ offers enormous design flexibility. (hindawi.com)
  • Currently supervising a PhD student (Maryam Sairi, sponsored by the Malaysian Government) on predicting the char yield of Benzoxazines by QSPR. (surrey.ac.uk)
  • mol -1 and the total order of reaction is 1.84, which is quite different from that of normal benzoxazine. (scientific.net)
  • Because of the wide availability and low-cost of starting materials (amines, phenols and formaldehyde), as well as ease of preparation (one-pot reaction) diverse benzoxazines are available. (wikipedia.org)
  • 19. The photochromic article of claim 18 wherein the organic photochromic substance is selected from the group consisting of spiro(indoline)naphthoxazines, spiro(indoline)benzoxazines, benzopyrans, naphthopyrans, chromenes, organo-metal dithizonates, fulgides and fulgimides and mixtures of such organic photochromic substances. (google.com)
  • Due to their prominent processability and excellent thermal and mechanical properties, epoxy (ER) modified benzoxazine (BOZ) blending systems have attracted more and more attention in a wide range of application areas, including adhesives, filler-reinforced composite materials, and coatings for electronic circuits. (rsc.org)
  • This new poly(benzoxazine imide) underwent cross-linking polymerization to form a highly cross-linked poly(benzoxazine imide), which, with additional thermal treatment, was converted to highly cross-linked polybenzoxazoles. (rsc.org)
  • In addition, this approach decreased the temperature for ring opening of the benzoxazine, accelerated the rate of benzoxazole ring formation of NDOPda Bz at a lower temperature, and improved the thermal stability of the formed polybenzoxazoles. (rsc.org)
  • Curing of benzoxazines takes place by thermal ring-opening polymerisation with or without catalyst. (wikipedia.org)
  • Benzoxazines" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (umassmed.edu)
  • Numerous research focus on the different curing temperature, and polymer properties, such as cross-linking, from benzoxazines derived from substituted phenols. (wikipedia.org)
  • The peak for NCH 2 and OCH 2 groups of oxazine ring was observed from δ 3.87-4.6 and δ 4.95-5.51 ppm, respectively confirming the formation of benzoxazine ring. (ijpsonline.com)