Benzoxazines: OXAZINES with a fused BENZENE ring.Oxazines: Six-membered heterocycles containing an oxygen and a nitrogen.Polymers: Compounds formed by the joining of smaller, usually repeating, units linked by covalent bonds. These compounds often form large macromolecules (e.g., BIOPOLYMERS; PLASTICS).Phloroglucinol: A trinitrobenzene derivative with antispasmodic properties that is used primarily as a laboratory reagent.Benzene: 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.Methacrylates: Acrylic acids or acrylates which are substituted in the C-2 position with a methyl group.Polymerization: Chemical reaction in which monomeric components are combined to form POLYMERS (e.g., POLYMETHYLMETHACRYLATE).Maleic Hydrazide: 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.Acetic Acid: 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)HydrazinesDatabases, Factual: 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.Fonofos: An organothiophosphorus cholinesterase inhibitor that is used as an insecticide.Software: Sequential operating programs and data which instruct the functioning of a digital computer.H-2 Antigens: The major group of transplantation antigens in the mouse.Science: The study of natural phenomena by observation, measurement, and experimentation.Deoxyguanosine: A nucleoside consisting of the base guanine and the sugar deoxyribose.H-1 parvovirus: A species in the genus PARVOVIRUS that has the ability to replicate and kill tumor cells in culture.Health Services Accessibility: 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.Great BritainEthylene Glycols: An ethylene compound with two hydroxy groups (-OH) located on adjacent carbons. They are viscous and colorless liquids. Some are used as anesthetics or hypnotics. However, the class is best known for their use as a coolant or antifreeze.Carbonates: Salts or ions of the theoretical carbonic acid, containing the radical CO2(3-). Carbonates are readily decomposed by acids. The carbonates of the alkali metals are water-soluble; all others are insoluble. (From Grant & Hackh's Chemical Dictionary, 5th ed)Calcium Carbonate: Carbonic acid calcium salt (CaCO3). An odorless, tasteless powder or crystal that occurs in nature. It is used therapeutically as a phosphate buffer in hemodialysis patients and as a calcium supplement.Allyl CompoundsDrug Contamination: The presence of organisms, or any foreign material that makes a drug preparation impure.United States Dept. of Health and Human Services: A cabinet department in the Executive Branch of the United States Government concerned with administering those agencies and offices having programs pertaining to health and human services.Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.National Institutes of Health (U.S.): An operating division of the US Department of Health and Human Services. It is concerned with the overall planning, promoting, and administering of programs pertaining to health and medical research. Until 1995, it was an agency of the United States PUBLIC HEALTH SERVICE.Anti-HIV Agents: Agents used to treat AIDS and/or stop the spread of the HIV infection. These do not include drugs used to treat symptoms or opportunistic infections associated with AIDS.Acquired Immunodeficiency Syndrome: An acquired defect of cellular immunity associated with infection by the human immunodeficiency virus (HIV), a CD4-positive T-lymphocyte count under 200 cells/microliter or less than 14% of total lymphocytes, and increased susceptibility to opportunistic infections and malignant neoplasms. Clinical manifestations also include emaciation (wasting) and dementia. These elements reflect criteria for AIDS as defined by the CDC in 1993.HIV Infections: Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).Clinical Trials as Topic: Works about pre-planned studies of the safety, efficacy, or optimum dosage schedule (if appropriate) of one or more diagnostic, therapeutic, or prophylactic drugs, devices, or techniques selected according to predetermined criteria of eligibility and observed for predefined evidence of favorable and unfavorable effects. This concept includes clinical trials conducted both in the U.S. and in other countries.PyransSpiro Compounds: A group of compounds consisting in part of two rings sharing one atom (usually a carbon) in common.Structure-Activity Relationship: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.Heterocyclic Compounds: Ring compounds having atoms other than carbon in their nuclei. (Grant & Hackh's Chemical Dictionary, 5th ed)Nitro Compounds: Compounds having the nitro group, -NO2, attached to carbon. When attached to nitrogen they are nitramines and attached to oxygen they are NITRATES.Eye Protective Devices: Personal devices for protection of the eyes from impact, flying objects, glare, liquids, or injurious radiation.PhotochemistryPatents as Topic: Exclusive legal rights or privileges applied to inventions, plants, etc.Microwaves: That portion of the electromagnetic spectrum from the UHF (ultrahigh frequency) radio waves and extending into the INFRARED RAYS frequencies.InkSolvents: Liquids that dissolve other substances (solutes), generally solids, without any change in chemical composition, as, water containing sugar. (Grant & Hackh's Chemical Dictionary, 5th ed)Inventions: A novel composition, device, or process, independently conceived de novo or derived from a pre-existing model.Intellectual Property: Property, such as patents, trademarks, and copyright, that results from creative effort. The Patent and Copyright Clause (Art. 1, Sec. 8, cl. 8) of the United States Constitution provides for promoting the progress of science and useful arts by securing for limited times to authors and inventors, the exclusive right to their respective writings and discoveries. (From Black's Law Dictionary, 5th ed, p1014)Foramen Ovale, Patent: A condition in which the FORAMEN OVALE in the ATRIAL SEPTUM fails to close shortly after birth. This results in abnormal communications between the two upper chambers of the heart. An isolated patent ovale foramen without other structural heart defects is usually of no hemodynamic significance.Epoxy Resins: Polymeric resins derived from OXIRANES and characterized by strength and thermosetting properties. Epoxy resins are often used as dental materials.Anhydrides: Chemical compounds derived from acids by the elimination of a molecule of water.Phthalic Anhydrides: Phthalic acid anhydrides. Can be substituted on any carbon atom. Used extensively in industry and as a reagent in the acylation of amino- and hydroxyl groups.Maleic Anhydrides: Used in copolymerization reactions, in the Diels-Alder(diene)synthesis, in the preparation of resins, pharmaceuticals and agricultural chemicals. It is a powerful irritant and causes burns.Acetic Anhydrides: Compounds used extensively as acetylation, oxidation and dehydrating agents and in the modification of proteins and enzymes.Epoxy Compounds: Organic compounds that include a cyclic ether with three ring atoms in their structure. They are commonly used as precursors for POLYMERS such as EPOXY RESINS.Succinic Anhydrides: A subclass of anhydrides with the general structure of dihydrofurandione. They can be substituted on any carbon atom. They modify and inhibit proteins and enzymes and are used in the acylation of amino- and hydroxyl groups.

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 ...
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:. ...
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 ...
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...
DuPont Pharmaceuticals new drug efavirenz (Sustiva) has enjoyed a favored position among treatment activists, offering both high levels of antiviral ...
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Increased discussion on timing (that is, trimester) of initiation of ARV drugs in ARV-naive pregnant women. Discussion of continuation of efavirenz in women receiving efavirenz-based ART who present for antenatal care in the first trimester ...
Failure of initial therapy with two nucleosides and efavirenz is not associated with early emergence of mutations in the C-terminus of HIV-1 reverse transcriptase ...
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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 ...
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.
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.
Easy to read patient leaflet for Sustiva (Efavirenz Tablets). Includes indications, proper use, special instructions, precautions, and possible side effects.
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.
BioAssay record AID 541841 submitted by ChEMBL: Inhibition of CYP2B6 in human liver microsomes assessed as 8-hydroxyefavirenz 14-hydroxylation after 10 mins.
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 ...
Moderate inhibitors of CYP3A4 (erythromycin, clarithromycin, fluconazole, amprenavir, fosamprenavir, aprepitant, verapamil, diltiazem) increase the level of dapoxetine systemic exposure! DOJ/CRD continues to use its traditional fair housing tools to prevent segregation and re-segregation of communities? "While there are men who come and complain that their partners are not participating in a sexual act the way they want them to, efavirenz lamivudine tenofovir price there are a variety of reasons why women dont. After the threshold of the motor endplate is reached, efavirenz lamivudine tenofovir price the muscle membrane is depolarized and excitation-contraction coupling is initiated? Discover parrot-fashion pulmicort buy the ghd ® Official Website ghdhaircom for the latest ghd! (152) The court also reiterated its prior reliance on peer review noting that no scientific or medical journal had published plaintiffs experts studies! Im bookmarking and will be tweeting this to my followers? ...
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.
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. ...
Camber Pharmaceuticals, Inc.: Efavirenz tablets in combination with other antiretroviral agents is indicated for the treatment of human immunodeficiency virus...
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.
c Monitor for therapeutic response and consider therapeutic drug monitoring to assure dosage adequacy in patients who weigh ,90 kg.. Key to Acronyms: COBI = cobicistat; EFV = efavirenz; EVG = elvitegravir; FTC = emtricitabine; MVC = maraviroc; NNRTI = non-nucleoside reverse transcriptase inhibitor; PI = protease inhibitor; TAF = tenofovir alafenamide. ...
Nelfinavir, efavirenz, or both after the failure of nucleoside treatment of HIV infection.AIDS Clinical Trials Group 364 Study Team ...
1IKX: Structural basis for the inhibitory efficacy of efavirenz (DMP-266), MSC194 and PNU142721 towards the HIV-1 RT K103N mutant.
A team of researchers from Johns Hopkins University School of Medicine reported that the way the body metabolizes the HIV medication efavirenz may ...
臺灣地區愛滋病毒感染者抗愛滋病毒藥物的治療建議【前 言】含兩種核苷酸反轉錄酶抑制劑(nucleostide reverse-transcriptase inhibitors;NRTI)併用一種非核苷酸
Efavirenz is currently the antiretroviral backbone recommended for HIV-tuberculosis-coinfected patients, but in the absence of an alternative to efavirenz in patients who cannot receive it, nevirapine is still prescribed for some HIV-tuberculosis-coinfected patients. This is the first study comparing pharmacokinetic parameters of rifampin and isoniazid when prescribed alone and with nevirapine when prescribed without a lead-in dose in Mozambican HIV-tuberculosis-coinfected patients. To our knowledge, our study contributes to the limited data on the pharmacokinetics of antituberculosis drugs in HIV-infected patients treated with efavirenz. Our main finding is that rifampin exposure was not altered to a clinically significant extent when combined with either nevirapine or efavirenz. A 29% significant decrease in isoniazid exposure (AUC) was demonstrated when coadministered with efavirenz but not nevirapine. The consequence of such a reduction is unknown. However, it has been suggested from an in ...
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. Aside from the synthesis and characterization of such multifunctional benzoxazines, reactivity and polymerization behavior is studied in dependence of the oxazine functionality. 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. 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.
A behavioral comparison of acute and chronic Delta9-tetrahydrocannabinol and cannabidiol in C57BL/6JArc mice. Cannabinoid Treatment int J Neuropsychopharmacol 2010;13(7):861-76. View abstract. Magen I Avraham Y Ackerman Z et al. Cannabidiol ameliorates cognitive hemp protein powder nutrition facts and motor impairments in mice with bile duct ligation. J Hepatol 2009;51(3):528-34.. Disclaimer These statements have not been evaluated by the FDA. These products are not intended to diagnose treat cure or prevent any disease. __USERID__ -certified-organic-hemp-oil-non-gmo-24-fl-oz-710-ml-1 Vitacost Certified Organic Hemp Oil - Non-GMO - 24 fl oz (710 mL) 4.. Rehabil. 2003;17(1):21-29. View abstract.. Braz J Med Biol Res 2006;39(4):421-9. View abstract. Zuardi AW Morais SL Guimaraes FS Mechoulam R.. End prohibition. Put this on the ballot. We are adults for crying Cannabinoid Treatment out loud.. No one in utah has access to prescription drugs that arent prescribed to them. Fred T Bring it to the ...
Prolonged exposure of rats to the synthetic cannabinoid receptor ligand, CP-55,940 (0.4 mg/kg, i.p. for 11 days), induced tolerance to analgesia, to the reduction in spontaneous locomotor activity and the incidence of splayed hind limbs. One hour after the last injection on day 11, the rats were killed and in situ hybridization was used to investigate the effect of treatment on G-protein alpha-subunit expression throughout the brain. Chronic cannabinoid exposure markedly reduced G alpha(s), G alpha(i) and G alpha(o) mRNA levels. The message for the alpha(s)-subunit was decreased in all the brain areas containing the basal autoradiographic signal; the decrease ranging from 25% in the thalamus to 45% in the mesencephalon. Also the basal G alpha(i) expression was reduced in tolerant rats showing the greatest decrease in the forebrain (63%) in the cerebellum (58%) and in the mesencephalon (38%). The reduction in G alpha(o) expression (25%) was more localized, being present only in the rostral portion of the
SUSTIVA® (sus-TEE-vah) [efavirenz (eh-FAH-vih-rehnz)] capsules and tablets. ALERT: Find out about medicines that should NOT be taken with SUSTIVA.. Please also read the section "MEDICINES YOU SHOULD NOT TAKE WITH SUSTIVA.". Read this information before you start taking SUSTIVA (efavirenz). Read it again each time you refill your prescription, in case there is any new information. This leaflet provides a summary about SUSTIVA and does not include everything there is to know about your medicine. This information is not meant to take the place of talking with your doctor.. What is SUSTIVA?. SUSTIVA is a medicine used in combination with other medicines to help treat infection with Human Immunodeficiency Virus type 1(HIV-1), the virus that causes AIDS (acquired immune deficiency syndrome). SUSTIVA is a type of anti-HIV drug called a "non-nucleoside reverse transcriptase inhibitor" (NNRTI). NNRTIs are not used in the treatment of Human Immunodeficiency Virus type 2 (HIV-2) infection.. SUSTIVA ...
4H-Indolo[4,3-fg][3,1]benzoxazine,6,6a,7,8,10,- 10a-hexahydro-7,8-dimethyl-10-(1-methylethenyl)-,(6aR,8R,10R,10aR)- 1,3-bis(2-methylprop-2-enyl)-2-prop-2-enoxy-benzene Benzeneacetic acid, alpha-methyl-4-(4-oxo-2-(propylthio)-3(4H)-quinazolinyl)-, methyl ester 4-methyl-6-(2,2,3,3,4,4,5,5-octafluoropentoxy)pyrimidin-2-amine 2-Propanol, 1-((1-methylpropyl)thio)-3-(6,7,10,11-tetramethoxyemetan-2-yl)-, 2HCl Benzyl (3S-(2(R*),3alpha,8abeta))-1-(3-benzylhexahydro-1,4-dioxopyrrolo(1,2-a)pyrazin-2(1H)-yl)-1-oxopropane-2-carbamate 4-(4,5-dichloro-6-oxo-pyridazin-1-yl)benzenesulfonamide 3-(benzyl-methyl-amino)-1-naphthalen-2-yl-propan-1-one 4-amino-4-methyl-pentanoic acid 6-amino-5H-purine-2-sulfonamide
The open-label design of the study has probably influenced adjudication of the primary outcomes, such as time to the occurrence of adverse effects or tolerability, thus making the study prone to performance bias. It was able to declare equivalence among the compared treatments on the basis of previously defined boundaries only in a post hoc assessment. The authors state that this differed from the A5142 study (2) by randomizing and blinding the nucleoside reverse transcriptase inhibitors (NRTI) and by using atazanavir plus ritonavir. The A5202 study blinded only patients assigned to the NRTI, and unblinding occurred in patients with high viral load status at screening at the recommendation of the data safety monitoring board. The prespecified analysis of the A5202 study demonstrated that a ritonavir-boosted protease inhibitor was not able to reach the noninferiority margin (compared with efavirenz) in a way similar to that of the A5142 study (2). Furthermore, the study did not find substantial ...
Gliomas (tumors in the brain) are especially aggressive malignant forms of cancer, often resulting in the death of affected patients within one to two years following diagnosis. There is no cure for gliomas and most available treatments provide only minor symptomatic relief.. A review of the modern scientific literature reveals numerous preclinical studies, some case reports, and one controlled clinical study demonstrating cannabinoids ability to act as antineoplastic agents, particularly on glioma cell lines.. Writing in the September 1998 issue of the journal FEBS Letters, investigators at Madrids Complutense University, School of Biology, first reported that delta-9-THC induced apoptosis (programmed cell death) in glioma cells in culture.[1] Investigators followed up their initial findings in 2000, reporting that the administration of both THC and the synthetic cannabinoid agonist WIN 55,212-2 "induced a considerable regression of malignant gliomas" in animals.[2] Researchers again ...
On September 27, 2012, Justice Barnes of the Federal Court granted Bristol-Myers Squibb (BMS) an Order prohibiting the Minister of Health from issuing a notice of compliance (NOC) to Mylan Pharmaceuticals ULC for a generic efavirenz product (BMSs SUSTIVA) until the expiry of Patent No. 2,101,572 ( 572), but not Patent No. 2,279,198 ( 198). Canada Intellectual Property Smart & Biggar/Fetherstonhaugh 15 Oct 2012
Hi, I am learning about how cannabinoids work and different effects they may have on humans and animals. I know THC and, to a lesser extent, CBD have been...
RESULTS: The actions of family physician or general practitioner are primary prevention, pre and post test counsel, request HIV test, active search for partners and first management. The first screening include b-HCG. Pregnants must be delivery to specialised service. The patients are divided in three groups: non symptomatic and with CD4 more than 350 are not treated; non symptomatic and CD4 between 200 and 350 are counselled to not treat at this moment; and CD4 less than 200 or symptomatic should be treated. Taking into account adherence, posology and side effects the suggested scheme is zidovudine, lamivudine plus efavirenz for men and nevirapine for women. The CD4 e viral load should be measure in 8 and 24 weeks to evaluate treatment failure. In this case, after dismiss biological factors, non-adherence, or immunologic recovery syndrome, the patient is delivered to the specialist ...
Although the application of medical marijuana and cannabinoid drugs is controversial, it is a part of modern-day medicine. The list of diseases in which cannabinoids are promoted as a treatment is...
68084-14-0 - GGDIRZQYYPQPJE-RQTFDDCJSA-K - Acetic acid, 2-((4-(2-(4-(2-(4-amino-7-sulfo-1-naphthalenyl)diazenyl)-7-sulfo-1-naphthalenyl)diazenyl)phenyl)amino)-2-oxo-, sodium salt (1:3) - Similar structures search, synonyms, formulas, resource links, and other chemical information.
N-(3,4-dioxo-3,4-dihydro-2-naphthalenyl)acetamide - chemical structural formula, chemical names, chemical properties, synthesis references
Batten, MP and Canty, AJ and Cavell, KJ and Skelton, BW and White, AH (2006) Synthesis and Structures of the Ligands 1-Methylimidazol-2-yl(pyridin-2-yl)-methanone {(py)(mim)CO} and 1-Benzylimidazol-2-yl(1-phenylaldimine)(PhN=CHbim) as their Tetracarbonylmolybdenum(0) Complexes[Mo(CO)4(L2-N,N)]. Zeitschrift fur Anorganische und Allgemein Chemie, 632 (5). pp. 876-878. ISSN 0044-2313 ...
Find ODEFSEY® (emtricitabine, rilpivirine & tenofovir alafenamide) study design information for treatment-naive adults. Read benefits & risks.
Find BMD data for ODEFSEY® (emtricitabine, rilpivirine & tenofovir alafenamide) in treatment-naive adults. Read benefits & risks.
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TY - JOUR. T1 - Efavirenz liquid formulation in human immunodeficiency virus-infected children. AU - Starr, Stuart E.. AU - Fletcher, Courtney V.. AU - Spector, Stephen A.. AU - Brundage, Richard C.. AU - Yong, Florence H.. AU - Douglas, Steven D.. AU - Flynn, Patrizia M.. AU - Kline, Mark W.. PY - 2002/7/23. Y1 - 2002/7/23. N2 - Background. This study determined the safety, pharmacokinetics, antiviral activity and immunologic effects of efavirenz liquid formulation, nelfinavir and nucleoside reverse transcriptase inhibitors (NRTIs) in HIV-infected children, 3 to 9 years of age. Methods. Plasma HIV-1 RNA and lymphocyte subsets were measured at various intervals after initiation of therapy. Pharmacokinetic studies were performed at Week 2, and doses of efavirenz and nelfinavir were adjusted if area under the curve values fell outside specified target ranges. Results. This combination of antiretrovirals was well-tolerated. Pharmacokinetic values were similar to those observed in a previous study ...
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Adult and adolescent guidelines of the U.S. Department of Health and Human Services state that maraviroc is "not recommended" for initial treatment of HIV infection. Maraviroc is effective only in persons with exclusively CCR5-tropic HIV. Tropism testing should be performed before initiating treatment with maraviroc, to verify that no CXCR4-tropic virus is present. In previously untreated patients, a randomized controlled study compared maraviroc with efavirenz, each drug being given in combination with zidovudine + lamivudine. All patients had only CCR5-tropic HIV according to the tropism assay available at the time of study entry. At 48 weeks, by intention-to-treat analysis, the maraviroc group had lower rates of virologic suppression to ,50 copies/mL than the efavirenz group (65% vs 69%); this result did not meet the studys criteria for noninferiority of maraviroc.(4) However, researchers later reanalyzed the baseline tropism status of the study subjects using a more sensitive tropism assay ...
This nested case-control study examined relationships between MDR1, CYP2B6, and CYP3A4 variants and hepatotoxicity during antiretroviral therapy with either efavirenz- or nevirapine-containing regimens. Decreased risk of hepatotoxicity was associated with MDR1 3435C→;T (odds ratio, 0.254; P = .021). An interaction between MDR1 and hepatitis B surface antigen status predicted risk with 82% accuracy (P , .001).. ...
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Journal compilation © 2009 John Wiley & Sons A/S. Cytokines in milk like transforming growth factor-beta (TGF-β) have been shown to induce oral tolerance in experimental animal studies. However, human studies are less consistent with these findings. The primary objective of this review was to conduct a systematic review of published studies on the association between TGF-β identified in human milk and immunological outcomes in infancy and early childhood. Human prospective clinical studies were identified through MEDLINE, CAB Abstracts, Biological Abstracts and Scopus. Selection criteria included: well described populations of mothers and infants, time of milk sampling, immunological outcome measures and analytical methods of TGF-β determination. We considered a wide range of immunological outcomes in infancy and early childhood, such as wheeze, atopy, eczema and the immunoglobulin switch. Twelve human studies were included in the review and 67% showed a positive association with TGF-β1 or ...
Panag Pharmas (Panag), a subsidiary of Tetra, PPP003 is a synthetic cannabinoid drug that selectively acts at the type 2 cannabinoid receptor (CB2R). "Panags scientific team and academic collaborators have been studying the role of the CB2R in acute immune responses for over a decade. The active molecule in PPP003 can reduce inflammation and dampen pro-inflammatory cytokine release, therefore, PPP003 should be carefully examined as a candidate drug to help reduce symptoms of acute lung inflammation and immune system dysregulation in those SARS-CoV-2 patients at risk", states Tetras CSO, Dr. Melanie Kelly, Ph.D.. Guy Chamberland, CEO & CRO of Tetra commented, "It is a time for all pharmaceutical companies to contribute to the management of COVID-19 patients. We agree with our Canadian political leaders this is a time of national emergency. Our Panag team has been performing research on the prevention and management of severe systemic immune dysregulation such as sepsis since the early 2000s. ...
Efavirenz (EFV) is a non-nucleoside reverse transcriptase inhibitor in wide use for the treatment of HIV infection. Although EFV is generally well tolerated, there is well-documented neuropsychiatric toxicity. The toxic effects of EFV in hepatocytes and keratinocytes have been linked to mitochondrial perturbations and changes in autophagy. Here, we studied the effect of EFV on mitochondria and autophagy in neuronal cell lines and primary neurons. In SH-SY5Y cells, EFV induced a drop in ATP production, which coincided with increased autophagy, mitochondrial fragmentation, and mitochondrial depolarization. EFV induced mitophagy was also detected by colocalization of mitochondria and autophagosomes and use of an outer mitochondrial membrane tandem fluorescent vector. Pharmacologic inhibition of autophagy with 3-methyladenine (3MA) increased the cytotoxic effect of EFV, suggesting that autophagy is promoting cell survival. EFV also reduces ATP production in primary neurons, induces autophagy, and ...
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This drug is used with other HIV medications to help control HIV infection. It helps to decrease the amount of HIV in your body so your immune system
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Supplementing starters on ART containing Efavirenz and Tenofovir with 4000 iu Vit D, and oral calcium, reduced BMD loss by 50% in the first year, say ACTtG A5280. Expected elevations in both PTH and bone turnover were reduced. It at least suggests th
A paper in the October issue of the Journal of Psychopharmacology will be of interest to my readership. It looks at the consequences of exposure to an exogenous cannabinoid agonist Byrnes JJ, Johnson NL, Schenk ME, Byrnes EM. Cannabinoid exposure in adolescent female rats induces transgenerational effects on morphine conditioned place preference in male offspring.J…
OBJECTIVES. We designed two different studies to evaluate two different combination antiretroviral therapy (cART) stopping strategies namely a staggered stop approach (STOP 1 study) and a protected stop approach (STOP 2 study) to find the best universal stop strategy.. PATIENTS AND METHODS. Patients who stopped cART for any reason were recruited. In STOP 1, 10 patients on efavirenz continued dual nucleos(t)ide reverse transcriptase inhibitors (NRTIs) for 1 week after discontinuing efavirenz. Efavirenz concentrations were measured weekly for up to 3 weeks. In STOP 2, 20 patients stopped their cART and replaced it with two tablets of lopinavir/ritonavir (Kaletra) (100/50 mg) twice daily for 4 weeks. Lopinavir, efavirenz, nevirapine and tenofovir concentrations were measured weekly for up to 4 weeks. Virological and resistance testing were performed.. RESULTS. In STOP 1 five patients still had efavirenz present (median t(1/2)=148.4 h) 3 weeks after stopping. In STOP 2, 15/20 patients had a ...
Aminoalkylindoles (AAIs) are a family of cannabinergic compound that act as a cannabinoid receptor agonist. They were invented by pharmaceutical company Sterling-Winthrop in the early 1990s as potential nonsteroidal anti-inflammatory agents. Aminoalkylindole are now commonly found in synthetic cannabis designer drugs. In the United States, the DEA added the aminoalkylindole JWH-200 to Schedule I of the Controlled Substances Act on 1 March 2011 for 12 months. Emmanuel S. Onaivi (2006). Marijuana and Cannabinoid Research: Methods and Protocols. Springer. pp. 128-. ISBN 978-1-59259-999-8. "Synthetic Cannabinoids". American Association for Clinical Chemistry. 2013-02-01. Retrieved 2013-11-17. "Schedules of Controlled Substances: Temporary Placement of Five Synthetic Cannabinoids Into Schedule I". Federal Register. 2011-03-01. Retrieved 2013-11-17. Aminoalkylindoles, ...
Cannabinoid agonists, including marijuana containing delta-9-tetrahydrocannabinol (THC), are found rewarding by humans. In addition to human self-reports and experimental studies that show marijuana is rewarding, contributions from preclinical studies also have implicated cannabinoid receptors in reward-motivated behavior. One way to assess these preclinical effects of cannabinoids is intracranial self-stimulation (ICSS), where an animal performs a response to receive electrical stimulation of a specific brain area or circuit known to be involved in reward. Drugs of abuse, such as psychomotor stimulants, facilitate responding for ICSS. While a few studies have shown facilitating effects of cannabinoids in rats, several have shown the opposite effect, and no studies so far have evaluated cannabinoids in mouse ICSS. Furthermore there are no studies evaluating specific inhibitors of endocannabinoid catabolic enzymes in ICSS in any species. In these studies we assessed the cannabinoid agonist THC, as well
RESULTS: Antiretroviral therapy is recommended for all adults with HIV infection. Evidence for benefits of treatment and quality of available data increase at lower CD4 cell counts. Recommended initial regimens include 2 nucleoside reverse transcriptase inhibitors (NRTIs; abacavir/lamivudine or tenofovir disoproxil fumarate/emtricitabine) and a third single or boosted drug, which should be an integrase strand transfer inhibitor (dolutegravir, elvitegravir, or raltegravir), a nonnucleoside reverse transcriptase inhibitor (efavirenz or rilpivirine) or a boosted protease inhibitor (darunavir or atazanavir). Alternative regimens are available. Boosted protease inhibitor monotherapy is generally not recommended, but NRTI-sparing approaches may be considered. New guidance for optimal timing of monitoring of laboratory parameters is provided. Suspected treatment failure warrants rapid confirmation, performance of resistance testing while the patient is receiving the failing regimen, and evaluation of ...
5-methyl-3-(4-methylpiperazin-1-yl)pyridazino[3,4-b][1,4]benzoxazine ...
Bernardi, L; Coda, S; Bonsignori, A; Pegrassi, L; Suchowsky, G. K. (1969). "Central depressant properties of 3,1-benzoxazine ...
Benzoxazines formed by the reaction of phenols, formaldehyde and primary amines which on heating to ~400 °F (~200 °C) ... doi:10.1002/14356007.a22_651 Handbook of Benzoxazine Resins, ed. Hatsuo Ishida And Tarek Agag, Elsevier B.V., 2011, ISBN 978-0- ... Development of polymeric materials as a class of benzoxazines. ...
"Synthesis and pharmacology of benzoxazines as highly selective antagonists at M(4) muscarinic receptors". Journal of Medicinal ...
Fe(acac)3 also catalyzes the ring-opening polymerization of 1,3-benzoxazine. Beyond the area of polymerization, Fe(acac)3 has ... 3-benzoxazine". Journal of polymer science. Part A, Polymer chemistry. 48 (2): 479. doi:10.1002/pola.23810. Williamson, K. T.; ...
... benzoxazines MeSH D03.383.533.500 --- ifosfamide MeSH D03.383.533.640 --- morpholines MeSH D03.383.533.640.250 --- ...
Benzoxazines [more specifically: cyclopropylethynylated benzoxazines] Substituted benzoxazines Efavirenz, the active ...
Priming maize resistance by its neighbors: activating 1,4-benzoxazine-3-ones synthesis and defense gene expression to alleviate ...
3-benzoxazine-1,4-dione, II), and N-hydroxyphthalimide (III). It was not until the 1950s that Cohn's product was definitely ...
... benzoxazine-1-carboxylic acid ethyl ester, CAS# 23062-91-1) PD-0298029 Tropicamide - moderate selectivity over other muscarinic ...
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 ...
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 ...
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. ...
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. ...
Study of the Complexation of a New Crown-containing Benzoxazine Spiropyran with Metal Cations. ...
... 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 ...
Learn more about 3-4-dihydro-2h-1-4-benzoxazine-6-boronic-acidpinacol-ester. We enable science by offering product choice, ... Description: 3,4-Dihydro-2H-1,4-benzoxazine-6-boronic acid pinacol ester ... 3,4-Dihydro-2H-1,4-benzoxazine-6-boronic acid pinacol ester ...
  • A new RTM system based on a novel benzoxazine/epoxy chemistry has been developed and is in the final phase of commercial introduction to the market place. (netcomposites.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)
  • The curing kinetic of benzoxazine-epoxy hybrid networks by nonisothermal differential scanning calorimetry was noted by Jubsilp et al. (hindawi.com)
  • Benzoxazine precursors were synthesized using 4-hydroxybenzaldehyde as phenolic component, paraformaldehyde, and two different functional polyetheramines. (aiche.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)
  • Tomohiko Ohwada: '4H-1, 2-Benzoxazines with Electron-withdrawing Substituents on the Benzene Ring. (nii.ac.jp)
  • Low-Dissipation Thermosets Derived from Oligo(2,6-Dimethyl Phenylene Oxide)-Containing Benzoxazines. (nih.gov)
  • 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)
  • Bioinspired Design Provides High-Strength Benzoxazine Structural Adhesives. (escholarship.org)
  • Benzoxazines" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (umassmed.edu)
  • Currently supervising a PhD student (Maryam Sairi, sponsored by the Malaysian Government) on predicting the char yield of Benzoxazines by QSPR. (surrey.ac.uk)
  • 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)
  • 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)
  • mol -1 and the total order of reaction is 1.84, which is quite different from that of normal benzoxazine. (scientific.net)
  • Benzoxazines formed by the reaction of phenols, formaldehyde and primary amines which on heating to ~400 °F (~200 °C) polymerise to produce polybenzoxazine networks. (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)
  • 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)
  • 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)
  • This graph shows the total number of publications written about "Benzoxazines" by people in this website by year, and whether "Benzoxazines" was a major or minor topic of these publications. (umassmed.edu)
  • Below are the most recent publications written about "Benzoxazines" by people in Profiles. (umassmed.edu)