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Cytochrome P450 2E1 is the Principal Catalyst of Human Oxidative
Cytochrome P450 2E1 is the Principal Catalyst of Human Oxidative

... similarly using typical protein concentrations of 1 mg/ml and incubation times of 60 or 90 min. Metabolites and internal standards were analyzed by ion HPLC with conductivity detection. Analyses were performed using a DX300 HPLC-IC system (Dionex Corp. Sunnyvale, CA), consisting of an AGP gradient p ...
Bioavailability & Bioequivalence
Bioavailability & Bioequivalence

...  Filtration occurs in the glomerulus; secretion is primarily restricted to the proximal tubules  Reabsorption occurs all along the nephron; Active reabsorption usually occurs in the proximal tubule  Appearance of drug in the urine is the net result of filtration, secretion, and reabsorption ...
Guidelines for ATC classification and DDD assignment
Guidelines for ATC classification and DDD assignment

... - To develop methods, manuals and guidelines for the practical application and appropriate use of the ATC/DDD system in drug utilization studies in a variety of settings, particularly those applicable to developing countries. - To work with groups involved in rational drug use initiatives to integr ...
effect of cytochrome p450 2d6 and 3a enzyme inhibition on
effect of cytochrome p450 2d6 and 3a enzyme inhibition on

... to use oxycodone in the treatment of chronic pain also in outpatient care settings. Oxycodone is metabolized mainly in the liver by CYP enzymes. CYP3A and to a lesser degree, CYP2D6 are responsible for the oxidative metabolism of oxycodone (Lalovic et al. 2004). Due to its CYP-mediated metabolism, o ...
Timolol Metabolism in Human Liver Microsomes Is Mediated
Timolol Metabolism in Human Liver Microsomes Is Mediated

... The disappearance of timolol was determined semiquantitatively from LC/MS runs with the time-of-flight instrument by comparing the peak area in an appropriate 0-min sample to that of the corresponding metabolized sample (incubated with NADPH for 20, 40, or 60 min). The effects of the inhibitors on t ...
Amphotericin B as a mycolic acid specific targeting agent in tuberculosis
Amphotericin B as a mycolic acid specific targeting agent in tuberculosis

... linked to Amphotericin B via a Schiff base to a linker molecule, terephthalaldehyde. Although this molecule showed a loss of biological activity, a discovery was made by serendipity that could have great impact in understanding how Mycobacterium tuberculosis enters and survives in the host macrophag ...
View Full Article - PDF - International Research Journals
View Full Article - PDF - International Research Journals

... the oral absorption of vancomycin and teicoplanin is very low so they must be administered intravenously to control systemic infections, which is not the preferred route of administration for many patients (Andre et al., 2010). Oxazolidinones are a novel class of synthetic antimicrobials with potent ...
The Cytochrome P450 2B6 (CYP2B6) Is the Main Catalyst of
The Cytochrome P450 2B6 (CYP2B6) Is the Main Catalyst of

... the pharmacokinetics of efavirenz varies widely among individuals (Marzolini et al., 2001; Smith et al., 2001), and probably for this reason, the severity of drug interactions with efavirenz is variable and unpredictable (Smith et al., 2001; Lopez-Cortes et al., 2002). The propensity for drug intera ...
Hypericin - The Facts About a Controversial Agent
Hypericin - The Facts About a Controversial Agent

... concentrations above 10-3 mol/L suggesting that greater concentrations induce formation of high molecular weight aggregates. For this reason most of the product specifications of commercially available hypericin do not specify this critical value. ACTIVITY OF HYPERICIN ON ENZYMES Several pharmacolog ...
Effects of grapefruit juice on the pharmacokinetics of selected
Effects of grapefruit juice on the pharmacokinetics of selected

... can be excreted from the body. This metabolism occurs by phase I and phase II reactions. In phase I, the majority of drugs undergo biotransformation reactions that are generally mediated by CYP enzymes, oxidative reactions being the most common. In phase II reactions, drug molecules or their metabol ...
Potential medicinal benefits of Cosmos caudatus (Ulam Raja): A
Potential medicinal benefits of Cosmos caudatus (Ulam Raja): A

... In another study, Wong et al. (2006) assessed the anti-oxidant activities of aqueous extracts of 25 tropical plants using DPPH scavenging and ferric ion reducing anti-oxidant potential (FRAP) assays.[15] Among the 25 plants, C. caudatus exhibited the highest DPPH free radical-scavenging activity and ...
The Proton Pump Inhibitor, Omeprazole, but Not Lansoprazole or
The Proton Pump Inhibitor, Omeprazole, but Not Lansoprazole or

... part, to inhibition of CYP2C19 by omeprazole. However, clinically relevant DDIs with omeprazole are generally of low magnitude [ⱕ120% (2.2-fold) increase in plasma AUC of CYP2C19 substrates; (MTDI database)]. By way of comparison, there is up to a 14.6-fold increase in the area under the curve (AUC) ...
Targeting the Bacterial Division Protein FtsZ
Targeting the Bacterial Division Protein FtsZ

... division proteins in E. coli. FtsZ and the early cell division proteins localize to the division site before cell septation starts. The proteins are recruited to the Z-ring in a sequential and approximately linear pathway. The requirement of an upstream protein for localization of a downstream prote ...
IDENTIFICATION OF NATURAL PRODUCTS AS ANTIDIABETIC AGENTS Laura Guasch Pàmies
IDENTIFICATION OF NATURAL PRODUCTS AS ANTIDIABETIC AGENTS Laura Guasch Pàmies

... recommended in conditions in which a patient has decreased renal or hepatic function. Metformin is the first-line drug of choice for the treatment of T2DM, particularly in overweight and obese patients and those with normal kidney function [15]. Agonists of the peroxisome proliferator-activated nucl ...
ERGOLINE ALKALOIDS ERGOT ALKALOIDS ÇAVDAR MAHMUZU
ERGOLINE ALKALOIDS ERGOT ALKALOIDS ÇAVDAR MAHMUZU

... • Frequently, the alkaloid production is dependent on the phosphate concentration of the medium, and for many strains, on the precise concentrations of minerals (iron, zinc, copper, boron) which directly influence the productivity. • The oxygenation of the culture medium must be intense. Cell differ ...
Pharmacology of platelet inhibition in humans: implications of the
Pharmacology of platelet inhibition in humans: implications of the

... Aspirin is quickly deacetylated in vivo to salicylate. It has been suggested that in sites readily accessible to aspirin, such as circulating platelet cyclooxygenase, it might be expected to act in its own right as the acetylsalicylate ion and hence to be more potent than salicylate.7 It would also ...
Active Transport of Fentanyl by the Blood-Brain Barrier1
Active Transport of Fentanyl by the Blood-Brain Barrier1

... To corroborate these findings, a study was done to determine the rates of release of [3H]fentanyl from cells preloaded with [3H]fentanyl under control conditions, and one was done in which the supernatant contained 10 mM cold fentanyl (EC75 for saturating the inward transport mechanism). Figure 2 sh ...
Olive - Hindawi Publishing Corporation
Olive - Hindawi Publishing Corporation

... shrubs including olive tree and its relatives numbering about 600 species [3]. The family is divided into several tribes, i.e., Fontanesieae, Forsythieae, Jasmineae, Myxopyreae, and Oleeae [4]. These are mostly native of all continents except the Antarctic; including tropical, subtropical, and tempe ...
67Dihydroxybergamottin Contributes to the Grapefruit
67Dihydroxybergamottin Contributes to the Grapefruit

C 3  R
C 3 R

... possesses the highest activity ever recorded for a P450 (4). By combinations of sitedirected and random mutagenesis many BM3 mutants have been obtained which are able to convert drugs and drug-like molecules to human relevant metabolites (5-8). In our previous work, four mutants of BM3 have been eva ...
Duloxetine Inhibits Effects of MDMA (``Ecstasy``) In Vitro and in
Duloxetine Inhibits Effects of MDMA (``Ecstasy``) In Vitro and in

... effects of dual SERT and NET inhibition with duloxetine on the pharmacokinetics (PK) and pharmacodynamics (PD) of MDMA in humans. Duloxetine was used because it is the most potent and selective dual SERT and NET inhibitor, although it also inhibits the DAT with 10- to 100-fold lower potency compared ...
week5
week5

... 1. Find the complex structures of ShK with Kv1.1, Kv1.2 and Kv1.3, and validate them using mutagenesis data. Determine the PMFs and the binding free energy and compare with experiment for further validation. Use the binding mode to predict mutations that will improve the Kv1.3/Kv1.1 selectivity. 2. ...
Antiatherogenic Properties of Naringenin, a Citrus Flavonoid
Antiatherogenic Properties of Naringenin, a Citrus Flavonoid

... IC50 (50% inhibition concentration) for cell growth was > 1 mM for both naringenin and hesperetin in the human hepatoma cell line HepG2, the Macacus’ rhesus monkey kidney cell line MA-104, and the human lung cancer cell line A549. The results of these studies indicate that these flavonoids have rela ...
INHIBITION OF OAT3-MEDIATED RENAL UPTAKE AS A
INHIBITION OF OAT3-MEDIATED RENAL UPTAKE AS A

... unchanged form (Lippert et al., 1995). Since the average absolute oral bioavailability of fexofenadine was reported to be 33% (Dresser et al., 2005), about 36% of the bioavailable fexofenadine can be excreted into the urine during a 24-h period, and renal elimination makes a significant contribution ...
Midazolam Oxidation by Cytochrome P450 3A4 and Active
Midazolam Oxidation by Cytochrome P450 3A4 and Active

... Ala-305, Tyr-307, and Thr-309 with a smaller amino acid decreased this ratio. Kinetic analyses of nine key mutants revealed that the alteration in regioselectivity is caused by a change in kinetic parameters (Vmax and KM) for the formation of both metabolites in most cases. The study revealed the ro ...
1 2 3 4 5 ... 67 >

Discovery and development of neuraminidase inhibitors

Neuraminidase inhibitors inhibit enzymatic activity of the enzyme neuraminidase (sialidase). These type of inhibitors have been introduced as anti-influenza drugs as they prevent the virus from exiting infected cells and thus stop further spreading of the virus. Neuraminidase inhibitors for human neuraminidase (hNEU) have the potential to be useful drugs as the enzyme plays a role in several signaling pathways in cells and is implicated in diseases such as diabetes and cancer.
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