Granska/Öppna
... facilitate transfer of compounds to the fetal circulation as an efflux transporter (Unadkat et al. 2004, Bakos et al. 2007, Myllynen et al. 2007). MRP1 has been shown to have a crucial role in permeability of drugs, for example, in the brain and in gastrointestinal tissues, but its functional role i ...
... facilitate transfer of compounds to the fetal circulation as an efflux transporter (Unadkat et al. 2004, Bakos et al. 2007, Myllynen et al. 2007). MRP1 has been shown to have a crucial role in permeability of drugs, for example, in the brain and in gastrointestinal tissues, but its functional role i ...
Ahead of print online version Moxidectin causes adult worm
... Forrester et al. 2002). Some reports also demonstrate the efficacy of MOX against those nematodes that did not respond to IVM (Craig et al. 1992, Coles et al. 1994), suggesting some differences in the mode of action of these two compounds. The proposed study has been planned to evaluate the in vitro ...
... Forrester et al. 2002). Some reports also demonstrate the efficacy of MOX against those nematodes that did not respond to IVM (Craig et al. 1992, Coles et al. 1994), suggesting some differences in the mode of action of these two compounds. The proposed study has been planned to evaluate the in vitro ...
effects of cytochrome p450 enzyme inhibitors on the
... Cytochrome P450 (CYP) enzymes play a pivotal role in the metabolism of many drugs. Inhibition of CYP enzymes usually increases the plasma concentrations of their substrate drugs and can thus alter the safety and efficacy of these drugs. The metabolism of many widely used nonsteroidal anti-inflammato ...
... Cytochrome P450 (CYP) enzymes play a pivotal role in the metabolism of many drugs. Inhibition of CYP enzymes usually increases the plasma concentrations of their substrate drugs and can thus alter the safety and efficacy of these drugs. The metabolism of many widely used nonsteroidal anti-inflammato ...
Potent inhibition of human cytochrome P450 3A isoforms
... Aims: In this study, we examined the inhibitory effects of Δ9-tetrahydrocannabinol (Δ9-THC), cannabidiol (CBD), and cannabinol (CBN), the three major cannabinoids, on the activity of human cytochrome P450 (CYP) 3A enzymes. Furthermore, we investigated the kinetics and structural requirement for the ...
... Aims: In this study, we examined the inhibitory effects of Δ9-tetrahydrocannabinol (Δ9-THC), cannabidiol (CBD), and cannabinol (CBN), the three major cannabinoids, on the activity of human cytochrome P450 (CYP) 3A enzymes. Furthermore, we investigated the kinetics and structural requirement for the ...
Angiotensin-Converting Enzyme Inhibitor-Induced
... Background: A dry, persistent cough is a well-described class effect of the angiotensin-converting enzyme (ACE) inhibitor medications. The mechanism of ACE inhibitor-induced cough remains unresolved, but likely involves the protussive mediators bradykinin and substance P, agents that are degraded by ...
... Background: A dry, persistent cough is a well-described class effect of the angiotensin-converting enzyme (ACE) inhibitor medications. The mechanism of ACE inhibitor-induced cough remains unresolved, but likely involves the protussive mediators bradykinin and substance P, agents that are degraded by ...
Identification and control of HIV drug therapy using fuzzy systems
... SAMIR TALSSI is a Professor at higher institutes of applied engineering IGA-Casablanca. His interest area is artificial intelligence and its applications in epidemiology. Talssi was a Member in the High Council Education in Morocco and has over 10 years of experience as manager and educator. Profess ...
... SAMIR TALSSI is a Professor at higher institutes of applied engineering IGA-Casablanca. His interest area is artificial intelligence and its applications in epidemiology. Talssi was a Member in the High Council Education in Morocco and has over 10 years of experience as manager and educator. Profess ...
Characterization of Two Pharmacophores on the Multidrug
... pristinamycin IIA; TTX, tentoxin; cLF, cyclo-leucinylphenylalanine; VRP, verapamil; PRG, progesterone; VBL, vinblastine; BSe-TTX, (benzoyl-4benzoyl)methylserine-tentoxin. ...
... pristinamycin IIA; TTX, tentoxin; cLF, cyclo-leucinylphenylalanine; VRP, verapamil; PRG, progesterone; VBL, vinblastine; BSe-TTX, (benzoyl-4benzoyl)methylserine-tentoxin. ...
biomedical aids research: recent and upcoming advances
... about drug toxicity emerged in this study, but these did not warrant any changes to current guidelines at this time. Linkage to and retention in care for pregnant women needs attention as the Global Plan towards the elimination of new HIV infections among children by 2015 and keeping their mothers a ...
... about drug toxicity emerged in this study, but these did not warrant any changes to current guidelines at this time. Linkage to and retention in care for pregnant women needs attention as the Global Plan towards the elimination of new HIV infections among children by 2015 and keeping their mothers a ...
View/Open
... DRUGS AFFECTING RENIN-ANGIOTENSIN SYSTEM AND PLASMA KININS involved in cognitive function and memory in animals. Thus Ang IV improves memory. Some vascular, renal and other peripheral effects of Ang IV have also been described. Angiotensin (1-7) This heptapeptide can be produced from Ang I or Ang II ...
... DRUGS AFFECTING RENIN-ANGIOTENSIN SYSTEM AND PLASMA KININS involved in cognitive function and memory in animals. Thus Ang IV improves memory. Some vascular, renal and other peripheral effects of Ang IV have also been described. Angiotensin (1-7) This heptapeptide can be produced from Ang I or Ang II ...
An Introduction to Medicinal Chemistry
... different. In this case you crave sedation or a calming influence, and it is the nicotine in the cigarette smoke which induces that effect. There can be little doubt that alcohol is a drug and as such causes society more problems than all other drugs put together. One only has to study road accident ...
... different. In this case you crave sedation or a calming influence, and it is the nicotine in the cigarette smoke which induces that effect. There can be little doubt that alcohol is a drug and as such causes society more problems than all other drugs put together. One only has to study road accident ...
Atorvastatin
... ranging from 43—60%. Triglycerides are lowered in patients with hypertriglyceridemia by as much as 45%[1379] and HDL cholesterol increases by as much as 12% with atorvastatin monotherapy. The combination of atorvastatin and colestipol produced a 10% greater reduction in LDL-cholesterol than atorvast ...
... ranging from 43—60%. Triglycerides are lowered in patients with hypertriglyceridemia by as much as 45%[1379] and HDL cholesterol increases by as much as 12% with atorvastatin monotherapy. The combination of atorvastatin and colestipol produced a 10% greater reduction in LDL-cholesterol than atorvast ...
Model-based Analysis of the Effects of Thioridazine Enantiomers on the... Papillary Action Potential
... primarily due to (+)-thioridazine, a similar but left-shifted dose-response curve should be expected. The IKr inhibition determined using the forward method was almost identical to that reported by Drolet et al. [4] for the racemate, as were the determined values at 1 and 10 mg L-1 using the inverse ...
... primarily due to (+)-thioridazine, a similar but left-shifted dose-response curve should be expected. The IKr inhibition determined using the forward method was almost identical to that reported by Drolet et al. [4] for the racemate, as were the determined values at 1 and 10 mg L-1 using the inverse ...
enzyme induction and inhibition
... limitation it is possible in man to compare drugs as enzyme inducers by the construction of doseresponse curves. The effect of phenobarbitone on warfarin and antipyrine metabolism has been found to be dose dependent as is the effect of rifampicin on antipyrine and cortisol hydroxylation. In clinical ...
... limitation it is possible in man to compare drugs as enzyme inducers by the construction of doseresponse curves. The effect of phenobarbitone on warfarin and antipyrine metabolism has been found to be dose dependent as is the effect of rifampicin on antipyrine and cortisol hydroxylation. In clinical ...
Oral and perioral herpes simplex virus type 1 (HSV
... polymerase as a substrate analogue of the pyrophosphate formed during DNA synthesis. Foscarnet inhibits not only all human herpesviruses, but also HIV (Crumpacker, 1992). Intravenous foscarnet is considered second-line therapy for the treatment of CMV in patients who present with severe neutropenia ...
... polymerase as a substrate analogue of the pyrophosphate formed during DNA synthesis. Foscarnet inhibits not only all human herpesviruses, but also HIV (Crumpacker, 1992). Intravenous foscarnet is considered second-line therapy for the treatment of CMV in patients who present with severe neutropenia ...
carbapenam and monobactam - Home
... Meropenem is not hydrolyzed by DHP-I and is resistant to most β-lactamases, including a few carbapenemases that hydrolyze ...
... Meropenem is not hydrolyzed by DHP-I and is resistant to most β-lactamases, including a few carbapenemases that hydrolyze ...
(embelin)-a second solid gold of india
... & co-workers [52] observed inhibitory effect of wound healing in invitro wound healing model studies using fibroblast as well as endothelial cells. However, the reasons for inhibitory effect are yet to be explored (Results are not yet published). Enzyme inhibitory activity An enzyme inhibitor is a s ...
... & co-workers [52] observed inhibitory effect of wound healing in invitro wound healing model studies using fibroblast as well as endothelial cells. However, the reasons for inhibitory effect are yet to be explored (Results are not yet published). Enzyme inhibitory activity An enzyme inhibitor is a s ...
DENS 521 4th SF
... first two generations, although their antistaphylococcal activity is reduced. They are remarkably active against most G-ve enteric isolates Some third-generation cephalosporins (e.g., ceftazidime and cefoperazone) also are active against most isolates of P. aeruginosa In healthy subjects, their ...
... first two generations, although their antistaphylococcal activity is reduced. They are remarkably active against most G-ve enteric isolates Some third-generation cephalosporins (e.g., ceftazidime and cefoperazone) also are active against most isolates of P. aeruginosa In healthy subjects, their ...
Review on Prodrugs
... The latter are usually referred to as bioprecursor prodrugs. Conventional carrier-linked prodrugs often have a synthetic handle, a spacer or linker, between the active drug and the promoiety when the desired prodrug moiety cannot be attached directly to the parent molecule because of steric hindranc ...
... The latter are usually referred to as bioprecursor prodrugs. Conventional carrier-linked prodrugs often have a synthetic handle, a spacer or linker, between the active drug and the promoiety when the desired prodrug moiety cannot be attached directly to the parent molecule because of steric hindranc ...
Innovative Biotechnology Companies and their Academic Origins
... - Importantly, caspases are produced in cells as active proteases in cell degradation - IAPs (inhibitors of apoptosis proteins) bind caspases, preventing cell death - The BIR domain (baculoviral IAP repeat) directly inhibits caspase enzymatic activity - Smac (second mitochondria-derived activator of ...
... - Importantly, caspases are produced in cells as active proteases in cell degradation - IAPs (inhibitors of apoptosis proteins) bind caspases, preventing cell death - The BIR domain (baculoviral IAP repeat) directly inhibits caspase enzymatic activity - Smac (second mitochondria-derived activator of ...
CAIX: A Potential Target for Cancer Therapy
... treatment options. An alternative novel therapeutic target involved in multiple intracellular pathways may therefore be sAC (Chapter 7). The use of sAC inhibition in cancer is however still relatively new, since only limited but conflicting data is currently available in literature. Therefore, befor ...
... treatment options. An alternative novel therapeutic target involved in multiple intracellular pathways may therefore be sAC (Chapter 7). The use of sAC inhibition in cancer is however still relatively new, since only limited but conflicting data is currently available in literature. Therefore, befor ...
Chemical, pharmacokinetic and pharmacodynamic properties of
... triglyceride-rich lipoproteins [5,6]. In addition, statins may exert beneficial cardiovascular effects independent of their lipid-modifying properties [7]. These pleiotropic properties may be explained by inhibition of synthesis of nonsteroidal isoprenoid compounds, which are also produced from meva ...
... triglyceride-rich lipoproteins [5,6]. In addition, statins may exert beneficial cardiovascular effects independent of their lipid-modifying properties [7]. These pleiotropic properties may be explained by inhibition of synthesis of nonsteroidal isoprenoid compounds, which are also produced from meva ...
CYP2B6, CYP2D6, and CYP3A4 Catalyze the Primary Oxidative
... conditions were not altered from the kinetic analyses, except that the mechanism-based inhibitors diethyldithiocarbamate, thio-TEPA, furafylline, and troleandomycin were preincubated for 20 min at 37°C with all incubation constituents before initiating the reaction by adding the substrate. Control i ...
... conditions were not altered from the kinetic analyses, except that the mechanism-based inhibitors diethyldithiocarbamate, thio-TEPA, furafylline, and troleandomycin were preincubated for 20 min at 37°C with all incubation constituents before initiating the reaction by adding the substrate. Control i ...
Prodrugs—from Serendipity to Rational Design
... Acknowledgments . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . References . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . ...
... Acknowledgments . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . References . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . ...
Inhibition and induction of human cytochrome P450 (CYP) enzymes
... metabolic routes. It is also possible to use enzyme-speci® c antibodies and to test which metabolic routes are inhibited and to what extent by a particular anti-CYP antibody. In a panel of human liver microsomes it is possible to correlate the metabolism of a compound under study with the activities ...
... metabolic routes. It is also possible to use enzyme-speci® c antibodies and to test which metabolic routes are inhibited and to what extent by a particular anti-CYP antibody. In a panel of human liver microsomes it is possible to correlate the metabolism of a compound under study with the activities ...
In vitro metabolism and drug-drug interaction potential of irosustat, a
... sequence identity. Each family is divided into subfamilies indicated by a capital letter (i.e. CYP2C, CYP3A). Each subfamily contains members with more than 55% amino acid sequence identity but coded by separate genes. Members can be further subdivided into allele or variant categories. Alleles are ...
... sequence identity. Each family is divided into subfamilies indicated by a capital letter (i.e. CYP2C, CYP3A). Each subfamily contains members with more than 55% amino acid sequence identity but coded by separate genes. Members can be further subdivided into allele or variant categories. Alleles are ...