Search results for "Kinetic"
showing 10 items of 3064 documents
Some aspects related to stability, critical concentrations and kinetics of flocculation of the calcium phytate colloid
1986
Abstract As 99mTcCa phytate is an important radiopharmaceutical and its colloidal nature presents problems, we investigated some of them. This work describes the study of the colloidal behaviour of the calcium phytate colloid in terms of its formation, stability and kinetics of flocculation. The study of spontaneous, and centrifugation-induced flocculation allows the determination of two critical concentrations of sol flocculation. The titrations of calcium phytate colloid at different concentrations provide information on the colloidal formation conditions. Moreover, a study on flocculation kinetics was made by turbidity measurements.
Binding of Cu2+, Zn2+, and Ni(2+)-GnRH complexes with the rat pituitary receptor.
1997
Complex of copper with the gonadotropin-releasing hormone, GnRH, competed more efficiently for the GnRH receptor than native GVRH, while complexes of nickel with GnRH and zinc with GnRH had slightly lower affinity. Copper ion added to the incubation mixture inhibited the buserelin binding to the receptor.
Molecular docking and oxidation kinetics of 3-phenyl coumarin derivatives by human CYP2A13
2021
CYP2A13 enzyme is expressed in human extrahepatic tissues, while CYP2A6 is a hepatic enzyme. Reactions catalysed by CYP2A13 activate tobacco-specific nitrosamines and some other toxic xenobiotics in lungs.To compare oxidation characteristics and substrate-enzyme active site interactions in CYP2A13 vs CYP2A6, we evaluated CYP2A13 mediated oxidation characteristics of 23 coumarin derivatives and modelled their interactions at the enzyme active site.CYP2A13 did not oxidise six coumarin derivatives to corresponding fluorescent 7-hydroxycoumarins. The Km-values of the other coumarins varied 0.85���97 ��M, Vmax-values of the oxidation reaction varied 0.25���60 min���1, and intrinsic clearance var…
In vitro glucuronidation of 7-hydroxycoumarin derivatives in intestine and liver microsomes of Beagle dogs
2019
Beagle dog is a standard animal model for evaluating nonclinical pharmacokinetics of new drug candidates. Glucuronidation in intestine and liver is an important first-pass drug metabolic pathway, especially for phenolic compounds. This study evaluated the glucuronidation characteristics of several 7-hydroxycoumarin derivatives in beagle dog's intestine and liver in vitro. To this end, glucuronidation rates of 7-hydroxycoumarin (compound 1), 7-hydroxy-4-trifluoromethylcoumarin (2), 6-methoxy-7-hydroxycoumarin (3), 7-hydroxy-3-(4-tolyl)coumarin (4), 3-(4-fluorophenyl)coumarin (5), 7-hydroxy-3-(4-hydroxyphenyl)coumarin (6), 7-hydroxy-3-(4-methoxyphenyl)coumarin (7), and 7-hydroxy-3-(1H-1,2,4-t…
Substrate Selectivity of Coumarin Derivatives by Human CYP1 Enzymes: In Vitro Enzyme Kinetics and In Silico Modeling
2021
Of the three enzymes in the human cytochrome P450 family 1, CYP1A2 is an important enzyme mediating metabolism of xenobiotics including drugs in the liver, while CYP1A1 and CYP1B1 are expressed in extrahepatic tissues. Currently used CYP substrates, such as 7-ethoxycoumarin and 7-ethoxyresorufin, are oxidized by all individual CYP1 forms. The main aim of this study was to find profluorescent coumarin substrates that are more selective for the individual CYP1 forms. Eleven 3-phenylcoumarin derivatives were synthetized, their enzyme kinetic parameters were determined, and their interactions in the active sites of CYP1 enzymes were analyzed by docking and molecular dynamic simulations. All cou…
Candida antarctica Lipase A-Based Enantiorecognition of a Highly Strained 4-Dibenzocyclooctynol (DIBO) Used for PET Imaging
2020
The enantiomers of aromatic 4-dibenzocyclooctynol (DIBO), used for radiolabeling and subsequent conjugation of biomolecules to form radioligands for positron emission tomography (PET), were separated by kinetic resolution using lipase A from Candida antarctica (CAL-A). In optimized conditions, (R)-DIBO [(R)-1, ee 95%] and its acetylated (S)-ester [(S)-2, ee 96%] were isolated. In silico docking results explained the ability of CAL-A to differentiate the enantiomers of DIBO and to accommodate various acyl donors. Anhydrous MgCl2 was used for binding water from the reaction medium and, thus, for obtaining higher conversion by preventing hydrolysis of the product (S)-2 into the starting materi…
External evaluation of population pharmacokinetic models of vancomycin in neonates: the transferability of published models to different clinical set…
2012
AimsVancomycin is one of the most evaluated antibiotics in neonates using modeling and simulation approaches. However no clear consensus on optimal dosing has been achieved. The objective of the present study was to perform an external evaluation of published models, in order to test their predictive performances in an independent dataset and to identify the possible study-related factors influencing the transferability of pharmacokinetic models to different clinical settings.MethodPublished neonatal vancomycin pharmacokinetic models were screened from the literature. The predictive performance of six models was evaluated using an independent dataset (112 concentrations from 78 neonates). T…
Modeling the influence of potassium content and heating rate on biomass pyrolysis
2017
This study presents a combined kinetic and particle model that describes the effect of potassium and heating rate during the fast pyrolysis of woody and herbaceous biomass. The model calculates the mass loss rate, over a wide range of operating conditions relevant to suspension firing. The shrinking particle model considers internal and external heat transfer limitations and incorporates catalytic effects of potassium on the product yields. Modeling parameters were tuned with experimentally determined char yields at high heating rates (>200 K s−1) using a wire mesh reactor, a single particle burner, and a drop tube reactor. The experimental data demonstrated that heating rate and potassium …
SIA “Kinetics Nail Systems” uzņēmējdarbības riski, finanšu analīze un novērtējums turpmākai uzņēmuma attīstībai
2019
Diplomdarba tēma ir “SIA “Kinetics Nail Systems” uzņēmējdarbības riski, finanšu analīze un novērtējums turpmākai uzņēmuma attīstībai”. Darbu veido ievads, trīs nodaļas, secinājumi un priekšlikumi. Diplomdarba mērķis ir apkopot uzņēmējdarbības risku un finanšu analīzes teorētiskos aspektus, lai veiktu SIA “Kinetics Nail Systems” uzņēmējdarbības risku novērtēšanu, finanšu analīzi, par iegūtajiem rezultātiem izdarītu secinājumus un izstrādātu priekšlikumus turpmākai uzņēmuma attīstībai. Darba izstrādes rezultātā secināts, ka SIA “Kinetics Nail Systems” ir pakļauts vairākiem uzņēmējdarbības riskiem, kā arī uzņēmuma finansiālais stāvoklis ir stabils, bet to iespējams uzlabot. Risku novēršanai un…
Physical chemical properties and kinetics of redox processes in water/soybean oil microemulsions
2008
Microemulsoes de agua em oleo (ME w/o) constituidas de agua, oleo de soja, SDS (dodecil sulfato de sodio) e diversos alcoois de cadeia curta foram caracterizadas sob o ponto de vista fisico-quimico e de propriedades eletroanaliticas. Foram testados diferentes co-surfactantes e razoes surfactante:cosurfactante, sendo a ME com a composicao mais favoravel utilizada para estudar a cinetica de processos redox. Para tanto, realizaram-se medidas de voltametria ciclica utilizando como eletrodo de trabalho um ultramicroeletrodo de disco de Pt e, como eletrodo de referencia e auxiliar, foram usados Ag/AgCl e Pt, respectivamente, e ferroceno como uma sonda. Verificou-se que a estabilidade termodinâmic…