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Copyright of Congreso Internacional de Investigacion Academia Journals is the property of PDHTech, LLC and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Congreso Internacional de Investigacion Academia Journals is the property of PDHTech, LLC and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Congreso Internacional de Investigacion Academia Journals is the property of PDHTech, LLC and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Congreso Internacional de Investigacion Academia Journals is the property of PDHTech, LLC and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Congreso Internacional de Investigacion Academia Journals is the property of PDHTech, LLC and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Composé tricyclique, Tricyclic compound, Compuesto tricíclico, Dérivé de la dibenzoazépine, Dibenzazepine derivatives, Dibenzoazepina derivado, Anticonvulsivant, Anticonvulsant, Anticonvulsivante, Antidépresseur, Antidepressant agent, Antidepresor, Carbamazépine, Carbamazepine, Carbamazepina, Chromatographie affinité, Affinity chromatography, Cromatografía afinidad, Cinétique, Kinetics, Cinética, Constante vitesse, Rate constant, Constante velocidad, Dissociation, Disociación, Détecteur UV, Ultraviolet detector, Detector UV, Fixation biologique, Biological fixation, Fijación biológica, Homme, Human, Hombre, Imipramine, Imipramina, Interaction moléculaire, Molecular interaction, Interacción molecular, Normothymique, Mood stabilizer, Estabilizador humor, Paramètre cinétique, Kinetic parameter, Parámetro cinético, Profil raie, Line shape, Perfil raya espectral, Protéine sérique, Serum protein, Proteína sérica, Psychotrope, Psychotropic, Psicotropo, Sérumalbumine, Serum albumin, Seroalbúmina, Drug-protein binding, High-performance affinity chromatography, Human serum albumin, Peak profiling, Sciences biologiques et medicales, Biological and medical sciences, Sciences medicales, Medical sciences, Pharmacologie. Traitements medicamenteux, Pharmacology. Drug treatments, Pharmacologie générale, General pharmacology, Pharmacocinétique. Pharmacogénétique. Interactions médicament-récepteur, Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions, Neuropharmacologie, Neuropharmacology, Psychoanaleptiques: stimulant snc, antidépresseur, nootrope, normothymique..., (maladie d'alzheimer), Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease), Anticonvulsivants. Antiépileptiques. Antiparkinsoniens, Anticonvulsants. Antiepileptics. Antiparkinson agents, Psychologie. Psychanalyse. Psychiatrie, Psychology. Psychoanalysis. Psychiatry, Psychopharmacologie, Psychopharmacology, Psychoanaleptiques: stimulant SNC antidépresseur, nootrope, normothymique…, Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer…, Biochemistry, molecular biology, biophysics, Biochimie, biologie moléculaire, biophysique, Analytical chemistry, Chimie analytique, Pharmacology drugs, Pharmacologie, galénique, and Pollution

Carbamazepine and imipramine are drugs that have significant binding to human serum albumin (HSA), the most abundant serum protein in blood and a common transport protein for many drugs in the body. Information on the kinetics of these drug interactions with HSA would be valuable in understanding the pharmacokinetic behavior of these drugs and could provide data that might lead to the creation of improved assays for these analytes in biological samples. In this report, an approach based on peak profiling was used with high-performance affinity chromatography to measure the dissociation rate constants for carbamazepine and imipramine with HSA. This approach compared the elution profiles for each drug and a non-retained species on an HSA column and control column over a board range of flow rates. Various approaches for the corrections of non-specific binding between these drugs and the support were considered and compared in this process. Dissociation rate constants of 1.7 (±0.2) s―1 and 0.67 (±0.04)s―1 at pH 7.4 and 37 C were estimated by this approach for HSA in its interactions with carbamazepine and imipramine, respectively. These results gave good agreement with rate constants that have determined by other methods or for similar solute interactions with HSA. The approach described in this report for kinetic studies is not limited to these particular drugs or HSA but can also be extended to other drugs and proteins.

Carboxylic ester hydrolases, Enzyme, Enzima, Esterases, Hydrolases, Alcaloïde, Alkaloid, Alcaloide, Antialzheimer, Antialzheimer agent, Anticholinestérasique, Anticholinesterase agent, Anticolinesterasa agente, Bioréacteur, Bioreactor, Biorreactor, Carbamate organique, Organic carbamate, Carbamato orgánico, Cholinesterase, Chromatographie HPLC, HPLC chromatography, Cromatografía HPLC, Cinétique, Kinetics, Cinética, Colonne monolithique, Monolithic column, Columna monolítica, Composé aromatique, Aromatic compound, Compuesto aromático, Composé tricyclique, Tricyclic compound, Compuesto tricíclico, Enzyme immobilisée, Immobilized enzyme, Enzima inmovilizada, Homme, Human, Hombre, Hétérocycle azote, Nitrogen heterocycle, Heterociclo nitrógeno, In vitro, Inhibiteur enzyme, Enzyme inhibitor, Inhibidor enzima, Relation structure activité, Structure activity relation, Relación estructura actividad, Réseau diode, Diode array, Red diodo, Spectrométrie UV visible, Ultraviolet visible spectrometry, Espectrometría UV visible, Physostigmine dérivé, Pyrrolo[2,3-b]indole dérivé, Pyrroloindole, Covalent immobilization, Cymserine, Human butyrylcholinesterase, Kinetic constants, Monolithic disks, On-line studies, Phenserine, Pseudo-irreversible inhibitors, Sciences biologiques et medicales, Biological and medical sciences, Sciences medicales, Medical sciences, Pharmacologie. Traitements medicamenteux, Pharmacology. Drug treatments, Neuropharmacologie, Neuropharmacology, Psychoanaleptiques: stimulant snc, antidépresseur, nootrope, normothymique..., (maladie d'alzheimer), Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease), Psychologie. Psychanalyse. Psychiatrie, Psychology. Psychoanalysis. Psychiatry, Psychopharmacologie, Psychopharmacology, Psychoanaleptiques: stimulant SNC antidépresseur, nootrope, normothymique…, Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer…, Biochemistry, molecular biology, biophysics, Biochimie, biologie moléculaire, biophysique, Analytical chemistry, Chimie analytique, Pharmacology drugs, Pharmacologie, galénique, and Pollution

Focus of this work was the development and characterization of a new immobilized enzyme reactor (IMER) containing human recombinant butyrylcholinesterase (rBChE) for the on-line kinetic characterization of specific, pseudo-irreversible and brain-targeted BChE inhibitors as potential drug candidates for Alzheimer's disease (AD). Specifically, a rBChE-IMER containing 0.99 U of covalently bound target enzyme was purposely developed and inserted into a HPLC system connected to a UV-vis detector. Selected reversible cholinesterase inhibitors, (-)-phenserine and (-)-cymserine analogues, were then kinetically characterized by rBChE-IMER, and by classical in solution assays and their carbamoylation and decarbamoylation constants were determined. The results support the elucidation of the potency, inhibition duration, mode of action and specific structure/activity relations of these agents and allow cross-validation of the two assay techniques.

Carboxylic ester hydrolases, Encéphale pathologie, Cerebral disorder, Encéfalo patología, Enzyme, Enzima, Esterases, Hydrolases, Maladie dégénérative, Degenerative disease, Enfermedad degenerativa, Système nerveux central pathologie, Central nervous system disease, Sistema nervosio central patología, Système nerveux pathologie, Nervous system diseases, Sistema nervioso patología, Acetylcholinesterase, Cinétique, Kinetics, Cinética, Conformation, Conformación, Cristallographie, Crystallography, Cristalografía, Démence Alzheimer, Alzheimer disease, Demencia Alzheimer, Hydrolyse, Hydrolysis, Hidrólisis, Structure 3 dimensions, Three dimensional structure, Estructura 3 dimensiones, Structure moléculaire, Molecular structure, Estructura molecular, Substrat, Substrate, Substrato, Traitement, Treatment, Tratamiento, Acétylcholinestérase, Cristallographie cinétique, Maladie d'Alzheimer, Paysage conformationnel, Trafic de substrats et produits, Sciences biologiques et medicales, Biological and medical sciences, Sciences biologiques fondamentales et appliquees. Psychologie, Fundamental and applied biological sciences. Psychology, Biochimie analytique, structurale et metabolique, Analytical, structural and metabolic biochemistry, Enzymes et inhibiteurs d'enzymes, Enzymes and enzyme inhibitors, Transférases, Transferases, Sciences medicales, Medical sciences, Neurologie, Neurology, Maladies dégénératives et hérédodégénératives du système nerveux. Leucodystrophies. Maladies à prions, Degenerative and inherited degenerative diseases of the nervous system. Leukodystrophies. Prion diseases, Psychopathologie. Psychiatrie, Psychopathology. Psychiatry, Etude clinique de l'adulte et de l'adolescent, Adult and adolescent clinical studies, Troubles mentaux organiques. Neuropsychologie, Organic mental disorders. Neuropsychology, Psychologie. Psychanalyse. Psychiatrie, Psychology. Psychoanalysis. Psychiatry, PSYCHOPATHOLOGIE. PSYCHIATRIE, Pharmacology drugs, and Pharmacologie, galénique

L'acétylcholinestérase est une enzyme très rapide, essentielle à la neurotransmission cholinergique. Elle est la cible de toutes les molécules actuellement utilisées dans le traitement de la maladie d'Alzheimer, et les progrès à venir dans la modulation de son activité ont besoin d'une connaissance plus fine de sa structure et de sa dynamique. L'exploration du paysage conformationnel d'une protéine par la méthode de cristallographie aux rayons X réclame l'utilisation d'astuces expérimentales afin de dépasser la nature généralement statique des résultats obtenus. Nous présentons ici trois approches expérimentales ayant permis d'obtenir des informations structurales sur la dynamique de l'acétylcholinestérase, lesquelles sont importantes, puisque pertinentes, pour le structure-based drug-design.

Analyse sensorielle, Sensory analysis, Análisis sensorial, Arôme, Aroma, Carraghénane, Carrageenan, Carragenano, Chromatographie phase gazeuse, Gas chromatography, Cromatografía fase gaseosa, Cinétique, Kinetics, Cinética, Emulsifiant, Emulsifier, Emulsionador, Espace tête, Headspace, Espacio cabeza, Libération, Release, Liberación, Olfaction, Olfación, Perception sensorielle, Sensorial perception, Percepción sensorial, Polyoside, Polysaccharide, Poliósido, Propriété rhéologique, Rheological properties, Propiedad reológica, Texture, Textura, Transfert masse, Mass transfer, Transferencia masa, aroma release, carrageenans, gels, headspace analysis, mass transfer, partitioning, sensory analysis, Sciences biologiques et medicales, Biological and medical sciences, Sciences biologiques fondamentales et appliquees. Psychologie, Fundamental and applied biological sciences. Psychology, Industries agroalimentaires, Food industries, Industries des arômes, Aroma and flavouring agent industries, Food science technology, Sciences technologies alimentaires, Chemical industry parachemical industry, and Industrie chimique et parachimique

Different model food systems were made with iota- and kappa-carrageenans. Their viscoelastic characteristics were determined and four different systems were classified according to their gel strength by a sensory panel. The sensory results were in total agreement with the rheological parameters (storage and loss modulus). Flavour molecules from different chemical classes and with different chain lengths for the same chemical class were then incorporated in two of the most different systems. These samples were compared for their ortho- and retronasal intensities. No significant difference was perceived in odour intensity, except for ethyl hexanoate, which was found to be retained by iotacarrageenans. Nevertheless, in-mouth aroma perception was significantly different between the two systems. Aroma was perceived more intensely in the less firm system. The release kinetic results are interpreted in terms of partition and mass transfer coefficients. Sensory differences are not totally explained by physicochemical results, which suggests that interactions between senses may occur.

Air expiré, Expired air, Aire expirado, Arôme, Aroma, Cinétique, Kinetics, Cinética, Composé volatil, Volatile compound, Compuesto volátil, Ionisation chimique, Chemical ionization, Ionización química, Libération, Release, Liberación, Long terme, Long term, Largo plazo, Persistance, Persistence, Persistencia, Pression atmosphérique, Atmospheric pressure, Presión atmosférica, Spectrométrie masse, Mass spectrometry, Espectrometría masa, APCI-MS, MS Nose, aroma, flavour release, nasal mucosa, odorant transport, respiration, Sciences biologiques et medicales, Biological and medical sciences, Sciences biologiques fondamentales et appliquees. Psychologie, Fundamental and applied biological sciences. Psychology, Vertebres: systeme respiratoire, Vertebrates: respiratory system, Appareil respiratoire: anatomie, métabolisme, échanges gazeux, mécanique ventilatoire, hémodynamique respiratoire, Respiratory system: anatomy, metabolism, gas exchange, ventilatory mechanics, respiratory hemodynamics, Respiration aérienne, Air breathing, Food science technology, Sciences technologies alimentaires, Chemical industry parachemical industry, and Industrie chimique et parachimique

The long-term persistence of five volatiles in the breath was studied to determine the effects of respiration and the physical properties of each of the volatiles. The long-term persistence of each of the volatiles in the breath was modelled successfully and used to show that the breath volatile concentration 1 min after consuming the solution was greater when panelists exhaled at a slower rate. The air-water partition coefficient (Kaw) was influential in controlling the initial stages of persistence; compounds with a higher Kaw were found to decay at a much faster rate than compounds with a low Kaw. The decay rate during the later stages was constant for all the volatiles, which indicates that the rate-limiting factor during the later stages of persistence does not depend on the individual properties of the volatiles.