Search results for "Azide"
showing 10 items of 334 documents
Antihypertensive efficacy and effects of nitrendipine on cardiac and renal hemodynamics in mild to moderate hypertensive patients: Randomized control…
1992
In this study antihypertensive efficacy, safety, and the effects of short-term nitrendipine administration on central and renal hemodynamics were evaluated in mild to moderate hypertensives. Our final goal was to ascertain whether the reduction in blood pressure induced by nitrendipine treatment was associated with maintained renal function. After a run-in period with placebo, 26 hypertensives without cardiac or renal disease were randomly assigned to a double-blind 8-week controlled trial with nitrendipine (N) 20 mg once a day (13 pts) or hydrochlorothiazide (HCT) 25 mg once a day (13 pts). Renal hemodynamic measurements included effective renal plasma flow (ERPF) and glomerular filtration…
Effects of cilazapril on renal haemodynamics and function in hypertensive patients: a randomised controlled study versus hydrochlorothiazide.
1995
In this study the efficacy and safety of short-term cilazapril administration on renal haemodynamics were evaluated in mild to moderate hypertensive subjects. Our final goal was to evaluate whether the reduction in blood pressure achieved by treatment was associated with maintained renal function. After a run-in period with placebo, 40 hypertensive subjects without renal or cardiac diseases were randomly allocated to a double-blind 4 week controlled trial with cilazapril 5 mg once a day (20 patients) or hydrochlorothiazide 25 mg once a day (20 patients). Renal haemodynamics measurements included effective renal plasma flow (ERPF) and glomerular filtration rate (GFR) by radionuclide study us…
Screening of pharmacologic adulterant classes in herbal formulations using voltammetry of microparticles.
2013
A solid state electrochemical method for screening different families of adulterant chemicals illegally added to commercial phytotherapuetic formulations is described. The proposed method, based on the voltammetry of microparticles approach, permits a fast and sensitive way to distinguish between anorexics (amfepramone, fenproporex, sibutramine), benzozodiazepinic anxiolytics (clonazepam, flurazepam, alprazolam, midazolam, medazepam, chlordiazepoxide, diazepam), antidepressants (bupropione, fluoxetine, sertraline, paroxetine), diuretics (hydrochlorothiazide, furosemide, chlortalidone, amiloride, spironolactone), and hypoglycemics (glimepiride, chlorpropamide, glibenclamide) based on charact…
Actions of two GABAA receptor benzodiazepine-site ligands that are mediated via non-γ2-dependent modulation.
2011
The potent sedative-hypnotic zolpidem and the convulsant methyl-6,7-dimethoxy-4-ethyl-β-carboline-3-carboxylate (DMCM) act primarily by binding to the benzodiazepine site of the main inhibitory neurotransmitter receptor, the pentameric γ-aminobutyric acid type A receptor (GABA(A)). This binding depends critically on the wild-type F77 residue of the GABA(A) receptor γ2 subunit. Mice with γ2 subunit F77I point mutation (γ2I77 mouse line) lose the high-affinity nanomolar binding of these ligands as well as their most robust behavioral actions at low doses. Interestingly, the γ2I77 mice offer a tool to study the actions of these substances mediated via other possible binding sites of the GABA(A…
Manejo de la hiperglucemia con fármacos no insulínicos en pacientes adultos con diabetes tipo 2
2019
Resumen: El adecuado tratamiento de la diabetes mellitus tipo 2 (DM2) incluye la alimentación saludable y el ejercicio (150 min/semana) como pilares básicos. Para el tratamiento farmacológico, la metformina es el fármaco de elección inicial, salvo contraindicación o intolerancia; en caso de mal control, se dispone de 8 familias terapéuticas (6 orales y 2 inyectables) como posibles combinaciones. Se presenta un algoritmo y unas recomendaciones para el tratamiento de la DM2. En prevención secundaria cardiovascular se recomienda asociar un inhibidor del cotransportador sodio-glucosa tipo 2 (iSGLT2) o un agonista del receptor de glucagon-like peptide-1 (arGLP1) en pacientes con obesidad. En pre…
A multifunctional bioconjugate module for versatile photoaffinity labeling and click chemistry of RNA
2011
A multifunctional reagent based on a coumarin scaffold was developed for derivatization of naive RNA. The alkylating agent N3BC [7-azido-4-(bromomethyl)coumarin], obtained by Pechmann condensation, is selective for uridine. N3BC and its RNA conjugates are pre-fluorophores which permits controlled modular and stepwise RNA derivatization. The success of RNA alkylation by N3BC can be monitored by photolysis of the azido moiety, which generates a coumarin fluorophore that can be excited with UV light of 320 nm. The azidocoumarin-modified RNA can be flexibly employed in structure-function studies. Versatile applications include direct use in photo-crosslinking studies to cognate proteins, as dem…
Diastereoselective Synthesis of 2-Phenylselenenyl-1,3-anti-Diols and 2-Phenylselenenyl-1,3-anti-Azido-Alcohols via Hydroxy- and Azido-Selenenylation …
2005
A method to synthesize 2-phenylselenenyl-1,3-anti-diols and 2-phenyl- selenenyl-1,3-anti-azidoalcohols via hydroxy- or azido-selenenylation of trans-allylic alcohols is reported. Moreover, the first example of hydroxyl-selenenylation of an allylic azide is presented. Yields ranging from moderate to good and diastereomeric ratios up to 95:5 are achieved.
Thermodynamic parameters of the interaction between Co(II) bovine carbonic anhydrase and anionic inhibitors
1992
The pH dependence of the apparent affinity constants of perchlorate for cobalt(II)bovine carbonic anhydrase II has been measured by electronic absorption spectroscopy. The obtained data have been analyzed in terms of the ionization of two acidic groups of CoBCAII, and the affinity of perchlorate for the two water-containing species of the enzyme have been estimated. Furthermore, the affinity constants of nitrate, perchlorate, and azide for CoBCAII in the temperature range 5 degrees C-30 degrees C have been determined by spectrophotometric titrations at pH 7. The affinity constants for these ligands decrease with increasing temperatures. The temperature dependence of binding was used to esti…
Polyaspartylhydrazide Copolymer-Based Supramolecular Vesicular Aggregates as Delivery Devices for Anticancer Drugs
2008
In this paper we report on three different hydrophilic copolymers based on alpha,beta-polyaspartylhydrazide (PAHy) bearing butyric groups in the side chain (C 4) (PAHy-C 4) or a combination of butyric groups and positive charged residues ((carboxypropyl)trimethylammonium chloride, CPTACl) (PAHy-C 4-CPTA) that were synthesized and used for the preparation of new supramolecular vesicular aggregates (SVAs) containing gemcitabine as an antitumor drug. Gemcitabine-loaded SVAs containing synthesized PAHy derivatives were characterized from the physicochemical and technological point of view and the in vitro toxicity and anticancer activity on two different human cancer cell lines, i.e., CaCo-2 (h…
Dielectric Behavior of Aqueous Solutions of α,β-Poly(aspartyl hydrazide) and α,β-Poly(N-hydroxyethyl aspartamide): An Investigation of the Structural…
1994
The dielectric properties of aqueous solutions of α,β-poly(aspartyl hydrazide) (PAHy) and of α,β-poly( N-hydroxyethyl aspartamide) (PHEA) were measured at 25 ° C in the frequency range of 100 MHz to 15 GHz using a time domain reflection method (TDR). Single time relaxation processes were found at 2 GHz and 15 GHz, respectively. The low frequency dispersion was inter preted in terms of the dynamics of polymeric segments based on the dielectric relaxation strength and the relaxation time. The high frequency process which is attributed to the rotational relaxation of water, indicated that water mole cules surrounding the polymeric backbone and in the pure state have a similar rotational behav…