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Blocking Properties (blocking + property)
Selected AbstractsEffects of labedipinedilol-A, third-generation dihydropyridine-type calcium blocker, on ouabain-induced arrhythmiaDRUG DEVELOPMENT RESEARCH, Issue 1 2008Jhy-Chong Liang Abstract Labedipinedilol-A, a novel dihydropyridine-type calcium antagonist with ,/,-adrenoceptor blocking properties, has been reported to produce a cardioprotective effect against ischemia reperfusion injury in rats. We investigated the protective effects of labedipinedilol-A on ouabain-induced tonotropy and arrhythmias in isolated whole atria, and using patch-clamp techniques to study the underlying mechanism of its antiarrhythmic activity on isolated cardiac myocytes. Labedipinedilol-A (10,µM) suppressed the tonotropic effect of ouabain significantly and prolonged the onset time of extra-systole (arrhythmia) induced by ouabain in isolate atria. In the voltage-clamp study, labedipinedilol-A (1,100,µM) reduced the peak amplitude of sodium inward current (INa) and L-type calcium current (ICa-L), and shifted the current-voltage (I-V) curve upward in a concentration-dependent manner. In contrast, the addition of labedipinedilol-A increased transient outward potassium current (Ito) and inward rectifier potassium current (IK1) significantly. Labedipinedilol-A (10,µM) also effectively depressed the isoproterenol-induced increase in the Ca2+ current. These results show that labedipinedilol-A blocks ICa-L and INa, and increases Ito and IK1. These findings indicate that labedipinedilol-A produces direct cardiac action, probably due to the inhibition of cardiac Na+ and Ca2+ channels. Our results suggest that labedipinedilol-A may reduce the membrane conduction through inhibition of ionic channels which decrease ouabain-induced arrhythmia. Drug Dev Res 69:26,33, 2008 © 2008 Wiley-Liss, Inc. [source] Doping of the Metal Oxide Nanostructure and its Influence in Organic ElectronicsADVANCED FUNCTIONAL MATERIALS, Issue 8 2009Mi-Hyae Park Abstract Synthesizing metal oxides through the sol,gel process provides a convenient way for forming a nanostructured layer in wide band gap semiconductors. In this paper, a unique method of introducing dopants into the metal oxide semiconductor is presented. The doped TiO2 is prepared by adding a Cs2CO3 solution to a nanocrystalline TiO2 solution that is synthesized via a non-hydrolytic sol,gel process. The properties of the TiO2:Cs layer are investigated and the results show stable nanostructure morphology. In addition to providing morphological stability, Cs in TiO2 also gives rise to a more desirable work function for charge transport in organic electronics. Polymer solar cells based on the poly(3-hexylthiophene) (P3HT): methanofullerene (PC70BM) system with the addition of a TiO2:Cs interfacial layer exhibit excellent characteristics with a power conversion efficiency of up to 4.2%. The improved device performance is attributed to an improved polymer/metal contact, more efficient electron extraction, and better hole blocking properties. The effectiveness of this unique functionality also extends to polymer light emitting devices, where a lower driving voltage, improved efficiency, and extended lifetime are demonstrated. [source] Extracellular Acidosis Modulates Drug Block of Kv4.3 Currents by Flecainide and QuinidineJOURNAL OF CARDIOVASCULAR ELECTROPHYSIOLOGY, Issue 6 2003Suresh Singarayar M.D. Introduction: As a molecular model of the effect of ischemia on drug block of the transient outward potassium current, the effect of acidosis on the blocking properties of flecainide and quinidine on Kv4.3 currents was studied. Methods and Results: Kv4.3 channels were stably expressed in Chinese hamster ovary cells. Whole-cell, voltage clamp techniques were used to measure the effect of flecainide and quinidine on Kv4.3 currents in solutions of pH 7.4 and 6.0. Extracellular acidosis attenuated flecainide block of Kv4.3 currents, with the IC50 for flecainide (based on current-time integrals) increasing from7.8 ± 1.1 ,Mat pH 7.4 to125.1 ± 1.1 ,Mat pH 6.0. Similar effects were observed for quinidine (IC50 5.2 ± 1.1 ,Mat pH 7.4 and22.1 ± 1.3 ,Mat pH 6.0). Following block by either drug, Kv4.3 channels showed a hyperpolarizing shift in the voltage sensitivity of inactivation and a slowing in the time to recover from inactivation/block that was unaffected by acidosis. In contrast, acidosis attenuated the effects on the time course of inactivation and the degree of tonic- and frequency-dependent block for both drugs. Conclusion: Extracellular acidosis significantly decreases the potency of blockade of Kv4.3 by both flecainide and quinidine. This change in potency may be due to allosteric changes in the channel, changes in the proportion of uncharged drug, and/or changes in the kinetics of drug binding or unbinding. These findings are in contrast to the effects of extracellular acidosis on block of the fast sodium channel by these agents and provide a molecular mechanism for divergent modulation of drug block potentially leading to ischemia-associated proarrhythmia.(J Cardiovasc Electrophysiol, Vol. 14, pp. 641-650, June 2003) [source] Association between amantadine and the onset of dementia in Parkinson's diseaseMOVEMENT DISORDERS, Issue 9 2006Rivka Inzelberg MD Abstract The objective of this study is to compare the occurrence of dementia among Parkinson's disease (PD) patients treated with amantadine (AM group) with those never exposed to it (NoAM group). PD dementia shares neuroanatomical and biochemical similarities with Alzheimer's disease (AD). Memantine, an N -methyl- D -aspartate (NMDA) receptor antagonist has been shown to be beneficial in AD. Memantine is a dimethyl derivative of amantadine, which also possesses NMDA receptor blocking properties. We hypothesized that amantadine could have a beneficial effect on the occurrence of PD dementia. PD patients attending the Movement Disorders Clinics in Hillel Yaffe, Asaf Harofe Medical Centers (Israel) and Pisa (Italy) were included. Taking the onset of dementia as the endpoint, survival curves for AM and NoAM patients were estimated by the Kaplan,Meier method. The study population consisted of 593 patients (age, 69.5 ± 9.9 years; PD duration, 9.2 ± 6.0 years; 263 patients (44%) amantadine treated). The endpoint of dementia was reached by 116 patients (20%). PD duration until dementia was significantly longer for AM patients (9.1 ± 5.7 years) than for NoAM patients (5.9 ± 4.6 years, P = 0.006). The duration of amantadine exposure positively correlated with PD duration until dementia (P = 0.0001). Survival analysis, taking dementia onset as endpoint, showed slower mental decline in AM patients (Log rank P = 0.0049, Wilcoxon P = 0.0024). Mini-Mental State Examination scores were significantly higher for AM patients than for the NoAM group (P = 0.01). Age of PD onset also significantly influenced the duration of PD until dementia. Amantadine use may delay the onset of dementia in PD patients and may attenuate its severity. © 2006 Movement Disorder Society [source] The gel swelling properties of alginate fibers and their applications in wound managementPOLYMERS FOR ADVANCED TECHNOLOGIES, Issue 1 2008Yimin Qin Abstract Calcium alginate fibers have a novel gel-forming capability in that, upon the ion exchange between sodium ions in the contact solution and calcium ions in the fiber, the fiber slowly transforms into a fibrous gel. This paper reviews the principles of the gel-forming process for alginate fibers and analyzed the gelling behavior of various types of alginate fibers. The absorption characteristics of alginate wound dressings were analyzed and it was found that alginate wound dressings absorb a large quantity of liquid into the fiber structure, in addition to those held between the fibers in the textile structure. This gives rise to the unique gel blocking properties of alginate wound dressings. In addition, alginate wound dressings also have novel hemostatic and antimicrobial properties as well as the ability to promote wound healing. They are now widely used in the management of highly exuding wounds such as leg ulcers, pressure sores, and surgical wounds. Copyright © 2007 John Wiley & Sons, Ltd. [source] Fabrication of Patterned Polydiacetylene Composite Films Using a Replica-Molding (REM) TechniqueMACROMOLECULAR RAPID COMMUNICATIONS, Issue 3 2010Oktay Yarimaga Abstract Functional three-dimensional (3D) micropatterns of diacetylene supramolecules embedded in a host polymer have been successfully fabricated by a replica-molding (REM) technique. Dimensional reduction as a result of liquid evaporation during the curing process does not affect the conformational features of the transferred patterns. Polymerization of the diacetylene vesicles using 254,nm UV-light irradiation from the back-side of the transparent substrate induces blue colored polydiacetylene (PDA) micro-images. Interestingly, the polymerization selectively occurs in the molded areas because of the sub-300,nm light blocking property of SU-8. 3D fluorescence patterns are readily obtained by heat treatment of the blue images on the film. [source] | |||||||||||||