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Träfflista för sökning "hsv:(MEDICIN OCH HÄLSOVETENSKAP) hsv:(Medicinska och farmaceutiska grundvetenskaper) hsv:(Farmaceutiska vetenskaper) srt2:(2000-2009);srt2:(2008)"

Sökning: hsv:(MEDICIN OCH HÄLSOVETENSKAP) hsv:(Medicinska och farmaceutiska grundvetenskaper) hsv:(Farmaceutiska vetenskaper) > (2000-2009) > (2008)

  • Resultat 141-150 av 172
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141.
  • Rönn, Robert, et al. (författare)
  • Hepatitis C Virus NS3 Protease Inhibitors Comprising a Novel Aromatic P1 Moiety
  • 2008
  • Ingår i: Bioorganic & Medicinal Chemistry. - : Elsevier BV. - 0968-0896 .- 1464-3391. ; 16:6, s. 2955-2967
  • Tidskriftsartikel (refereegranskat)abstract
    • Inhibition of the hepatitis C virus (HCV) NS3 protease has emerged as an attractive approach to defeat the global hepatitis C epidemic. In this work, we present the synthesis and biochemical evaluation of HCV NS3 protease inhibitors comprising a non-natural aromatic P-1 moiety. A series of inhibitors with aminobenzoyl sulfonamides displaying submicromolar potencies in the full-length NS3 protease assay was prepared through a microwave-irradiated, palladium-catalyzed, amidocarbonylation protocol.
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142.
  • Rönn, Robert, et al. (författare)
  • New developments in the discovery of agents to treat hepatitis C
  • 2008
  • Ingår i: Current Topics in Medicinal Chemistry. - : Bentham Science Publishers Ltd.. - 1568-0266 .- 1873-4294. ; 8:7, s. 533-562
  • Forskningsöversikt (refereegranskat)abstract
    • Hepatitis C virus (HCV) has deceived researchers for seventeen years now and although the current therapy regimen has been optimized by the development of pegylated interferon-alpha and the addition of ribavirin, no new agent to treat HCV infected patients has yet reached the market. A new era is approaching the HCV research due to new developments for the propagation of the virus in a cell-based system, which may lead to new drug innovations. Efforts in the search of new treatments for HCV infected patients are either focused on direct antiviral drugs, targeting the structural components or enzymes encoded by the virus, or indirect antiviral drugs, targeting host cell components (immunomodulators etc.). An inspection of the drug pipeline for HCV reveals representatives from both classes and of different mechanisms of action. Among the direct acting antiviral agents, inhibitors of the NS3 protease, the NS5B polymerase, and the viral RNA are the most intensively explored. However, there is also on-going and promising preclinical research, in different stages, on other potential targets as the structural protein E2 (for cell-entry inhibitors), the NS3 helicase, the p7 ion-channel, and the multifunctional NS5A protein. The combat of HCV will certainly require a combination of drugs of different mechanisms in order to reduce the emergence of resistance. The latest developments in the discovery of agents to treat HCV are reviewed, with special focus on direct small-molecule antiviral drugs, from a medicinal chemistry perspective.
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143.
  • Saber, Amanj, 1972-, et al. (författare)
  • Middle Ear Application of Hyaluronic Acid Gel Loaded with Neomycin in a Guinea Pig Model
  • 2008
  • Konferensbidrag (refereegranskat)abstract
    • Background: One alternative for controlled drug delivery to the inner ear is application of medication to the middle ear cavity on the promise that it will diffuse through the round window membrane (RWM) into the inner ear.Objective: to evaluate the efficacy of hyaluronic acid gel (HYA) as a vehicle for drugs that are aimed to treat inner ear disorders.Methods: in this study the cochlear hair cell loss and RWM morphology were investigated after topical application. Neomycin was chosen as tracer for drug release and the ototoxic effect was evaluated. HYA, (0.5%) loaded with 3 different concentrations of neomycin, was injected to the middle ear cavity of guinea pigs. the ototoxic effect of neomycin in HYA gel was compared to that of neomycin solution applied to the middle ear cavity. Phalloidin stained surface preparation of the organ of Corti was used to estimate hair cell loss induced by neomycin. the thickness of the midportion of the RWM was measured and compared with that of controls using light and electrom microscope.Result: Neomycin induced a considerable hair cell loss in guinea pigs receiving middle ear injection of HYA loaded with the drug. One week after topical application the thickness of the RWM was dependent upon the concentration of neomycin administered to the middle ear. At 4 weeks the thickness of the RWM had returned to normal.Conclusion: HYA is a safe vehicle for drugs aimed to pass into the inner ear through the RWM. Neomycin was released from HYA and transported into the inner ear as evidenced by hair cell loss. Key words: Round window membrane (RWM), hyaluronic acid gel, HYA, hair cell loss, thickness.
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144.
  • Scholz, Birger, et al. (författare)
  • Striatal proteomic analysis suggests that first L-dopa dose equates to chronic exposure
  • 2008
  • Ingår i: PLoS ONE. - : Public Library of Science (PLoS). - 1932-6203. ; 3:2, s. e1589-
  • Tidskriftsartikel (refereegranskat)abstract
    • L-3,4-dihydroxypheylalanine (L-dopa)-induced dyskinesia represent a debilitating complication of therapy for Parkinson's disease (PD) that result from a progressive sensitization through repeated L-dopa exposures. The MPTP macaque model was used to study the proteome in dopamine-depleted striatum with and without subsequent acute and chronic L-dopa treatment using two-dimensional difference in-gel electrophoresis (2D-DIGE) and mass spectrometry. The present data suggest that the dopamine-depleted striatum is so sensitive to de novo L-dopa treatment that the first ever administration alone would be able (i) to induce rapid post-translational modification-based proteomic changes that are specific to this first exposure and (ii), possibly, lead to irreversible protein level changes that would be not further modified by chronic L-dopa treatment. The apparent equivalence between first and chronic L-dopa administration suggests that priming would be the direct consequence of dopamine loss, the first L-dopa administrations only exacerbating the sensitization process but not inducing it.
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145.
  • Siegel, G., et al. (författare)
  • Ginkgo biloba and its Influence on Nanoplaque Formation and Vascular Function
  • 2008
  • Ingår i: Diabetes stoffwechsel und herz. - 1861-7603. ; 17, s. S23-S35
  • Tidskriftsartikel (refereegranskat)abstract
    • Background: In a pilot study, we demonstrated the beneficial effects of Ginkgo biloba (EGb 761) on atherosclerotic nanoplaque formation and size, the oxLDL/LDL quotient and the lipoprotein(a) concentration, the increase in superoxide dismutase activity, as well as the cAMP and cGMP concentrations. Method: The measurable variables formerly used were supplemented by a biomarker spectrum, through which the latest parameter and markers of plaque stability and progression, oxidative stress, and inflammation could be determined. Results: In 11 patients with early-stage metabolic syndrome, atherosclerotic nanoplaque formation fell by 14.3 +/- 2.9 (p < 0.0077) and nanoplaque size by 23.4 +/- 3.7 % (p < 0.0004), respectively, after a two-month regime with Ginkgo biloba extract. Superoxide dismutase and glutathione peroxidase (GPx) activities were upregulated by 19.6 +/- 10.0 % (p < 0.0785) and 11.6 +/- 2.3 % (p < 0.001), respectively. The quotient oxLDL/LDL fell by 21.0 +/- 4.3 % (p < 0.002), and lipoprotein(a) concentration by 26.3 t 4.8 % (p < 0.001). The concentrations of cAMP and cGMP were augmented by43.5 12.0% (p < 0.001)and 32.9 +/- 10.4% (p < 0.001), respectively. The serum Call concentration fell by 5.4 +/- 1.6 % (p < 0.0076). We could also show a favourable development of 8-iso-PGF(2 alpha), oxLDL/LDL, SOD, GPx, hsCRP MPO,TNF alpha, TGF beta(1), and MMP-9. Conclusion: Ginkgo with its pleiotropic effects should be assigned a fixed rank among the anti-ageing medical therapeutics.
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146.
  • Silwer, Louise, et al. (författare)
  • Prevalence of purchase of antihypertensive and serum lipid-reducing drugs in Sweden : individual data from national registers
  • 2008
  • Ingår i: Pharmacoepidemiology and Drug Safety. - Chichester, West Sussex : John Wiley & Sons. - 1053-8569 .- 1099-1557. ; 17:1, s. 37-42
  • Tidskriftsartikel (refereegranskat)abstract
    • PURPOSE: To determine the prevalence of purchase of prescribed antihypertensive and/or serum lipid-reducing pharmaceutical preparations among different age groups, from the age of 45, in the Swedish population. Further, to calculate the percentage of the population, from the age of 60, who purchased these pharmaceuticals without having had a circulatory diagnosis in the Hospital Discharge Register the last 7 years, or having purchased nitrate vasodilators, as an attempt to estimate the proportion of primary preventive treatments. METHODS: A cross-sectional study, of individual data on prescriptions for antihypertensives (C02-C03, C07-C09) and serum lipid-reducing agents (C10), dispensed from July to December 2005 for the Swedish population. Data were obtained from the new Swedish Prescribed Drugs Register. The data were related to population statistics, and linked to data on diagnoses of cardiovascular disease (I00-I99), from the Swedish Hospital Discharge Register 1998-2004. Data on individuals with purchase of antihypertensive or serum lipid-reducing agents, but without a diagnosis of cardiovascular disease, were also linked to purchase of nitrate vasodilators (C01D). RESULTS: Among Swedes of 60 years and above, 53% purchased antihypertensive or serum lipid-reducing pharmaceuticals, and 30% purchased the pharmaceuticals without having been hospitalized for a coronary or cerebrovascular event during the previous 7 years, or having purchased prescribed nitrate vasodilators during 6 months. CONCLUSION: Over half of the Swedish senior population purchased prescribed antihypertensive or serum lipid-reducing drugs during 6 months in 2005. The magnitude of the prevalence points to the importance of intensified follow-up of both adverse effects and of effectiveness of these drugs.
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147.
  • Sjödin, Elin, et al. (författare)
  • Intestinal and hepatobiliary transport of ximelagatran and its metabolites in pigs
  • 2008
  • Ingår i: Drug Metabolism And Disposition. - : American Society for Pharmacology & Experimental Therapeutics (ASPET). - 0090-9556 .- 1521-009X. ; 36:8, s. 1519-1528
  • Tidskriftsartikel (refereegranskat)abstract
    • The direct thrombin inhibitor melagatran is formed from ximelagatran via two intermediate metabolites, OH-melagatran and ethylmelagatran. The biotransformation of ximelagatran does not involve cytochrome P450 isoenzymes, and it has been suggested that a reported interaction with erythromycin may instead be mediated by transport proteins. A pig model that simultaneously enables bile collection, sampling from three blood vessels and perfusion of a jejunal segment, was used to investigate the biotransformation of ximelagatran and the effect of erythromycin on the intestinal and hepatobiliary transport of ximelagatran and its metabolites. The pigs received enteral ximelagatran (n = 6), enteral ximelagatran together with erythromycin (n = 6), i.v. ximelagatran (n = 4), or i.v. melagatran (n = 4). The plasma exposure of the intermediates was found to depend on the route of ximelagatran administration. Erythromycin increased the area under the plasma concentration-time curve (AUC) of melagatran by 45% and reduced its biliary clearance from 3.0 +/- 1.3 to 1.5 +/- 1.1 ml/min/kg. Extensive biliary exposure of melagatran and ethylmelagatran, mediated by active transport, was evident from the 100- and 1000-fold greater AUC, respectively, in bile than in plasma. Intestinal efflux transporters seemed to be of minor importance for the disposition of ximelagatran and its metabolites considering the high estimated f(abs) of ximelagatran (80 +/- 20%) and the negligible amount of the compounds excreted in the perfused intestinal segment. These findings suggest that transporters located at the sinusoidal and/or canalicular membranes of hepatocytes determine the hepatic disposition of ximelagatran and its metabolites, and are likely to mediate the ximelagatran-erythromycin pharmacokinetic interaction.
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148.
  • Sjögren, M., et al. (författare)
  • Antifouling activity of the sponge metabolite agelasine D and synthesised analogs on Balanus improvisus
  • 2008
  • Ingår i: Biofouling. - : Informa UK Limited. - 0892-7014 .- 1029-2454. ; 24:4, s. 251-258
  • Tidskriftsartikel (refereegranskat)abstract
    • This study reports a screening study for antifouling (AF) activity of the natural compound agelasine D isolated from marine sponges of the genus Agelas and 20 synthesised analogs of agelasines and agelasimines. Agelasine D, together with two of the analogs, ie AV1003A and AKB695, displayed a strong inhibitory effect on settlement of Balanus improvisus cypris larvae. Agelasine D had an EC50 value of 0.11 mu M while the two analogs AV1033A and AKB695 had EC50 values of 0.23 and 0.3 mu M, respectively. None of these three compounds affected larval mortality as was the case with several of the analogs tested. Moreover, the effect of AV1033A and AKB695 was reversible. When cyprids after 24 h exposure to the compounds were transferred to fresh seawater, the settlement frequency compared with the controls was completely recovered. The properties of the agelasine D analogs AV1003A and AKB695 make them highly attractive candidates as AF agents in future marine coatings.
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149.
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150.
  • Skårberg, Kurt, et al. (författare)
  • The development of multiple drug use among anabolic-androgenic steroid users : six subjective case reports
  • 2008
  • Ingår i: Substance Abuse Treatment, Prevention, and Policy. - London : BioMed Central. - 1747-597X. ; 3, s. 24-
  • Tidskriftsartikel (refereegranskat)abstract
    • BACKGROUND: The inappropriate use of anabolic androgenic steroids (AAS) was originally a problem among athletes but AAS are now often used in nonsport situations and by patients attending regular addiction clinics. The aim of this study was to improve understanding of the development of multiple drug use in patients seeking treatment at an addiction clinic for AAS-related problems. METHODS: We interviewed six patients (four men and two women) with experience of AAS use who were attending an addiction clinic for what they believed were AAS-related problems. The patients were interviewed in-depth about their life stories, with special emphasis on social background, substance use, the development of total drug use and subjective experienced psychological and physical side effects. RESULTS: There was significant variation in the development of drug use in relation to social background, onset of drug use, relationship to AAS use and experience of AAS effects. All patients had initially experienced positive effects from AAS but, over time, the negative experiences had outweighed the positive effects. All patients were dedicated to excess training and took AAS in combination with gym training, indicating that the use of these drugs is closely related to this form of training. Use of multiple drugs was common either in parallel with AAS use or serially. CONCLUSIONS: The study shows the importance of understanding how AAS use can develop either with or without the concomitant use of other drugs of abuse. The use of AAS can, however, progress to the use of other drugs. The study also indicates the importance of obtaining accurate, comprehensive information about the development of AAS use in designing treatment programmes and prevention strategies in this area.
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