Institution
Solvay
Company•Brussels, Belgium•
About: Solvay is a company organization based out in Brussels, Belgium. It is known for research contribution in the topics: Catalysis & Polymer. The organization has 6083 authors who have published 7004 publications receiving 105745 citations.
Topics: Catalysis, Polymer, Polymerization, Alkyl, Aqueous solution
Papers published on a yearly basis
Papers
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TL;DR: Replacement of the amidine -NH(2) moiety with a -NHCH(3) group proved to be the key change for gaining oral biovailability in this series of compounds leading to the identification of 80.
Abstract: A series of novel 3,4-diarylpyrazolines was synthesized and evaluated in cannabinoid (hCB(1) and hCB(2)) receptor assays. The 3,4-diarylpyrazolines elicited potent in vitro CB(1) antagonistic activities and in general exhibited high CB(1) vs CB(2) receptor subtype selectivities. Some key representatives showed potent pharmacological in vivo activities after oral dosing in both a CB agonist-induced blood pressure model and a CB agonist-induced hypothermia model. Chiral separation of racemic 67, followed by crystallization and an X-ray diffraction study, elucidated the absolute configuration of the eutomer 80 (SLV319) at its C(4) position as 4S. Bioanalytical studies revealed a high CNS-plasma ratio for the development candidate 80. Molecular modeling studies showed a relatively close three-dimensional structural overlap between 80 and the known CB(1) receptor antagonist rimonabant (SR141716A). Further analysis of the X-ray diffraction data of 80 revealed the presence of an intramolecular hydrogen bond that was confirmed by computational methods. Computational models and X-ray diffraction data indicated a different intramolecular hydrogen bonding pattern in the in vivo inactive compound 6. In addition, X-ray diffraction studies of 6 revealed a tighter intermolecular packing than 80, which also may contribute to its poorer absorption in vivo. Replacement of the amidine -NH(2) moiety with a -NHCH(3) group proved to be the key change for gaining oral biovailability in this series of compounds leading to the identification of 80.
188 citations
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TL;DR: In this paper, a phase diagram of PVDF/diluent is presented and the effect of different parameters such as polymer concentration, quenching temperature, air gap, and bore fluid temperature on the morphologies, properties, and water permeability of the PVDF membranes were investigated.
188 citations
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TL;DR: At subantihypertensive doses of moxonidine, an agent that reduces sympathetic activity, ameliorates renal structural and functional damage in SNX animals, possibly through central inhibition of efferent sympathetic nerve traffic.
Abstract: .: A potential role of the sympathetic nervous system in progression of renal failure has received little attention. This study examined whether nonhypotensive doses of moxonidine, an agent that reduces sympathetic activity, affects glomerulosclerosis, urine albumin excretion, and indices of renal handling of norepinephrine (NE) in subtotally nephrectomized (SNX) rats. Sprague Dawley rats were SNX or sham-operated (control). SNX rats were either left untreated or treated with moxonidine in a dose (1.5 mg/kg body wt per d) that did not modify telemetrically monitored 24-h BP. Glomerular and renal morphology were evaluated by quantitative histology, immunohistochemistry, and in situ hybridization. Urine albumin excretion rate was analyzed by enzyme-linked immunosorbent assay, and kidney angiotensin II and NE content were measured using HPLC, (3)H-NE uptake, and release. Body and kidney weight and BP were not significantly different between SNX with or without moxonidine. The glomerulosclerosis index was significantly lower in moxonidine-treated (0.88 +/- 0.09) compared with untreated (1.55 +/- 0.28) SNX rats, as was the index of vascular damage (0.32 +/- 0.14 versus 0.67 +/- 0.16). The number of proliferating cell nuclear antigen-positive glomerular and tubular cells per area was significantly higher in untreated SNX rats than in controls and moxonidine-treated SNX rats. The same was true for urine albumin excretion rate. Renal angiotensin II tissue concentration was not affected by moxonidine. In untreated SNX rats, renal nerve stimulation and exogenous NE induced an increase in isolated kidney perfusion pressure (102 +/- 21 versus 63 +/- 8 mmHg). Renal endogenous NE content was significantly lower in SNX rats than in controls (86 +/- 14 versus 140 +/- 17 pg/mg wet weight). Cortical uptake of [(3)H]-NE was not different, but cortical NE release was significantly higher in SNX rats than in controls. Reduced function of presynaptic inhibitory alpha-adreno-receptors is unlikely because an alpha(2)-adrenoceptor antagonist increased NE release. At subantihypertensive doses, moxonidine ameliorates renal structural and functional damage in SNX animals, possibly through central inhibition of efferent sympathetic nerve traffic. In kidneys of SNX rats, indirect evidence was found for increased activity of a reduced number of nerve fibers.
188 citations
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TL;DR: A model is given which can describe the phenomenon of hormesis, and has the EC50 as one of its parameters, which has the advantage that theEC50 and its confidence interval can be determined directly by nonlinear regression.
186 citations
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TL;DR: With increasing vaccine use, all countries will be better prepared for the next pandemic and those countries that use but do not produce influenza vaccine will find it difficult to obtain supplies of pandemic vaccine.
185 citations
Authors
Showing all 6091 results
Name | H-index | Papers | Citations |
---|---|---|---|
Adi F. Gazdar | 157 | 776 | 104116 |
Mohammad Khaja Nazeeruddin | 129 | 646 | 85630 |
Jack P. Antel | 105 | 519 | 43950 |
Philippe Dubois | 101 | 1098 | 48086 |
Enrico Drioli | 95 | 987 | 37962 |
Martin Winter | 93 | 751 | 45506 |
Gian F. Giudice | 93 | 264 | 50392 |
Johannes Hebebrand | 91 | 581 | 38408 |
Michael Graetzel | 89 | 360 | 43269 |
Andrew J. Martin | 84 | 819 | 36203 |
Alan D. Rogol | 81 | 461 | 24865 |
Anthony L. Spek | 81 | 1090 | 59190 |
William J. Tremaine | 80 | 282 | 24233 |
Marc Henneaux | 76 | 411 | 27840 |
Stephen Lam | 76 | 413 | 20693 |