Abstract
We demonstrate that the polar cortex makes cytokinesis inherently unstable. We show that limited asymmetric polar contractions occur during cytokinesis, and that perturbing the polar cortex leads to cell shape oscillations, resulting in furrow displacement and aneuploidy. A theoretical model based o...
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PMID: 21822289
PDF is available here.
Abstract
We evaluated the efficacy of derivatives of creatine and amino acids (CrAA) for decreasing cerebral injury in rats with transient middle cerebral artery occlusion (MCAO). Neuroprotective effects of amides of creatine and glycine (CrGlyOEt), phenylalanine (CrPheNH2), thyrosine (CrTyrNH2), and GABA (C...
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PMID: 21961295
PDF is available here.
Abstract
With two β-mercaptoethyl groups on the N, a tertiary amide of structure 1 is always poised for intramolecular thioesterification however it flips about the C-N bond. It is shown that a peptide with such a C-terminal N,N-bis(2-mercaptoethyl)-amide (BMEA) can be used directly for nati...
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PMID: 21175148
PDF is available here.
Abstract
With two β-mercaptoethyl groups on the N, a tertiary amide of structure 1 is always poised for intramolecular thioesterification however it flips about the C-N bond. It is shown that a peptide with such a C-terminal N,N-bis(2-mercaptoethyl)-amide (BMEA) can be used directly for nati...
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PMID: 21175148
PDF is available here.
Abstract
We compared the intraarticular analgesic effects of ropivacaine and morphine with or without Xefocam and the need for rescue i.v. morphine at rest and during movement in patients undergoing anterior cruciate ligament reconstruction under spinal anesthesia. Anterior cruciate ligament reconstruction (...
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PMID: 21991728
PDF is available here.
Abstract
We summarize synthetic methodology for custom QS agonists and antagonists against the Lux system in Gram-negative bacteria....
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PMID: 21031318
PDF is available here.
Abstract
This prospective, randomized, double blind study was designed to determine whether reduction in volume from 20 to 10 mL of ropivacaine 0.5% for ultrasound-guided interscalene block might decrease the incidence of diaphragmatic paresis and preserve pulmonary function....
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PMID: 21751435
PDF is available here.
Abstract
The present study documents the chemosensitizing anti-leukemic activity of the leflunomide metabolite (LFM) analog, LFM-A13, a dual-function inhibitor of Bruton's tyrosine kinase (BTK) and Polo-like kinases (PLK), against human leukemic B-cell precursors. The results in 135 xenografted NOD/SCID mice...
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PMID: 21650085
PDF is available here.
Abstract
We addressed whether performance on an implicit mental rotation task reflects these RA-induced changes in body schema brain representations. Studying these changes in healthy volunteers may shed light on normal function and the central mechanisms of pain.
Performance pattern was studied in upper lim...
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PMID: 21169795
PDF is available here.
Abstract
We examined the role of Y-27632 on human umbilical cord Wharton's jelly stem cells (hWJSCs) for (1) thaw-survival (2) proliferation and (3) preservation of stemness and differentiation potential after cryopreservation. hWJSCs were allotted to 4 groups [Gp I: Untreated hWJSC controls; Gp II: Pretreat...
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PMID: 20711690
PDF is available here.
Abstract
We previously demonstrated that RhoA and its effector, Rho-kinase (Rho-associated coiled-coil containing protein kinase, ROCK), are involved in the pathogenesis of diabetic nephropathy. However, its role in MCP-1 induction by TNF-α has not been elucidated. In the present study, we investigated whet...
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PMID: 20977889
PDF is available here.
Abstract
Three different tetraazamacrocyclic ligands containing four amide substituents that feature groups (namely allyl, styryl and propargyl groups) suitable for polymerisation have been synthesised. Gadolinium(III) complexes of these three ligands have been prepared as potential monomers for the synthesi...
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PMID: 20877892
PDF is available here.
Abstract
S-Nitrosocaptopril, a biologically active S-nitrosothiol, is generated as protonated species and isolated in the gas phase by electrospray ionization coupled to Fourier Transform Ion Cyclotron Resonance (FT-ICR) or ion-trap mass spectrometry. The structural and IR spectroscopic characterization of p...
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PMID: 20852770
PDF is available here.
Abstract
Systemic toxicity, usually from overdose or intravascular dose, is feared because it mainly affects the heart and brain, and may be acutely life-threatening.
Pharmacological studies of local anesthetic toxicity have largely been reviewed primarily relating to the evaluation of ropivacaine and levobu...
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PMID: 20738226
PDF is available here.
Abstract
SmI(2)/H(2)O promotes selective α-monodefluorinations, while addition of an amine results in complete α-defluorination reactions.
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PMID: 20838692
PDF is available here.
Abstract
C(1)-symmetric isoquinoline-based chiral diaminocarbene ligands (MIQ) have been developed to block three quadrants of the metal coordination sphere, complementing C(2)-symmetric biisoquinoline-based ligands (BIQ). MIQ-Cu complexes catalyzed conjugate borylation of various α,β-unsaturated amides in...
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PMID: 20835472
PDF is available here.
Abstract
A dianionic phenoxyamido ligand was the first to be used to stabilize organo-rare-earth metal amido complexes. Amine elimination reaction of Nd[N(TMS)(2)](3)(μ-Cl)Li(THF)(3) (TMS = SiMe(3)) with aminophenol [HNOH] {[HNOH] = N-p-methylphenyl(2-hydroxy-3,5-di-tert-butyl)benzylamine} in a 1 : 1 mo...
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PMID: 20820599
PDF is available here.
Abstract
We present our experience with ultrasound-guided TAP perineural catheter insertion and subsequent management of ambulatory TAP local anesthetic infusions after inguinal hernia repair.
Three patients scheduled for unilateral open inguinal hernia repair underwent preoperative posterior TAP catheter pl...
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PMID: 20975474
PDF is available here.
Abstract
This study was performed to determine the minimum effective volume of ropivacaine 0.75% required to produce effective shoulder analgesia for an ultrasound (US)-guided block at the C7 root level with assessment of pulmonary function.
Using the Dixon and Massey up-and-down method study design, 20 pati...
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PMID: 20975468
PDF is available here.
Abstract
We prospectively investigated the analgesic effect of ultrasound-guided continuous supraclavicular BPB with ropivacaine at different infusion rates.
Thirty-nine patients scheduled to undergo shoulder surgery were randomly assigned to four groups; receiving no continuous BPB (control group, n = 10),...
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PMID: 21077306
PDF is available here.
Paul D Andrews,
Melissa Becroft,
Anders Aspegren,
Jane Gilmour,
Martyn J James,
Scott McRae,
Robert Kime,
Robert W Allcock,
Achamma Abraham,
Zhong Jiang,
Raimund Strehl,
Joanne C Mountford,
Graeme Milligan,
Miles D Houslay,
David R Adams and
Julie A Frearson
Abstract
We have developed a high-content assay for human embryonic stem cell survival and used this to screen a range of libraries of 'lead-like' small molecules and known bioactives. From this we identified 18 confirmed hits with four structural classes being represented by multiple compounds: a series of...
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PMID: 20854259
PDF is available here.
Abstract
We have investigated the fundamental amidation reaction by a model system consisting of an electrochemically functionalised Au surface by aminophenyl and 4-nitrobenzoic acid activated by EEDQ. The development of the NO(2) related stretching vibrations with time reveals that the amidation process is...
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PMID: 20737098
PDF is available here.
Abstract
Catalyzed by Rhodococcus erythropolis AJ270, a nitrile hydratase and amidase containing microbial whole cell catalyst, a number of racemic 1-arylmethyl- and 1-allyl-4-oxoazetidine-2-carbonitriles and carboxamides underwent efficient transformations under very mild conditions to produce enantiopure f...
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PMID: 20721414
PDF is available here.
Abstract
We compared the action of lidocaine, articaine, ropivacaine and mepivacaine in a dose 2.5 or 5mg/kg/ml/h infused from 10min before left anterior descending coronary artery occlusion until the end of the experiment. In the rat ischemia- and re-perfusion-induced arrhythmia models, the following parame...
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PMID: 20615402
PDF is available here.
Abstract
We discuss metal-protein interactions in the Ag-lysozyme complex by spectroscopic measurements. The analysis of the variation in relative intensities of SERS bands reveals the orientation and the change in conformation of the protein molecules on the Ag surface with time. The interaction kinetics of...
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PMID: 20685371
PDF is available here.
Abstract
As a continuation of our research and with the aim of obtaining new anti-tuberculosis agents which can improve the current chemotherapeutic anti-tuberculosis treatments, forty-three new quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives were synthesized and evaluated for in vitro anti-tuberculosis...
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PMID: 20656380
PDF is available here.
Abstract
We proposed that this reaction proceeded by the consecutive cyclization to aziridines via the SN2 process involving the activation of the C-Br bond based on the intermolecular Br…Li(+) coordination, as a result of studies of reaction mechanisms....
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PMID: 20930486
PDF is available here.
Abstract
Although a number of chemicals have been isolated from Lantana camara, only a few have been evaluated for their biological significance. As part of our drug discovery program for cytotoxic agents from Indian medicinal plants, roots of L. camara L. were chemically investigated, which resulted in the...
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PMID: 21121249
PDF is available here.
Abstract
We investigated the effects of aliskiren, a direct oral renin inhibitor, on the activities of free and (P)RR-bound forms of human mature renin. We also elucidated the effect of aliskiren on the 'renin activity' of the receptor-bound form of prorenin. Aliskiren had an IC(50) of 0.72 nmol l(-1) ag...
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PMID: 20664543
PDF is available here.
Abstract
Chemoenzymatic dynamic kinetic resolution (DKR) of amines involving sulfanyl radical-induced racemization happened to be the very first switchable DKR process allowing the synthesis of either (R)- or (S)-amides, in good yield and high enantiomeric excess, depending on the nature of the enzyme; the d...
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PMID: 20661510
PDF is available here.
Abstract
We find that the experimental Amide I-II band predominantly results from a mixture of partially unfolded P(II) and unfolded beta conformational equilibrium of aqueous 2-Ala at room temperature....
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PMID: 20539891
PDF is available here.
Abstract
A highly enantioselective group 5 metal amide catalyst system is reported for the hydroaminoalkylation of secondary amines to give chiral amines in good yields with excellent ee values (up to 93%) by loading of 5% precatalyst.
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PMID: 20668747
PDF is available here.
Abstract
We investigated the binding site of ACT058362 and SB706375 in both hUT2R and rUT2R to explain the dramatically lower (approximately 400-fold) affinity of ACT058362 for rUT2R and the similar affinity (approximately 10 nM) of SB706375 for both UT2Rs. These studies used MembStruk and MSCDock to predict...
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PMID: 20683923
PDF is available here.
Abstract
We use intra-articular injections delivered directly into the soft tissue of the knee. Our current intra-articular injection is 60 mL of 0.5% ropivacaine with 0.5 mg of epinephrine. In patients with a normal renal function, 30 mg of ketorolac is added. The injection is administered throughout all of...
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PMID: 20839683
PDF is available here.
Abstract
All 3 prostaglandin/amide drugs are highly effective at lowering IOP. No differences in effect between the drugs or between members of different racial groups were detected, although the study sample size was too small to be certain to detect differences, if they existed....
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PMID: 20051890
PDF is available here.
Abstract
A range of amide derivatives of L-dopa were synthesized and investigated for their pharmacological activity and their ability to be converted to L-dopa using the unilaterally 6-hydroxydopamine (6-OHDA)-lesioned rat, as an experimental model of Parkinson's disease. The diacetyl derivative of L-dopa a...
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PMID: 20646792
PDF is available here.
Abstract
A series of novel enaminone amides with improved side effect were synthesized by Hogenkamp et al. To explore the action mechanisms of enaminone amides, the homology model of rat alpha1beta2gamma2 GABAR was generated using the cryo-electron microscopy structure of the nAChR of Torpedo marmorata and t...
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PMID: 20684859
PDF is available here.
Abstract
Together with apigenine dimethylether and piperchabamide A, a new amide alkaloid, Kaousine and the Z form of antiepilepsirine were isolated from the aerial part of Piper capense L.f (Piperaceae). Their structures were elucidated by spectrometric methods and their in vitro antiparasitic activities we...
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PMID: 20227469
PDF is available here.
Abstract
We present a theoretical study of the possibility to use isotope label two-dimensional infrared (2DIR) spectroscopy to obtain site specific structural information in trpzip2. This small beta-hairpin peptide was designed as a model system for studying protein folding in beta-sheet structures. In orde...
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PMID: 20596553
PDF is available here.
Yifeng Xiong,
Brett Ullman,
Jin-Sun Karoline Choi,
Martin Cherrier,
Sonja Strah-Pleynet,
Marc Decaire,
Peter I Dosa,
Konrad Feichtinger,
Bradley R Teegarden,
John M Frazer,
Woo H Yoon,
Yun Shan,
Kevin Whelan,
Erin K Hauser,
Andrew J Grottick,
Graeme Semple and
Hussien Al-Shamma
Abstract
We herein report the discovery of a series of potent and selective serotonin 5-HT(2A) receptor antagonists based on a phenethylpiperazine amide core structure. When tested in a rat sleep pharmacology model, these compounds increased both sleep consolidation and deep sleep. Within this series of comp...
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PMID: 20684606
PDF is available here.
Abstract
We have shown that osteoblasts produce LPA, raising the possibility that it mediates intercellular signaling among osteoblasts and osteoclasts. Here we investigated the expression, signaling and function of LPA receptors in osteoclasts. Focal application of LPA elicited transient increases in cytoso...
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PMID: 20551326
PDF is available here.
Abstract
We conjugated this drug to a N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer backbone. Dox was conjugated via an amide bond (Dox-HPMA(AM), PK1) or a hydrazone pH-sensitive bond (Dox-HPMA(HYD)). In contrast to Dox and Dox-HPMA(HYD), Dox-HPMA(AM) accumulates within the cell's intracellular membrane...
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PMID: 20556593
PDF is available here.
Abstract
Ropivacaine induced tonic inhibition of peak Na(+) currents of both subtypes in a dose- and frequency-dependent manner. rNav1.5 appeared to be more sensitive to ropivacaine. In addition, for both Na(+) channel subtypes, the steady-state inactivation curves, but not the activation curves, were signif...
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PMID: 20651810
PDF is available here.
Abstract
Filamentous benthic marine cyanobacteria are a prolific source of structurally unique bioactive secondary metabolites. A total of 12 secondary metabolites, belonging to the mixed polyketide-polypeptide structural class, were isolated from the marine cyanobacterium, Lyngbya majuscula, and were tested...
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PMID: 20658384
PDF is available here.
Angela M Lam,
Eisuke Murakami,
Christine Espiritu,
Holly M Micolochick Steuer,
Congrong Niu,
Meg Keilman,
Haiying Bao,
Veronique Zennou,
Nigel Bourne,
Justin G Julander,
John D Morrey,
Donald F Smee,
David N Frick,
Julie A Heck,
Peiyuan Wang,
Dhanapalan Nagarathnam,
Bruce S Ross,
Michael J Sofia,
Michael J Otto and
Phillip A Furman
Abstract
The hepatitis C virus (HCV) NS5B RNA polymerase facilitates the RNA synthesis step during the HCV replication cycle. Nucleoside analogs targeting the NS5B provide an attractive approach to treating HCV infections because of their high barrier to resistance and pan-genotype activity. PSI-7851, a pron...
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PMID: 20516278
PDF is available here.
Abstract
Reninangiotensinaldosterone system is a key link in regulation of blood pressure and causes the target organ damage in hypertensive patients. For many years is not lost interest in the pharmacological blockade of RAAS in order to achieve target levels of BP and prevent damage target organs, particul...
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PMID: 21089428
PDF is available here.
Abstract
A simple and rapid high-performance liquid chromatography method coupled with UV detector was developed and validated for the simultaneous determination of ropivacaine, bupivacaine and dexamethasone in biodegradable poly(lactic-co-glycolic acid) (PLGA) microspheres within 11 min. Chromatographic sep...
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PMID: 20686210
PDF is available here.
Abstract
We evaluated patient-controlled analgesia use, pain and satisfaction scores, complication rates, and ropivacaine levels associated with the use of periarticular multimodal drug infiltration in THA.
We randomized 64 patients undergoing THA to receive a periarticular intraoperative mul...
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PMID: 20020333
PDF is available here.
Abstract
We show that GLP-1 (9-36) amide directly suppresses glucose production in isolated mouse hepatocytes ex vivo independent of the GLP-1 receptor. These findings support direct insulinomimetic actions of the GLP-1 metabolite on gluconeogenesis in hepatocytes that are independent of insulin action and t...
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PMID: 20645222
PDF is available here.
Abstract
Ropivacaine is less potent than bupivacaine, but otherwise they have similar dose-response characteristics. The difference in potency is not statistically significant at ED90 doses....
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PMID: 20613484
PDF is available here.
Abstract
A stable and controllable Prussian blue (PB) layer electrodeposited on self-assembled monolayers (SAMs) of thioctic acid amide (T-NH(2)) on gold electrode was prepared. The PB, combining with biocompatible matrix chitosan, was used for the highly efficient immobilization of glucose oxidase (GOD) for...
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PMID: 20517545
PDF is available here.