Search results for "guanidine"
showing 10 items of 78 documents
Isolation of carcinoembryonic antigen N-terminal domains (N-A1) from soluble aggregates
2011
Abstract Carcinoembryonic antigen (CEA) was identified as a prominent tumor-associated antigen in human colorectal cancer and it is still intensively investigated. However, its physiological role remains unclear. The CEA molecule is composed of seven highly hydrophobic, immunoglobulin-like domains, six of which contain a single disulphide bridge. The production of recombinant protein containing Ig-like domains in bacterial expression systems often results in partial degradation or insolubility due to aggregation hampering the analysis of their native structure and function. Here, we present a new method of expression and purification of CEA N-terminal domains (N-A1) fused to MBP in Escheric…
H2-Antihistaminika, 28. Mitt. Synthese und H2-antagonistische Wirkung 3-(3-piperidinomethyl-phenoxy)propyl-substituierter Kohlensäurederivate und Ana…
1986
Es wurden 3-(3-piperidinomethyl-phenoxy)propyl-substituierte Kohlensaurederivate wie Harnstoffe, Thioharnstoffe, Guanidine und Cyanoguanidine sowie analoge Nitroethendiamine dargestellt und am isolierten Meerschweinchenvorhof und zum Teil an der histaminstimulierten Sauresekretion der narkotisierten Ratte auf H2-antagonistische Wirkung untersucht. H2-Antihistaminics, XXVIII: Syntheses and H2-Antagonistic Activity of Derivatives of Carbonic Acid and Analogues Carrying a 3-[3-(Piperidinomethyl)phenoxy]propyl Substituent Derivatives of carbonic acid such as ureas, thioureas, guanidines, and cyanoguanidines as well as the analogous nitroethenediamines were prepared with a 3-[3-(piperidinomethyl…
Affinity scale between a carrier and a drug in DPI studied by atomic force microscopy.
2002
The dry powder inhalers (DPIs) consist, in the most cases, of ordered mixture where the particles adhesion results of interactions between the drug and the carrier. Generally, one step of production process is the micronization of the drug particles in order to reduce the size for ordered mixing optimization. But this operation is known to partially create an amorphous surface. In this case, surrounding storage conditions, like relative humidity (RH), are able to modify the percentage of amorphous drug surface. The aim of this study was to investigate surface reactivity, surface energy and direct force measurements by atomic force microscopy (AFM) between lactose (carrier) and zanamivir (dr…
The anti-inflammatory and antinociceptive effects of NF-κB inhibitory guanidine derivative ME10092
2010
The guanidine compound ME10092 (1-(3,4-dimethoxy-2-chlorobenzylideneamino)-guanidine) is known to possess anti-radical and anti-ischemic activity but its molecular targets have not been identified. This study investigated whether ME10092 regulates the nuclear factor kappa B (NF-kappaB)-mediated signal transduction in vivo. The effect of ME10092 treatment (1-100 pmol/mouse) on nuclear translocation of NF-kappaB, activation of expression of inflammatory mediators and production of nitric oxide were measured in the lipopolysaccharide (LPS)-induced brain inflammation model in mice in vivo. The antinociceptive activity of ME10092 was tested in the formalin-induced paw licking test. ME10092 dose-…
Influence of experimental diabetes on regulatory mechanisms of vascular response of rabbit carotid artery to acetylcholine
2000
Summary The purpose of this study was to analyse the influence of experimental diabetes on vascular response of rabbit carotid artery to acetylcholine (Ach). We compared the Ach-induced relaxant response of isolated arterial segments obtained from both control and diabetic animals. To assess the influence of the endothelium, this cell layer was mechanically removed in some of the arterial segments (“rubbed arteries”) from each experimental group. Ach induced a concentration-related endothelium-mediated relaxation of carotid artery from control rabbits that was significantly higher with respect to that obtained in diabetic animals. Pre-treatment with NG-nitro-L-arginine (L-NA) induced a conc…
Intraoperative localization of malignant pheochromocytoma by 123-i-metaiodobenzylguanidine single probe measurement
1988
Metaiodobenzylguanidine (MIBG) imaging is a well-established method for locating intra- and extraadrenal pheochromocytomas. We investigated whether preoperative injection of 123-I-MIBG might be useful for intraoperative staging of chromaffine tumor cells. This was performed in a 46-year-old patient in whom the diagnosis of a malignant pheochromocytoma had been established by 123-I-MIBG imaging and enhanced catecholamine secretion. The rationale for intraoperative staging in this patient was a discrepancy between computed tomography (CI) of the abdomen and the radionuclide imaging, because scintigraphy revealed a mass with MIBG uptake in the right lower abdomen that could not be visualized b…
A novel form of ataxia oculomotor apraxia characterized by oxidative stress and apoptosis resistance
2007
Several different autosomal recessive genetic disorders characterized by ataxia with oculomotor apraxia (AOA) have been identified with the unifying feature of defective DNA damage recognition and/or repair. We describe here the characterization of a novel form of AOA showing increased sensitivity to agents that cause single-strand breaks (SSBs) in DNA but having no gross defect in the repair of these breaks. Evidence for the presence of residual SSBs in DNA was provided by dramatically increased levels of poly (ADP-ribose)polymerase (PARP-1) auto-poly (ADP-ribosyl)ation, the detection of increased levels of reactive oxygen/nitrogen species (ROS/RNS) and oxidative damage to DNA in the patie…
Involvement of the P2X7 purinergic receptor in colonic motor dysfunction associated with bowel inflammation in rats
2014
Background and Purpose Recent evidence indicates an involvement of P2X7 purinergic receptor (P2X7R) in the fine tuning of immune functions, as well as in driving enteric neuron apoptosis under intestinal inflammation. However, the participation of this receptor in the regulation of enteric neuromuscular functions remains undetermined. This study was aimed at investigating the role of P2X7Rs in the control of colonic motility in experimental colitis. Experimental Approach Colitis was induced in rats by 2,4-dinitrobenzenesulfonic acid. P2X7R distribution was examined by immunofluorescence analysis. The effects of A804598 (selective P2X7R antagonist) and BzATP (P2X7R agonist) were tested on co…
Two‐dimensional analysis of myocardial protein expression following myocardial ischemia and reperfusion in rabbits
2002
Myocardial ischemia and reperfusion injury (MI/R) can be related to leukocyte activation with subsequent release of cytokines and oxygen derived free radicals. Activation of the complement system has been implicated in the pathogenesis of myocardial ischemia and reperfusion injury. Inflammatory injury will subsequently result in cellular activation and protein synthesis. In the present study we analyzed the myocardial protein expression and its pattern following myocardial ischemia and reperfusion, with and without complement inhibition with the synthetic serine protease inhibitor Futhan/nafamstat mesilate (FUT-175) known to inhibit classical and alternative complement pathway in a rabbit m…
Diabetes-induced changes in endothelial mechanisms implicated in rabbit carotid arterial response to 5-hydroxytryptamine
2000
Abstract The influence of diabetes on endothelial mechanisms implicated in the response of isolated rabbit carotid arteries to 5-hydroxytryptamine (5- HT ) was studied. 5-HT induced a concentration–dependent contraction that was potentiated in arteries from diabetic rabbits with respect to that in arteries from control rabbits. Endothelium removal potentiated 5-HT contractions in arteries from both control and diabetic rabbits but increased the maximum effect only in arteries from diabetic rabbits. Incubation of arterial segments with N G -nitro- l -arginine ( l- NA) enhanced the contractile response to 5-HT. This l -NA enhancement was greater in arteries from diabetic rabbits than in arter…