bluuebunny/crossref_metadata_2025 huggingface dataset:
Neuro‐fuzzy modelling of spectroscopic data. Part A — Modelling of dye solutions
Authors: Marjoniemi Marja , Mäntysalo Esa
Published: July 2010

The applicability of an adaptive network‐based fuzzy inference system for modelling of spectroscopic absorbance data in the visible region has been studied. Some basic principles of neuro‐fuzzy modeling are discussed. The samples were of a two‐component dye solution over a concentration range of 0–900 mg/l for the one component (red) while the concentration of the other component (yellow) was kept constant. The modelled system had two inputs (wavelength and concentration) with the absorbance values as output. Input/output data sets were computed. Generalised bell‐shaped membership functions were used for the inputs.
Application of a chitosan/nonionic surfactant mixture to wool assessed by dyeing with a reactive dye
Authors: Jocić D , Julià M R , Erra P
Published: July 2010

Chitosan application to wool is known to be associated with problems such as its weak binding and uneven distribution. In an attempt to overcome such problems, chitosan was applied from a mixture with a nonionic surfactant. A weak time interaction was observed between chitosan and the surfactant over time, resulting in changes in the conformation of chitosan in solution, which was confirmed by viscosity measurements. The presence of chitosan/surfactant association improved the application to wool, which was assessed by dyeing the treated wool with a reactive dye at 60°C. Since this technique offers the possibility of producing deeper and more vivid colours without increasing the concentration of dye used, dyeing was also carried out at 95°C, closer to practical dyeing conditions. An improvement in the fixation of the reactive dye was observed.
Determination of the amino acid tryptophan in protein fibres
Authors: Schäfer Karola
Published: July 2010

Tryptophan can be used as an indicator amino acid for the photostability of proteins. The analysis of tryptophan and its degradation products is hampered by their instability in oxidative or strongly acidic media, or light. Various methods were employed to quantify tryptophan in wool and other protein fibres such as silk and human hair. Acid, alkaline and enzymatic methods were used to hydrolyse protein fibres. The amino acid tryptophan in wool and other protein fibres was determined by a colorimetric method, by amino acid analysis and by reversed‐phase HPLC. The different analytical methods were compared with regard to their results. The colorimetric method (p‐dimethylamino‐benzaldehyde) proved to give reliable results for the tryptophan content in wool and unpigmented protein fibres. This method can be used also for wool dyed with acid, metal complex or reactive dyes or for pigmented keratin fibres after correction for a blank sample. Interference between dye and colorimetric reagent also have to be evaluated.
Instrumental methods for assessing colour fastness. Part 2 — Staining
Authors: Sato T , Ueda M , Nakamura T , Luo M R
Published: July 2010

In Part 1 of this paper, different fastness formulae for change in colour were compared. In the present report, the same methodology was used to compare different staining formulae. A set of experimental results was used to test the performance of various staining formulae. The constant grade contours for each formula were also calculated. Their patterns were compared and their differences were identified.
The use of non–physical standards in colour communication and matching
Authors: Fenn R I , Park J
Published: July 2010

As a result of developments in spectrophotometry, together with improved accuracy in computer colour matching and laboratory dyeing, non–physical standards (reflectance data) can now be used for the successful communication, matching and quality control of colour. In colour palette generation, ‘matching by numbers’ has become a reality.
Application of the Maillard, Strecker and modified Strecker (P–Mannich) reactions for the chemical modifications of wool
Authors: Trézl Lajos , Vida Csaba , Petneházy Imre , Rusznák István , Bakó Peter , Töke László
Published: July 2010

The application of the Maillard, Strecker and modified Strecker reactions in the chemical modification of wool are described. A practical method for improving reactive or acid dye pick–up under milder conditions of wool dyeing was the aim of the present work. This can be achieved by means of chemical bonding of selected carbohydrates with wool.
Dyeing of silk with bifunctional reactive dyes: the relationship between exhaustion and fixation
Authors: Agarwal Deepali , Sen Kushal , Gulrajani M L
Published: July 2010

The influence of dye reactivity on the exhaustion of reactive dyes on silk has been studied. It was found that if reactivity is reduced by blocking or hydrolysing the reactive groups, exhaustion also decreases. A mechanism by which reactive dyes exhaust onto silk in neutral media is also proposed.
Effect of mordant bleaching on the optical and mechanical properties of black human hair
Authors: Oh K. , Park M. , Kang T.
Published: July 2010

Decoiorisation of black human hair containing an excessive amount of melanin was carried out by alkaline peroxide bleaching under different mordanting conditions. The effect of iron mordanting methods on the optical, mechanical and tactile properties of bleached fibre was investigated. Sequestering agents, such as citric acid and oxalic acid, or reducing agents including phosphorous acid and sodium bisulphite, were employed to improve the selective absorption of iron into the fibre. The initial rate of bleaching and tactile properties were significantly affected by the amount of iron in the fibre which, in turn, was dependent on the type of mordanting auxiliary employed. Among the various mordanting auxiliaries, citric acid was the most efficient agent for the industrial application since it provided good lustre, smooth handle, and relatively high strength retention to the bleached fibre with good bleaching efficiency.
The use of ultraviolet radiation in an adsorbable organohalogen‐free print preparation for wool and in wool dyeing: the Siroflash process
Authors: Millington Keith R
Published: July 2010

German legislation controlling the discharge of adsorbable organohalogens (AOX) in process effluents has focused attention on the need for environmentally acceptable alternatives to chlorination as a prepare‐for‐print (PFP) treatment for wool. The Siroflash process is a novel AOX‐free approach which involves continuous UV irradiation of dry wool fabric, followed by conventional wet oxidation using hydrogen peroxide or permonosulphuric acid. Although permonosulphuric acid or peroxide treatments alone are ineffective as a PFP, the colour yields of prints on Siroflash‐treated fabric are similar to those on chlorinated wool. The synergistic interaction between UV exposure and wet oxidation results in high levels of cystine oxidation, cuticle damage and loss of soluble protein, all of which are highly specific to irradiated surface fibres. UV irradiation of wool can significantly increase dyeing colour yields. The use of 1:1 metal‐complex dyes is particularly effective, and a 3% o. w. f. dyeing on UV‐treated fabric can produce a better depth of shade than a 5% dyeing on untreated fabric.
The kinetics of dyeing: a non‐isothermal approach
Authors: Popescu C
Published: July 2010

Non‐isothermal kinetics can prove to be an effective tool for investigating exhaustion curves. Applying non‐isothermal methods of analysis to exhaustion data for disperse dyes on polyester, it was shown that the intimate mechanism cannot be covered by a unique kinetic function, as the mechanism seems to be composed of several stages, each with its own kinetics. As a consequence, the overall kinetics change with both temperature and heating rate. It is suggested that such an analysis should be performed each time before proposing kinetic functions to fit the experimental data. Non‐isothermal kinetic analysis also proves the impossibility of designing temperature‐raising programmes that will ensure isoreactive dyeing for a blend of two or more dyes.
Tautomerism and fluorescent properties of aminovinylpyrazine dyes
Authors: Shirai Kazuko , Matsuoka Masaru
Published: July 2010

We have reacted diaminomaleonitrile with pyruvic aldehyde or pyruvic acid to produce 2, 3‐dicyano‐5‐methylpyrazine and 2, 3‐dicyano‐6‐hydroxy‐5‐methylpyrazine. Although these compounds showed no fluorescence, condensation with arylaldehyde yielded red to violet coloured styryl‐type dyes with strong orange to red fluorescence. We have investigated the tautomerism and fluorescent properties of these new pyrazine dyes by means of computer simulation, and have also investigated their spectral properties using molecular orbital and molecular mechanics calculation techniques. These studies revealed the dyes to have strong intramolecular charge‐transfer chromophoric systems and high solvatochromism both in absorption and fluorescence spectra.
Convective mass transfer in liquid treatment processes
Authors: Telegin F Yu
Published: July 2010

A mathematical description of convective mass transfer in the processes of solution flow round a single fibre and through a layer of fibres is proposed. It is shown that theoretical dependence of the rate of mass transfer on flow rate, viscosity of dye solution and rate of diffusion of soluble substance is similar to those that are determined empirically. The results of this investigation may be used for theoretical analysis of fibre layer structure in the filtration and mass transfer during dyeing and washing processes.
Synthesis of HMFAN and its chromium and cobalt complexes and their application on nylon 6 and wool
Authors: Kocaokutgen H , Erdem E , Gümrükçgüoglu I E
Published: July 2010

The synthesis of the dye o,o′‐dihydroxyazo‐HMFAN and its chromium and cobalt complexes, is described. These dyes have been applied to nylon 6 and wool fabrics. Dye exhaustion has been calculated according to the absorbances of the original and residual dyes in the dyebath. The fastness to light, washing and rubbing of the dyed fabrics have been measured. The spectral characterisation of these dyes is investigated by IR and UV/Vis spectroscopic techniques and thin‐layer chromatography.
Synthesis, application and evaluation of cationising agents for cellulosic fibres
Authors: Seong H S , Ko S W
Published: July 2010

Five cationising agents were synthesised, through the reaction of various trialkylamines with epichlorohydrin, and then used for the cationisation of cellulosic fibre. The cationised cellulosic fibres could be dyed with acid dyes and showed excellent antimicrobial activity in spite of the low degree of cationisation.
Measurement of the activity of dispersants
Authors: Daescu C
Published: July 2010

A general and quick spectrophotometric method for the determination of activity (and relative activity) of dispersants for disperse and vat dyeing processes is described.
Dyeing of modified cotton fibres with disperse dyes from supercritical carbon dioxide
Authors: Özcan A S , Clifford A A , Bartle K D , Broadbent P J , Lewis D M
Published: July 2010

Cotton, previously modified by reaction with benzoyl chloride and sodium benzoylthioglycollate, was dyed with disperse dyes APAN and DY82 in supercritical carbon dioxide at 100 °C and 300 bar. This process is compared with the dyeing of polyester and unmodified cotton under the same conditions. The modification of the cotton fabric was confirmed using FTIR. The dyed fibre was also subjected to an ISO 2 wash fastness test. The colour yields were assessed by K/S measurements before and after washing. Microscopic cross‐section analysis for both modified and dyed cotton and for polyester was also performed.
Wash fastness of fluorocarbon finishes on polyester fabrics
Authors: Dufour F , Jordan C , Viallier P
Published: July 2010

A fabric's surface tension provides a measure of its ability to repel water and oil, while water penetration can be evaluated from a fabric's hydrostatic pressure, which depends mainly on the pore size and thus on the weave. One way of making a surface hydrophobic is to coat it with fluorinated polymers, which confer a low surface tension, reducing the fabric's wettability while preserving its breathability. We have shown that polyester microfibre fabrics (which already have a tight weave and hence high hydrostatic pressure) can be treated with fluorinated finishes to increase water and oil repellency. Observation of a piece of fluorinated polyester microfibre fabric over a number of washings has shown that a regenerative heat treatment preserved the repellency of the fabric but had little influence on the decrease in hydrostatic pressure that occurs with washing.
Annular Lipoatrophy of the Ankles: Case Report and Review of the Literature
Authors: Kerns Mary Jo , Stinehelfer Susan , Mutasim Diya F. , Zalla Mark J.
Published: July 2010

Abstract:  Annular lipoatrophy of the ankles also termed “annular atrophic connective tissue panniculitis of the ankles,”“annular atrophy of the ankles,” and “atrophic annular panniculitis of the ankles,” is an inflammatory panniculitis that results in lipoatrophy with a predilection for the ankles. The disorder is seen predominantly in female children and demonstrates a mixed lobular panniculitis. It is likely a disorder of autoimmune etiology, supported by the findings of concurrent autoimmune disorders in several patients. We report a case of a 6‐year‐old female with annular lipoatrophy of the ankles associated with Hashimoto thyroiditis and review the epidemiology and proposed pathogenesis of annular lipoatrophy of the ankles.
The Effect of Emergency Department Crowding on Length of Stay and Medication Treatment Times in Discharged Patients With Acute Asthma
Authors: Pines Jesse M. , Prabhu Anjeli , Hilton Joshua A. , Hollander Judd E. , Datner Elizabeth M.
Published: July 2010

ACADEMIC EMERGENCY MEDICINE 2010; 17:834–839 © 2010 by the Society for Academic Emergency Medicine

Objectives:  This study sought to determine if emergency department (ED) crowding was associated with longer ED length of stay (LOS) and time to ordering medications (nebulizers and steroids) in patients treated and discharged with acute asthma and to study how delays in ordering may affect the relationship between ED crowding and ED LOS.

Methods:  A retrospective cohort study was performed in adult ED patients aged 18 years and older with a primary International Classification of Diseases, 9th Revision (ICD‐9), diagnosis of asthma who were treated and discharged from two EDs from January 1, 2007, to January 1, 2009. Four validated measures of ED crowding (ED occupancy, waiting patients, admitted patients, and patient‐hours) were assigned at the time of triage. The associations between the level of ED crowding and overall LOS and time to treatment orders were tested by analyzing trends across crowding quartiles, testing differences between the highest and lowest quartiles using Hodges‐Lehmann distances, and using relative risk (RR) regression for multivariable analysis.

Results:  A total of 1,716 patients were discharged with asthma over the study period (932 at the academic site and 734 at the community site). LOS was longer at the academic site than the community site for asthma patients by 90 minutes (95% confidence interval [CI] = 79 to 101 minutes). All four measures of ED crowding were associated with longer LOS and time to treatment order at both sites (p < 0.001). At the highest level of ED occupancy, patients spent 75 minutes (95% CI = 58 to 93 minutes) longer in the ED compared to the lowest quartile of ED occupancy. In addition, comparing the highest and lowest quartiles of ED occupancy, time to nebulizer order was 6 minutes longer (95% CI = 1 to 13 minutes), and time to steroid order was 16 minutes longer (95% CI = 0 to 38 minutes). In the multivariable analysis, the association between ED crowding and LOS remained significant. Delays in nebulizer and steroid orders explained some, but not all, of the relationship between ED crowding and ED LOS.

Conclusions:  Emergency department crowding is associated with longer ED LOS (by more than 1 hour) in patients who ultimately get discharged with asthma flares. Some but not all of longer LOS during crowded times is explained by delays in ordering asthma medications.
Efficiency and Economic Benefits of a Payer‐based Electronic Health Record in an Emergency Department
Authors: Daniel Gregory W. , Ewen Edward , Willey Vincent J. , Reese, IV Charles L. , Shirazi Farshad , Malone Daniel C.
Published: July 2010

ACADEMIC EMERGENCY MEDICINE 2010; 17:824–833 © 2010 by the Society for Academic Emergency Medicine

Objectives:  The objective was to evaluate the use of a payer‐based electronic health record (P‐EHR), which is a clinical summary of a patient’s medical and pharmacy claims history, in an emergency department (ED) on length of stay (LOS) and plan payments.

Methods:  A large urban ED partnered with the dominant health plan in the region and implemented P‐EHR technology in September 2005 for widespread use for health plan members presenting to the ED. A retrospective observational study design was used to evaluate this previously implemented P‐EHR. Health plan and electronic hospital data were used to identify 2,288 ED encounters. Encounters with P‐EHR use (n = 779) were identified between September 1, 2005, and February 17, 2006; encounters from the same health plan (n = 1,509) between November 1, 2004, and March 31, 2005, were compared. Outcomes were ED LOS and plan payment for the ED encounter. Analyses evaluated the effect of using the P‐EHR in the ED setting on study outcomes using multivariate regressions and the nonparametric bootstrap.

Results:  After covariate adjustment, among visits resulting in discharge (ED‐only), P‐EHR visits were 19 minutes shorter (95% confidence interval [CI] = 5 to 33 minutes) than non‐P‐EHR visits. Among visits resulting in hospitalization, the P‐EHR was associated with an average 77‐minute shorter ED LOS (95% CI = 28 to 126 minutes), compared to non–P‐EHR visits. The P‐EHR was associated with an average of $1,560 (95% CI = $43 to $2,910) lower total plan expenditures for hospitalized visits. No significant difference in total payments was observed among discharged visits.

Conclusions:  In the study ED, the P‐EHR was associated with a significant reduction in ED LOS overall and was associated with lower plan payments for visits that resulted in hospitalization.
Thyroid State and Voluntary Alcohol Consumption of Albino Rats
Authors: Hillbom M. E.
Published: July 2010

Male Wistar rats were made hypo‐ and hyperthyroid in a period of three weeks by the daily administration of propylthiouracil or 3,3′,5‐triiodo‐L‐thyronine, and the voluntary alcohol consumption of the animals was investigated. The triiodothyronine treatment increased, and propylthiouracil treatment decreased the total caloric intake of the animals. However, the portion of ethanol in the total caloric intake of the rats was significantly increased by propylthiouracil treatment and significantly decreased by triiodothyronine treatment while the total caloric intake did not correlate positively with the voluntary alcohol consumption of these animals. The absorption of ethanol from the intravascular space, the peritoneal cavity and the gastrointestinal tract as well as the rate of elimination of ethanol were increased by triiodothyronine treatment and decreased by propylthiouracil treatment. The acetaldehyde concentration during oxidation of ethanol was found to be higher (166 ± 22 nmol/ml of blood) in the hepatic venous blood of euthyroid animals, as compared with hypo‐ and hyperthyroid ones. Acetaldehyde accumulation was not found to be a factor regulating voluntary alcohol intake in these animals.
Effect of Lithium on Glucagon‐Stimulated Cyclic AMP Excretion in Rats
Authors: Olesen O. Vendelin , Jensen Jørgen , Thomsen Klaus
Published: July 2010

Rats were given food containing lithium in amounts leading to serum lithium concentrations of 0.6‐1.1 mM, and the urinary excretion of cyclic AMP after subcutaneous injection of glucagon was determined. The unstimulated cyclic AMP excretion was the same in the lithium‐treated and in the control rats, but after glucagon administration the lithium‐treated rats excreted significantly higher amounts of cyclic AMP than the control rats. This occurred whether lithium had been given during two days or six weeks before the glucagon injection. At all dose levels of glucagon, within the range of 50‐1000 μg/kg b. wt., the response of the lithium‐treated rats was about 70% higher than in the control rats. The increased cyclic AMP excretion was not due to the lithium‐induced polyuria since the difference between the lithium‐treated rats and control rats was also present when polyuric lithium rats were compared with polyuric control rats. The higher excretion of cyclic AMP could not be accounted for by an increased activity of the adenyl cyclase or a decreased degradation rate of cyclic AMP measured in liver homogenates. A somewhat lowered binding capacity of the protein kinases for cyclic AMP was found in the lithium‐treated rats; this might cause or contribute to the increased urinary cyclic AMP excretion.
Effects of the Herbicide 2,4,5‐T on the Incorporation of 14C‐Thymidine, 3H‐Uridine and 3H‐L‐Leucine into L 929 Cells
Authors: Dragsnes L. , Helgeland K.
Published: July 2010

Abstract: A rapid inhibition of the incorporation of 3H‐L‐leucine, 3H‐uridine and 14C‐thymidine into the macromolecular fraction of L 929 cells was found when 2.25 mM 2,4,5‐trichlorophenoxyacetic acid (2,4,5‐T) was added to the incubation medium. The reduced incorporation of 3H‐uridine and 14C‐thymidine could be explained by an inhibitory effect of 2,4,5‐T on the uptake of these compounds into the acid‐soluble precursor pool, whereas a direct effect on protein synthesis was indicated. Kinetic analysis of the uptake of uridine into the acid‐soluble pool indicated that 2,4,5‐T inhibited the facilitated transport of this nucleoside into the cell. The overall results are interpreted as indicating that 2,4,5‐T induced alterations in the permeability of the cellular plasma membrane.
Pharmacokinetics of Clofibrate and Chlorophenoxy Isobutyric Acid. I. Cross‐over Studies on Human Volunteers
Authors: Männistö P. T. , Tuomisto J. , Jounela A. , Penttilä O.
Published: July 2010

Abstract:The absorption characteristics of five clofibrate preparations were compared in a cross‐over study. After a single dose, four capsule preparations containing 500 mg each of oily clofibrate yielded nearly identical serum levels of chlorophenoxy isobutyric acid (CPIB) in the serum. On the contrary, 500 mg of the basic aluminium salt of CPIB given as a tablet gave significantly lower serum levels at each point of time. The excretion of the latter preparation in 24 hrs was only 1/3 of that of the other four preparations. One of the clofibrate preparations and the tablet preparation were compared in a cross‐over study lasting five days. 500 mg of both drugs were administered twice daily. The capsule preparation gave steady‐state serum levels of 50–65 mg/l of CPIB beginning on the 2nd day. The tablet preparation exhibited a slow rise in the serum levels, and on the 5th day of treatment the differences between the serum levels were no longer significant. The steady‐state and elimination kinetics were studied in a 17‐day hospital experiment. The plateau levels were 65–80 mg/ml after clofibrate 500 mg twice daily, and 50–60 mg/ml after aluminium chlorophenoxy butyrate, respectively. The daily excretion suggested that the absorption of clofibrate is complete, but that that of CPIB is only 60%. Hence, there was a discrepancy between the absorption and the nearly equal steady‐state serum levels. After discontinuing the administration of the aluminium salt, the course of the disappearance of CPIB was first‐order, and an elimination half‐time of 54 hrs was calculated. On the other hand, after clofibrate, a two‐process elimination was seen. The first process had an elimination half‐time of about 10 hrs and the second process had one identical to that observed after Al‐CPIB or 54 hrs. It is suggested that, after clofibrate, CPIB is found in two pools. The rapidly eliminating pool may mainly represent the drug in plasma, whereas the slowly eliminating pool might represent the take up of the drug in the liver and only slowly released into the circulation. When given as CPIB, some of the compound could be trapped by the liver, and then the rate of elimination would depend on the release from the liver. The slow absorption of CPIB and the delayed gastric emptying after Al+++may also contribute to the slow rise in the blood levels. When given as the ester, most of the drug would pass through the liver, and be hydrolyzed in the circulation to give high serum concentrations, and therefore the rate‐limiting step of initial elimination would be the renal handling of the drug. Some redistribution is also likely to take place at this initial stage.
Influence of Hematin, Carbon Tetrachloride and SKF 525‐A Administration on the Enhancement of Microsomal Monooxygenase and UDPglucuronosyltransferase by 3,4‐Benzpyrene in Rat Liver
Authors: Vainio Harri , Aitio Antero
Published: July 2010

Abstract:Both drug oxidation (cytochrome P‐450, and the overall hydroxylation reactions aryl hydrocarbon hydroxylase andp‐nitroanisole O‐demethylase) and glucuronidation (UDPglucuronosyltransferase both withp‐nitrophenol and 4‐methylumbelliferone as aglycones) were enhanced by administering a single intraperitoneal dose of 3,4‐benzpyrene to rats. The flavoprotein component in the microsomal monooxygenase system, NADPH cytochrome c reductase, was not influenced by 3,4‐benzpyrene administration. The intragastric administration of carbon tetrachloride (1 ml/kg body weight) almost totally blocked the microsomal drug oxidation and also suppressed the enhancement of both mixed function oxidase and UDPglucuronosyltransferase by 3,4‐benzpyrene. The inhibitor of heme synthesis, hematin, and inhibitor of cytochrome P‐450 dependent metabolism, SKF 525‐A, also suppressed the enhancement of both microsomal mixed function oxidase and UDPglucuronosyltransferase achieved by 3,4‐benzpyrene administration.
The Comparative Effect of Chlorhexidine and Cetrimonium Bromide on Erythrocyte Membranes
Authors: Jensen Jørn Erik
Published: July 2010

AbstractThe effect of chlorhexidine (Chx) and cetrimonium bromide (Ctab) on the haemolysis of erythrocytes has been studied. A concentration dependent release of haemoglobin was observed in isotonic media, with total haemolysis at 80 nmol Chx per 107cells and 20 nmol Ctab per 107cells. The rate of haemolysis induced by Chx shows a biphasic pattern in contrast to the uniphasic pattern of Ctab. In concentrations below 10 nmol per 107cells, Chx produces more haemolysis than Ctab whereas the opposite effect is observed at higher concentrations. Chx and Ctab stabilize the erythrocyte membrane against hypotonic shock. The concentrations of Chx and Ctab giving maximal stabilization are 0.25 nmol per 107cells and 2 nmol per 107cells respectively. The normal biconcave disc form of the erythrocytes is converted to cup forms and in‐vaginated spheres by Chx and Ctab. The binding of Chx to erythrocytes in isotonic media increases linearly with the total concentration up to about 25 nmol Chx per 107cells where the curve has a point of inflection. With more than 25 nmol Chx per 107cells the amount of Chx bound again increases linearly up to 120 nmol per 107cells. The slope of the curve above the point of inflection is approximately 4 times that of the curve below this point. No level of saturation of the binding is observed at the concentrations of Chx used in this study. The mode of action of Chx on erythrocyte membranes is discussed in the light of the present results.
(Z)‐Dimethylamino‐l‐(4‐bromophenyl)‐l‐(3‐pyridyl) propene (H 102/09), a New Selective Inhibitor of the Neuronal 5‐Hydroxytryptamine Uptake
Authors: Ross Svante B. , Ögren Sven–Ove , Renyi Anna L.
Published: July 2010

AbstractThe inhibition of the uptake of3H–(–)–noradrenaline (NA),3H–dopamine and14C–5–hydroxytryptamine (5–HT) in mouse brain slices by (Z)–3–dimethylamino–l–(4–bromophenyl)–l–(3–pyridyl)propene (H 102/09), desipramine and chlorimipramine and their releasing effect on the3H–amines previously accumulated in the slices were examined. The interactions with reserpine produced hypothermia and sedation and the 5–hydroxytryptophan (5–HTP) syndrome in mice were also studied. Due to the poor inhibitory activity on the NA uptake H 102/09 was a more selective inhibitor of the 5–HT uptake than was chlorimipramine, particularly after administrationin vivo,where it was as potent as chlorimipramine (ED50 = 19 μmol/kg intraperitoneally).In vitrochlorimipramine was 6 to 12 times more active than H 102/09. Desipramine was a very selective inhibitor of the NA uptakein vitroandin vivo.The compounds were generally more potent in inhibiting the uptake than in releasing the amines. However, in striatal slices the inhibition of DA uptake could be due to the releasing effect since the difference in potencies were small. The effect of desipramine on 5–HT uptake and that of H 102/09 on NA uptake could also involve a release component. The 5–HTP syndrome was potentiated by H 102/09 and chlorimipramine but not by desipramine. The reserpine hypothermia but not the sedation was potently antagonized and reversed by desipramine and by chlorimipramine at high doses but not by H 102/09, suggesting that NA but not 5–HT is involved in the hypothermic action of reserpine.
Bronchospasmolytic and Cardiovascular Effects in Anaesthetized Cats of Ibuterol and Terbutaline Given Intravenously and after Inhalation: Drug and Prodrug Compared
Authors: Andersson Per
Published: July 2010

AbstractThe bronchospasmolytic and cardiovascular effects of terbutaline and ibuterol were tested in the anaesthetized cat after inhalation and after intravenous infusion. A 5–min. inhalation of ibuterol in the concentrations 0.01–0.5 mM counteracted the serotonin–induced bronchoconstriction. In this respect it was 3 times as potent as terbutaline. The two compounds administered intravenously proved equi–effective. Neither inhalation nor intravenous infusion had any significant effect on the heart rate, pulse amplitude, or arterial blood pressure, in doses which counteracted the induced bronchospasm. Higher doses of the compounds caused a dose–dependent increase in heart rate and pulse amplitude, and a decrease in diastolic blood pressure. After intravenous infusion, the cardiovascular effects of the compounds were almost identical. Inhaled ibuterol had a more pronounced effect than inhaled terbutaline. It was concluded that both ibuterol and terbutaline, have a good margin between the bronchospasmolytic and the cardiovascular effects after inhalation and intravenous infusion. Esterification of the OH–groups in the ring of terbutaline with di–isobutyric acid did not change this relation.
Cerebrospinal‐fluid Concentrations of Nitrazepam in Man
Authors: Kangas L. , Kanto J. , Siirtola T. , Pekkarinen A.
Published: July 2010

Abstract The concentrations of nitrazepam in the plasma and cerebrospinal‐fluid (CSF) of 38 neurological patients were determined by gas chromatography 2‐36 hours after a single 5 mg oral dose. The percentage ratio between the mean CSF and the plasma concentrations increased from 8.0 % at 2 hours to 15.6 % at 36 hours. This percentage rise was significant (P < 0.001). The maximum concentration of nitrazepam in the plasma was 36.7 ± 5.7 ng/ml (at 2 hours) and CSF 3.0 ± 0.3 ng/ml (at 4 hours). During the β‐phase the half‐life of nitrazepam in plasma was about 27 hours and in the CSF markedly longer about 68 hours, indicating a very slow elimination of nitrazepam from the CSF.
Guanethidine Induced Sympathectomy in the Adult Rat. I. Functional Effects Following Subacute Administration
Authors: Nielsen Gunnar Damgård
Published: July 2010

AbstractGuanethidine sulphate 5 and 40 mg/kg was administered intraperitoneally to adult rats for 4, 8, 14, and 28 days followed by discontinuation for 1 day, after administration for 28 days and additionally for 8, 14, 29, and 60 days. Under chloralose‐urethane anaesthesia the mean arterial blood pressure and the mean heart rate were determined and the response of these parameters to intravenous noradrenaline 3‐1600 ng was recorded. The blood pressure was not significantly changed after guanethidine 5 mg/kg, but lowered by 40 mg/kg, the decrease being reversible on discontinuation. The response of both parameters to noradrenaline was increased by guanethidine depending on the dose. The hypersensitivity was partly reversible on discontinuation, but a significantly increased sensitivity of the heart rate to noradrenaline was observed 60 days after discontinuation of guanethidine 40 mg/kg for 28 days. Histologically a profound loss of nerve cells of the superior cervical ganglion was observed following guanethidine 40 mg/kg, whereas no change was observed after 5 mg/kg. The present investigation has demonstrated that guanethidine 5 mg/kg does not induce histological or permanent haemodynamic changes, whereas 40 mg/kg for 28 days result in an incomplete sympathectomy accompanied by a partially irreversible hypersensitivity to noradrenaline. There is no simple relation between the loss of ganglion cells and the haemodynamic changes, and hence the hypersensitivity to noradrenaline is only in part due to the destruction of the postganglionic sympathetic neurone obtained by long term administration of large doses of guanethidine.
The Kinetics of Imipramine‐N‐Oxide in Rats
Authors: Nagy Adam
Published: July 2010

AbstractRats were given imipramine‐N‐oxide as single intramuscular injection and then as repeated oral doses. Imipramine‐N‐oxide and the metabolites imipramine and desipramine were analysed in the blood cells, plasma and brain tissue. The concentration of imipramine‐N‐oxide increased simultaneously in the brain and blood, reaching a peak 45 minutes after a single dose. Imipramine was the quantitatively predominant metabolite in the blood cells and brain, while desipramine reached a higher concentration than imipramine in the plasma. Samples taken at different times after oral doses during continuous treatment showed fairly constant concentrations of imipramine‐N‐oxide and desipramine in the brain, whereas the concentration of imipramine was more fluctuating.
Serum Levels and Electrophysiological Effects of N‐Acetylprocainamide as Compared with Procainamide in the Dog Heartin situ
Authors: Amlie Jan P. , Nesje Ola A. , Frislid Karin , Lunde Per Knut M. , Landmark Knud
Published: July 2010

AbstractThe electrophysiological effects of procainamide and its major metabolite N‐acetylprocainamide were tested and compared on the heart of the anaesthetized dog by means of His bundle electrography and programmed electrical stimulation. Both drugs exerted a negative chronotropic effect. They also increased intra‐atrial and intraventricular conduction times; procainamide was, however, the more potent of the two drugs. In contrast to procainamide, N‐acetylprocainamide did not increase His‐Purkinje and atrioventricular nodal conduction times, and at the lowest dose employed, atrioventricular nodal conduction times were decreased during atrial pacing. Both drugs increased the functional and effective refractory period of the right atrium and ventricle. N‐acetylprocainamide increased the functional refractory period of the atrioventricular node, but to a lesser extent than procainamide.
Levels of Dopamine, Norepinephrine and 5‐Hydroxytryptamine in Different Regions of the Rat Brain in Thallium Toxicosis
Authors: Hasan Mahdi , Ali S. Fatehyab , Tariq M.
Published: July 2010

AbstractThe levels of dopamine, noradrenaline and 5‐hydroxytryptamine were estimated in the hypothalamus and limbic areas, corpus striatum, cerebellum and the brain‐stem of rats administered thallous acetate (5 mg/kg i.p.) daily for 7 days. Significant decreases in the concentration of dopamine occurred in the hypothalamus, limbic areas and corpus striatum. Noradrenaline did not reveal significant alteration in any of the regions of the brain examined. The concentration of 5‐hydroxytryptamine was significantly lowered in the corpus striatum, cerebellum and the brain‐stem.
The Effect of Nifedipine on Isolated Human Peripheral Vessels
Authors: Mikkelsen E. , Andersson K.‐E. , Pedersen O. Lederballe
Published: July 2010

Abstract Isometric tension was recorded in ring preparations of human peripherial arteries and veins contracted by potassium (127 mM) and noradrenaline (1.8 × 10‐5 M). In the veins, nifedipine had a marked relaxing effect on contractions induced by both agents, and also reduced the contractile amplitude when added prior to stimulation. The inhibiting effect of nifedipine was more marked on the potassium than on the noradrenaline‐evoked responses. This was in contrast to verapamil, which inhibited the noradrenaline‐induced contractions significantly more, than those produced by potassium. After immersion of the vein preparations in calcium‐free medium for 30 min., the potassium contracture decreased to 26±2.0% (mean ± S.E.M.) of the response in normal Krebs solution, and the noradrenaline‐evoked response to 7.1±0.8%. The responses to both agents were completely restored when the calcium concentration was increased from 0 to 4 mM. Nifedipine (1.5 × 10‐7 M) depressed the potassium contracture in calcium‐free solution to 7.3±1.6%, and the noradrenaline response to 5.5±1.6%; on addition of calcium, the response elicited by potassium increased to 16±1.7%, and that by noradrenaline to 56±8.6%. Compared with its actions on the veins, the effect of nifedipine on the arterial preparations was less pronounced. In the arteries, too, the inhibiting effect of nifedipine was significantly more pronounced on the potassium than on the noradrenaline‐induced contraction. Immersion for 30 min. in calcium‐free medium reduced the response to potassium to 61±6.0% and that to noradrenaline to 68±5.6% of the control in normal Krebs. Nifedipine (2.9 × 10‐7 M) further reduced the potassium contraction to 20±4.0%; the response to noradrenaline was unaffected, being 74±6.4% of the control.
Uptake of Glucuronides into Isolated Hepatocytes and their Effects on Glucuronide and Sulphate Conjugation
Authors: Norling Anja , Andersson Bo , Berggren Margareta , Moldéus Peter
Published: July 2010

Abstract Uptake studies, using radioactive labelled glucuronides, have demonstrated the ability of 4‐nitrophenyl glucuronide and phenolphthalein glucuronide to enter isolated rat hepatocytes. Of these glucuronides 4‐nitrophenyl glucuronide was distributed in a similar manner to O‐methylglucose, whereas phenolphthalein glucuronide was bound to cellular constituents. Phenolphthalein glucuronide had an effect on the conjugation of harmol in the isolated hepatocytes when glucuronidation was found to be markedly inhibited and sulphation slightly stimulated. The glucuronidation of 4‐nitrophenol, 4‐methylumbelliferone and harmol in native microsomes was inhibited by phenolphthalein glucuronide. 4‐Nitrophenyl glucuronide and also naphthyl glucuronide were without effect both in hepatocytes and microsomes. In control hepatocytes harmine was metabolized to form harmolsulphate mainly. Phenolphthalein glucuronide only affected this metabolic pattern to a minor extent. However, in hepatocytes from phenobarbital treated rats, where the rate of harmine metabolism is increased about five times and the main metabolite is harmol glucuronide, phenolphthalein glucuronide inhibited the formation of the conjugate with a concomitant increase in free harmol.
Differences in postsynaptic α‐Adrenoceptor Populations Between Isolated Cat Urethra and Various Other Isolated Tissues.
Authors: Gahlin Kerstin , Sparf Bengt
Published: July 2010

Abstract This study was undertaken with the aim of determining whether the postsynaptic α‐adrenergic receptor population of the cat urethra differed from that of other isolated tissues (rabbit aorta and rat vas deferens) and if so the possibility of selectively affect these receptors. For this purpose the substances 2‐methylammonio‐1‐(spiro[cyclopentane‐1, 1′‐indene]‐3′‐yl)ethanol(KABI2023), noradrenaline (NA) and dopamine (DA) were used. KABI 2023 and NA acted as full agonists on all three tissues investigated. DA was a full agonist on the vas deferens but was almost inactive on urethra. The contractile response of urethra to KABI 2023 was of an α‐adrenergic nature, as it could be blocked with phentolamine. Compared with NA, KABI 2023 showed a 10 times higher selectivity for the receptors of urethra than for those of aorta. Affinity constants (log KB) for phentolamine and haloperidol with use of the various agonists were estimated. The affinity of phentolamine was found to be significantly different when using NA and KABI 2023 as agonists on the urethra but not on the aorta. Corresponding findings were obtained with haloperidol. On the vas deferens a greater difference in log KB values than that on the urethra was found. On the basis of the results, it is suggested that the population of postsynaptic α‐adrenoceptors in the urethra (cat) differs from that in the aorta (rabbit). On the vas deferens a heterogenicity of postsynaptic receptors seem to exist which makes the interpretation of the results more difficult on this organ. In the presence of phentolamine and haloperidol the maximum responses to NA were potentiated on the aorta and vas deferens, but not on the urethra. Investigations to evaluate this difference are now in progress.
Is Ethanol‐Induced Damage of the Gastric Mucosa a Hyperosmotic Effect? Comparative Studies on the Effects of Ethanol, some other Hyperosmotic Solutions and Acetylsalicylic Acid on Rat Gastric Mucosa
Authors: Puurunen Juhani , Huttunen Pirkko , Hirvonen Jorma
Published: July 2010

Abstract:The involvement of hyperosmolarity in ethanol‐induced gastric mucosal damage was studied by comparing the effects of ethanol on the rat gastric mucosa with those caused by hyperosmotic glucose and choline chloride solutions, and by an almost isosmotic solution of acetylsalicylic acid. Upon intragastric instillation, all test solutions, namely 3M and 5M ethanol (3330 and 5590 mosmol/kg resp.), 3M glucose (3890 mosmol/kg), 1.5 M choline chloride (2840 mosmol/kg) and 20 mM acetylsalicylic acid, also containing 100 mM HCl and 50mM NaCl, produced macroscopic and microscopic lesions of the gastric mucosa. The haemorrhages induced by ethanol and acetylsalicylic acid solutions were more evenly distributed, whereas most lesions produced by the glucose and choline chloride solutions were located at the rumeno‐fundicjunction. There were no qualitative differences between the microscopic lesions caused by the various instillates, however. All the test solutions broke the gastric mucosal barrier and increased histamine release and pepsinogen output, but in the rats treated with acetylsalicylic acid these effects were less pronounced. Ethanol, glucose and choline chloride solutions increased gastric mucosal flow and fluid output from the stomach, whereas acetylsalicylic acid had no effect on these. The similarity between the ethanol‐induced changes and those caused by hyperosmotic solutions of glucose and choline chloride leads to the suggestion that ethanol may cause damage in the gastric mucosa at least in part, via hyperosmolarity.
The Mammalian Spot Test and its Use for the Testing of Potential Carcinogenicity of Welding Fume Particles and Hexavalent Chromium
Authors: Knudsen Ib
Published: July 2010

Abstract: Welding fume particles, potassium chromate and cyclophosphamide are tested in the mammalian spot test. Female mice C57BL/6J/BOM 9 weeks old have been mated to T‐stock male mice and treated with welding fume particles 100 mg/kg, potassium chromate 20 or 10 mg/kg, or cyclophosphamide 10 or 2.5 mg/kg intraperitoneally at day 8, 9 and 10 of pregnancy. The fur of the offspring was checked week 2 through week 5 after birth for coloured spots. The characterisation of the different types of spots are discussed. Welding fume particles 100 mg/kg and potassium chromate 10 mg/kg induce approximately to the same extent as cyclophosphamide 2.5 mg/kg, grayish or brownish spots in the fur. The mammalian spottest it at present under validation as an in vivo screening test for mutagenic and carcinogenic potential of chemicals. The positive results for potassium chromate and cyclophosphamide are in agreement with previous in vitro experiments and confirm the sensitivity of the test. The effect of welding fume particles in this in vivo system suggests a potential risk for humans directly exposed to welding fumes.
Electrocardiographic and Cardiovascular Changes in Cats and Dogs Caused by High Doses of Amitriptyline Given as Conventional Tablets or a Sustained Release Preparation
Authors: Boeck Vita , Jørgensen Aksel
Published: July 2010

Abstract Electrocardiographic and haemodynamic changes have been compared in anaesthetized cats and in conscious dogs after high doses of amitriptyline given as conventional tablets or as a sustained release form. Plasma or serum levels of amitriptyline and nortriptyline were determined. In anaesthetized cats tablets caused marked ECG changes in all 6 animals combined with pronounced acidosis in 3 of the animals. The sustained release form caused no electrocardiographic changes in 4 animals and moderate disturbances in 2 animals, without acidosis in any of the 6 cats. Almost identical haemodynamic changes were seen in both groups. The plasma levels did not indicate poorer absorption from one preparation than from the other. In conscious dogs tablets caused marked clinical signs including restlessness, sedation and convulsions (2 dogs). Pronounced electrocardiographic changes were seen in all 4 dogs. Bundle branch block developed in 3 dogs. The sustained release preparation caused slight to moderate sedation and no convulsions. Pronounced electrocardiographic changes without bundle branch block were seen in one dog. Moderate changes were seen in the remaining dogs. Acidosis was most pronounced after the tablets. The serum drug levels clearly show that the absorption is much slower after administration of the sustained release preparation than after tablet administration and that somewhat lower amounts of drug are absorbed from the sustained release preparation than from tablets. It is evident from the present studies, that administration of high doses of amitryptyline as a sustained release preparation causes less toxic manifestations than given as conventional tablets. Part of the explanation may be that less amitryptyline is absorbed from the sustained release preparation than from tablets because of the high dose (dogs), but the main reason is most likely that the absorption from the sustained release preparation is much slower than the absorption from tablets.
Lack of Antiinflammatory Activity of Metronidazole
Authors: Ganrot‐Norlin K. , Stålhandske T. , Karlström R.
Published: July 2010

Abstract: Metronidazole was given to rats with experimentally induced inflammation to evaluate whether the drug has any antiinflammatory effect. Inflammation was caused by injection of Freund's complete adjuvant into a paw. The oedema of the paw measured on the 4th day was not influenced after metronidazole 20 mg/kg/day or 160 mg/kg/day, whereas phenylbutazone 80 mg/kg/day significantly decreased the volume of the paw. The concentration of orosomucoid did not differ in the group of rats given metronidazole 20 mg/kg/day as compared to the control group. However, the orosomucoid concentration was lower in the group given metronidazole 160 mg/kg/day, as was the case in the phenylbutazone group. In groups of rats with polyarthritis studied on the 14th and 21st day there was no difference of arthritic index, volume of paw or orosomucoid concentration in neither low nor high dose metronidazole as compared to the control groups. The phenylbutazone groups, however, showed a lower arthritic index, lower volume of paw and lower orosomucoid concentration.