bluuebunny/crossref_metadata_2025_split huggingface dataset:
The inhibitory effect of sulphonylurea derivatives on liver glycogenosis increased by catecholamines
Authors: Pogátsa G , Kaldor A , Vizi E S 
Published: April 2011

Abstract
Hypoglycaemic sulphonylureas inhibit the increased glycogenosis and glucose release of the rat perfused liver produced by β-adrenergic agonists. The β-receptor antagonist propranolol exerted a similar effect. Dichloroisoprenaline increases the hypoglycaemic effect of chlorpropamide given in doses ineffective in the intact rat. Hypoglycaemic sulphonylureas have no effect on the catecholamine sensitivity of the nictitating membrane and heart auricle of the cat, indicating that their ability to inhibit glycogenosis induced by β-receptor agonists is not due to a β-receptor antagonist activity as is the action of propranolol.
Preparation and characterization of the tropic acid esters of tropan-3β-ol, granatan-3α-ol and granatan-3β-ol
Authors: Hunt R J , Robinson J B 
Published: April 2011

Abstract
The preparation and characterization of the tropic acid esters of tropan-3β-ol and granatan-3α and 3β-ol are reported. A rapid synthesis of pseudopelletierine is described.
The effect of antioxidants on the hydrolytic and oxidative degradation of sulphacetamide in aqueous solutions
Authors: Davies D J G , Meakin B J , Moss S H 
Published: April 2011

Abstract
The effect of heat and light stresses on the degradation of sulphacetamide solutions at pH 7, in the presence and absence of the antioxidants sodium metabisulphite and sodium edetate, have been investigated. Sodium metabisulphite accelerates the hydrolytic degradation of sulphacetamide to sulphanilamide, whereas sodium edetate does not change the rate. The absorption peak causing colour development due to heat stress is shown to differ from that due to light stress. The development due to both stimuli has been measured quantitatively with time. Sulphanilamide present in heat-degraded solutions is shown to be insignificant in the development of colour due to heat stress, but to have a major role in colour formation under light stress.
Some observations of the penetration and disruption of tablets by water
Authors: Ganderton D , Fraser D R 
Published: April 2011

Abstract
The effect of compressibility, particle size, granulation and the addition of starch on the pore structure on tablets of aspirin, calcium carbonate, lactose, magnesium carbonate, phenindione and sucrose has been measured using air permeability and liquid penetration techniques. The addition of starch to the various materials produced no significant effect on the pore structure of the dry tablet but caused disruption and alteration of this structure when the tablet was penetrated by water. This disruptive effect produced by starch depends on the compressibility of the constituent material and the pressure used to form the tablet.
Rheology of systems containing cetrimide-cetostearyl alcohol: variation with temperature
Authors: Barry B W , Saunders G M 
Published: April 2011

Abstract
The viscoelastic gel in the continuous phase of a liquid paraffin in water emulsion (stabilized by the mixed emulsifier cetrimide-cetostearyl alcohol) is similar to that formed by dispersing cetrimide and cetostearyl alcohol in water. The effect of temperature changes on the rheological properties of the emulsion and ternary system have been examined in continuous shear and in creep, and variations in the viscosities and compliances have been correlated with thermal phase transitions determined microscopically. The emulsion and ternary system were of maximum consistency at approximately 38° and 43° respectively; these temperatures respresent the transition from frozen smectic to liquid crystalline phase. At higher temperatures, the compliances rose and the viscosities fell as the network weakened and finally dissolved to form an isotropic solution.
The absorption, blood concentrations and excretion of pentazocine after oral, intramuscular or rectal administration to man
Authors: Beckett A H , Kourounakis P , Vaughan D P , Mitchard M 
Published: April 2011

Abstract
Blood concentrations, urinary excretion rates and faecal excretion of unchanged drug were measured after oral, intramuscular or rectal administration of pentazocine; Significant inter-subject variation was observed. Blood concentration-time curves are related to urinary excretion rates. Relative physiological availabilities by each route were determined.
The influence of protein binding on the excretion of some sulphanilamidopyrimidines in man
Authors: Walker Stuart R 
Published: April 2011

Abstract
The metabolism and excretion of sulphadimethoxine, sulphorthodimethoxine, sulphamethomidine, sulphasomidine and sulphadimethoxypyrimidine have been investigated in man. The plasma protein binding data including the percentage bound at various concentrations of the drugs, the number of binding sites (n), the binding capacity of plasma albumin (rmax) and the dissociation constant of the sulphonamide-albumin complex (K) for these compounds have been measured by ultrafiltration. The short-acting sulphasomidine is bound to a much lesser extent at the concentrations obtained clinically in the plasma than the long-acting drugs. Sulphasomidine occupies only one binding site on plasma albumin compared with the other sulphonamides investigated which occupy two sites. This may partly account for the rapid excretion of this compound in man. Sulphadimethoxine has two major metabolites, the N4-acetyl derivative and sulphadimethoxine-N1-glucuronide. N4-Acetyl sulphadimethoxine has similar binding constants to the parent compound. However the N1-glucuronide forms a weak complex with plasma albumin which has a lower binding capacity for this metabolite (rmax = 0.58) compared with sulphadimethoxine itself (rmax = 1.77). The results are discussed in relation to the excretion of these compounds.
The recovery of noradrenaline in adrenergic nerve terminals of the rat after reserpine treatment
Authors: HÄGGENDAL JAN , DAHLSTRÖM ANNICA 
Published: April 2011

Abstract
Tissue concentrations of endogenous noradrenaline in heart, submaxillary gland, and gastrocnemic muscle have been examined after one large dose of reserpine (10 mg/kg) to rats. After the initial depletion of the amine, the concentration started to rise between 24 and 36 h. For about one week thereafter the amine recovery proceeded comparatively fast, then the rate of the recovery slowed. Between the 4th and the 6th weeks there was a pronounced drop in the noradrenaline concentration in all three tissues, apparently beginning in the 4th week with a maximal decrease of about 20% in the 5th week after reserpine. Thereafter the concentrations increased to approach normal about 6 weeks after reserpine. These results are discussed in relation to the axonal down-transport of newly formed amine storage granules and to the life-span of these granules in the nerve terminals. The different parts of the noradrenaline recovery curve appeared to reflect the axonal down-flow of granules. A theoretical recovery curve was calculated, based on granular transport. This curve was similar to the observed recovery curve. The claim is made that the recovery of adrenergic function and noradrenaline levels after reserpine is due to a down-transport of newly formed, amine storage granules to the nerve terminals. There seems little need for the theory that the storage function reappears in old, reserpine-blocked granules, as a mechanism for noradrenaline recovery after a large dose of reserpine.
The effect of thymoxamine on peripheral blood vessels as monitored by the 133Xe clearance technique
Authors: DICK W CARSON , PROVAN C , RITCHIE D , BUCHANAN W WATSON 
Published: April 2011

Abstract
The rate of clearance of intra-articularly administred 133Xe provides an indirect method for the measurement of synovial tissue perfusion. The effect of an intra-articular injection of thymoxamine, and of isoprenaline was to increase the clearance rate whereas the converse was seen with noradrenaline. The prior administration of thymoxamine did not affect the isoprenaline response. In suitable doses, thymoxamine both prevented, and reversed the noradrenaline effect.
The metabolism and urinary excretion in man of phentermine, and the influence of N-methyl and p-chloro-substitution
Authors: BECKETT A H , BROOKES L G 
Published: April 2011

Abstract
The urinary excretion of phentermine, mephentermine and chlorphentermine was examined after oral administration of phentermine and chlorphentermine hydrochlorides and mephentermine sulphate to man under normal and acidic conditions of urinary pH. The rate of excretion of both phentermine and mephentermine fluctuated with changes in urine pH, a more acidic pH causing a faster rate of excretion; changes in urine flow rate had only a slight effect. The rate of excretion of chlorphentermine was affected by changes in pH and urinary flow rates. Phentermine and mephentermine were recovered almost quantitatively within 24 h from subjects under acidic urine control; only about 35% chlorphentermine was recovered under similar conditions.
Amphetamine tachyphylaxis in the pithed guinea-pig
Authors: Gerald Michael C 
Published: April 2011

Abstract
A single dose of (+)-amphetamine (8 mg kg−1, i.p.) administered 4 h before experimentation, reduced the pressor and positive chronotropic effects elicited by this drug (0·6 mg kg−1, i.v.) and augmented the rate of the development of tachyphylaxis to these responses in the pithed guinea-pig preparation. Amphetamine pretreatment reduced the pressor and positive chronotropic effects of phenylephrine (0·1 mg kg−1, i.v.) and the positive chronotropic effects of angiotensin (30 μg kg−1, i.v.). The rate of the development of tachyphylaxis to the cardiovascular responses elicited by phenylephrine and angiotensin was augmented by amphetamine pretreatment. These results suggest that an indirect mechanism (noradrenaline) may in part mediate the cardiovascular effects of these 3 drugs and/or that amphetamine may act as a competitive antagonist at adrenoceptor sites.
The quantification of kanamycin ototoxicity in the rat using conditioned tone discrimination
Authors: Harpur E S , D’arcy P F 
Published: April 2011

Abstract
Twelve male Lister hooded rats were conditioned to discriminate an 8 kHz tone (56·5 ± 0·5 dB re 0·0002 dyne cm−2) and were subsequently injected subcutaneously with kanamycin (400 mg kg−1 day−1) for 28 days; during this time and for five weeks after dosage was stopped, the nature and extent of the resultant hearing deficits were studied. The animals’ Preyer reflex thresholds were determined at intervals during the study. Only one rat was unaffected by the kanamycin dosage. The onset of hearing impairment (reduced discrimination performance), which was gradual in some rats and sudden in others, generally occurred during the fourth week of kanamycin dosage although the earliest onset was towards the end of the second week. In most animals the hearing impairment progressed after kanamycin was stopped and in one rat there was a latency between the end of drug dosage and onset of hearing impairment. Hearing impairment was irreversible in five rats. One rat, whose impairment was slight, recovered normal hearing. Some rats showed a reduced discrimination performance at a time when their Preyer reflex threshold showed no elevation suggesting that kanamycin, at least initially, caused a threshold elevation rather than reduced sensitivity to intense sounds.
The action of colloidal silicon dioxide as a glidant for lactose, paracetamol, oxytetracycline and their mixtures
Authors: Varthalis S , Pilpel N 
Published: April 2011

Abstract
Anomalies are observed in some of the physical and mechanical properties of mixtures of lactose, paracetamol and oxytetracycline when small amounts of colloidal silicon dioxide are added to them. Owing to its differing propensities to coat the particles of the host powders, the silicon dioxide acts as a glidant for the lactose and paracetamol, but as an antiglidant for the oxytetracycline.
The granulation of ternary mixtures: the effect of the solubility of the excipients
Authors: Jaiyeoba K T , Spring M S 
Published: April 2011

Abstract
The importance of excipient solubility in wet granulation has been shown using mixtures of lactose and boric acid containing third components of differing solubility characteristics. Sucrose dissolved in the binder solution and increased the amount of liquid available to form liquid bridges between other solid particles and therefore increased the number of solid bridges when the damp mass was dried. Thus, stronger, larger granules were formed. The results obtained with Sta-Rx 1500 and magnesium carbonate powders were also dependent upon the extent of solubility of these powders in the granulating solution.
Evaluation of glycine as an inactivator of glutaraldehyde
Authors: CHEUNG H Y , BROWN M R W 
Published: April 2011

Abstract
Glycine was evaluated as an inactivator of the sporicidal activity of glutaraldehyde. Spores from glucose depleted cultures of Bacillus stearothermophilus grown in a chemically defined medium were used. When glycine is used as an inactivator of glutaraldehyde, it lowers the pH value of the solution. Glycine 1% failed to inactivate 0.5% or higher concentrations of alkaline glutaraldehyde in sporicidal studies. If viable counts cannot be performed within the first hour after inactivation, the concentration of glycine should be at least 2% to inactivate effectively 2% alkaline glutaraldehyde.
The macroanionic activity of heparins in the presence of dextrose and calcium ion
Authors: ANDERSON W , HARTHILL J E 
Published: April 2011

Abstract
The effect of dextrose on heparin was investigated using the heparin-azur A interaction as a measure of macroanionic activity. Dextrose solutions did not diminish heparin – azur A metachromasia but prior autoclaving of the dextrose solution resulted in a slight decrease. When calcium chloride was added to the dextrose (autoclaved or unautoclaved) there was a reduction which was greater than that caused by calcium ion in the absence of dextrose. The effects of calcium ion and dextrose acting together were each concentration - dependent. A low molecular weight fraction (8400) was more susceptible to the effects of calcium in the presence of dextrose than a fraction of mol. wt. 19 000, hence unfractionated heparins with different amounts of various fractions may respond differently to calcium in the presence of dextrose. This has not been considered in earlier studies of the anticoagulant activity of unfractionated heparins in dextrose infusion and could have contributed to reported discrepancies, particularly in view of the variety of test methods used. At present, it is not possible to predict from in vitro tests whether dextrose will modify the in vivo anticoagulant activity of heparin.
Identification and measurement of desethylamiodarone in blood plasma specimens from amiodarone-treated patients
Authors: FLANAGAN R J , STOREY G C A , HOLT D W , FARMER P B 
Published: April 2011

Abstract
Desethylamiodarone has been identified as the principal lipophilic metabolite of amiodarone present in plasma specimens from amiodarone-treated patients. This structure has been confirmed by probe-injection mass spectrometry of column effluent fractions and comparison with the authentic compound using both chromatographic and mass spectrometric techniques. Although there is no information available as to the pharmacological activity of desethylamiodarone in man, the plasma concentrations of this metabolite attained during chronic amiodarone therapy are similar to those of the parent compound (0.1–4 mg litre−1).
Are dopamine receptors present on human lymphocytes?
Authors: FLEMINGER S , JENNER P , MARSDEN C D 
Published: April 2011

Abstract
The characteristics of [3H]spiperone binding to human lymphocytes have been examined. The haloperidol displaceable component of [3H]spiperone binding to human lymphocytes was not saturable, and stereoselective displacement by the isomers of butaclamol was not observed. There was no correlation between the ability of known dopamine active drugs to cause displacement of the ligand and their rank order of potency. Chloroquine, a drug with no dopaminergic action, was the most potent displacing agent examined. Fragmentation of the cells caused a marked decrease in the haloperidol displaceable component of [3H]spiperone binding, and saturable binding to the lymphocyte membrane fragments was not observed. Lysis of cells after equilibrium incubation with [3H]spiperone caused a marked reduction in the haloperidol displaceable component of ligand binding. Association of [3H]spiperone with lymphocytes was unaffected by the metabolic inhibitor iodoacetate, or by replacement of sodium ions by lithium ions in the incubation medium, suggesting that such association did not involve an active uptake process. We cannot confirm the existence of dopamine receptors on the surface of human lymphocytes. We suggest that the apparent association of [3H]spiperone with lymphocytes is due to some passive uptake process causing accumulation of the ligand within the cells.
The effect of membrane filters on cultured cells
Authors: ENGEL FREDERIK 
Published: April 2011

Abstract
The use of membrane filters for filtration of serum-containing culture media can change a medium in such a way that cells cultured therein attain a significantly higher lactate-glucose metabolism than the same type of cells cultured in unfiltered medium. Five different filtertypes were examined, but the response was only found after filtration with MF-filters of Millipore (mixed esters of cellulose). Furthermore, in two of the three cell lines examined minor growth inhibitions were also observed. The MF-filters were found to contain a compound bound to the filter material so that serum-containing medium, but not serum-free medium, or water, could extract it in amounts sufficient for metabolic – and growth effects. The compound in MF-filters is closely related to Triton-X-100 both with respect to u.v.-spectra and to biological effects.
Reaction of ampicillin with serum albumin to produce penicilloyl-protein conjugates and a piperazinedione
Authors: BUNDGAARD HANS , HANSEN JENS 
Published: April 2011

Abstract
Formation of penicilloyl-protein conjugates in the body by reaction of penicillins with nucleophilic groups of proteins is considered to be involved in penicillin allergy. In this study the kinetics and mechanism of reaction of ampicillin with human and bovine serum albumin in aqueous solution at 37 °C and pH 6.6–10.4 have been investigated and compared with the reaction of benzylpenicillin previously reported. In addition to forming penicilloyl-protein conjugates, ampicillin was found to react with the proteins to yield a free piperazine-2,5-dione derivative. This product is suggested to arise from intramolecular aminolysis of an N-(penicilloyl)imidazole intermediate at pH 6–8 and of a penicilloyl ester intermediate at higher pH values. The piperazinedione formation was found to compete effectively with formation of penicilloyl-protein conjugates at physiological pH and, along with studies of ampicillin with protein model compounds, the reaction allowed suggestions to be made about the penicillin-reacting sites in the proteins.
Interaction of local anaesthetics with model phospholipid membranes. The effect of pH and phospholipid composition studied by quenching of an intramembrane fluorescent probe
Authors: SUREWICZ W K , LEYKO W 
Published: April 2011

Abstract
The interaction of local anaesthetics, tetracaine and procaine, with model phospholipid membranes has been examined by measurement of drug-induced quenching of the fluorescence of a membrane incorporated probe, 12-(9-anthroyl)stearic acid. The pH dependence of quenching curves obtained for neutral phosphatidylcholine and acidic phosphatidylserine bilayers indicates that, contrary to previous suggestions, both charged and uncharged forms of amine local anaesthetics may be incorporated into lipid membranes.
Acute effects of ethanol and acetaldehyde on plasma phosphate level
Authors: MATSUBARA K , NAKAHARA M , TAKAHASHI S , FUKUI Y 
Published: April 2011

Abstract
Oral administration of ethanol in a dose of 65 mmol kg−1 produced marked change of plasma phosphate level in rabbits. Hypophosphataemia was observed for the first 2 h after administration followed by significant increase of plasma phosphate at 5 h. Hypophosphataemia did not appear when ethanol was given to the rabbits pretreated with pyrazole. When animals were injected with disulfiram in advance, the duration of hyperphosphataemia due to ethanol was prolonged. Administration of acetaldehyde at a dose of 1.5 mmol kg−1 produced hyperphosphataemia. In this study, plasma phosphate was not associated with change in calcium level. These results suggest that the hypophosphataemia observed was related to the metabolic process of ethanol utilizing alcohol dehydrogenase, and that acetaldehyde, a metabolite of ethanol, might induce the hyperphosphataemia in the animals.
The uptake of mepacrine by horse polymorphonuclear leucocytes in vitro
Authors: Read N G , Trist D G 
Published: April 2011

Abstract
The uptake of mepacrine by isolated horse polymorphonuclear leucocytes (PMN) was measured using spectrophotofluorimetry. Two phases of uptake were observed, the first, rapid fraction, essentially complete by 10 min, and a second, slow fraction, which was still proceeding after 60 min. The appearance of mepacrine within the PMN was also visualized by fluorescence microscopy. Discrete yellow points of fluorescence were observed in the cytoplasm of PMN within 30 s. These discrete points corresponded both in size and number to the PMN granules. After 5 min, the nuclei showed faint fluorescence which increased in intensity with time. It was concluded that the accumulation of mepacrine by horse PMN consists of at least two phases, an initial rapid component which represents uptake of the drug through the plasma membrane into the cytoplasmic granules, and a subsequent slower component, possibly representing nuclear binding.
Role of lipoproteins and erythrocytes in the in vitro binding and distribution of cyclosporin A in the blood
Authors: Lemaire M , Tillement J P 
Published: April 2011

Abstract
The distribution of cyclosporin A between plasma, leucocytes and erythrocytes was studied in vitro by means of sedimentation in Ficoll-Paque and dextran. The uptake by erythrocytes was found to be about 50% and the fraction of cyclosporin A bound to leucocytes amounted to 15%. Fractionation of plasma by ultracentrifugation also showed that two thirds of the drug were associated with lipoproteins whereas binding studies with isolated lipoproteins and plasma also indicated that lipoproteins were the major complexing constituents for cyclosporin A in plasma. The binding of cyclosporin A to erythrocytes and lipoproteins seems to be a linear process. The binding to the leucocytes may be a saturable process, however it is of minor importance in terms of the overall binding capacity in the blood.