bluuebunny/crossref_metadata_2025_split huggingface dataset:
The diuretic activity of clorexolone and some related phthalimides and 1-oxoisoindolines
Authors: CORNISH E J , LEE G E , WRAGG W R 
Published: April 2011

Abstract
N-Substituted 4-chloro-5-sulphamoylphthalimides showed diuretic activity in the rat. Reduction of the carbonyl group in the position para to the 5-sulphamoyl group in the phthalimides produced even more active compounds. The relationship between potency and the nature of the N-substituent was examined in 32 phthalimides and 10 reduced derivatives. Maximum potency was found in the N-cycloalkyl and N-cycloalkylmethyl compounds, one of which, 5-chloro-2-cyclohexyl-1-oxo-6-sulphamoylisoindoline (clorexolone), was 300 times as active as chlorothiazide in the rat. This compound was examined in more detail in both the rat and the dog.
The analgesic and related properties of 6-deoxy-6, 6-ethylenedioxy-7, 8-dihydro-14-hydroxycodeine hydrochloride
Authors: BARRON D I , HALL PATRICIA L , VALLANCE D K 
Published: April 2011

Abstract
The compound 6-deoxy-6, 6-ethylenedioxy-7, 8-dihydro-14-hydroxycodeine hydrochloride possesses analgesic potency greater than either morphine or codeine when examined by a variety of methods in mice and rats. Compared with these two analgesics the compound showed greater separation between effective analgesic doses and doses producing inhibition of gastrointestinal motility or death, but not for mydriasis or respiratory depression. Some evidence for a lower addictive liability than morphine is discussed.
The electrically stimulated ileum of the guinea-pig for measuring acetylcholine antagonism at different sites
Authors: LEACH G D H 
Published: April 2011

Abstract
The transmurally stimulated guinea-pig ileum preparation was used to determine quantitatively the antagonism developed by hexamethonium and atropine against the emptying reaction and the longitudinal muscle response. Hexamethonium in concentrations of 1·5–6·0 μg/ml blocked the emptying reaction but larger doses, 8–10 μg/ml, failed to depress the longitudinal response to less than 50% of its original height. Atropine, on the other hand, in concentrations of 0·001–0·02 μg/ml, reduced the longitudinal response without affecting the emptying reaction. Thus, the preparation discriminates between acetylcholine antagonists acting at either the nicotinic or muscarinic site.
Enlargement of salivary glands in rats after chronic administration of physalaemin or isoprenaline
Authors: BERTACCINI G , DE CARO G , CHELI R 
Published: April 2011

Abstract
Chronic administration of physalaemin and isoprenaline to rats produced a significant salivary glands enlargement which was moderate (34% fresh weight increase and 48% dry weight increase compared with control glands) after the peptide administration and striking after the amine (630% fresh weight increase and 600% dry weight increase compared with control glands). Physalaemin caused only hypertrophy of the gland, whereas isoprenaline induced a marked hyperplasia.
Pyrazolotriazines: a new class of tumour-inhibitory agents
Authors: BALDWIN R W , PARTRIDGE M W , STEVENS M F G 
Published: April 2011

Abstract
A series of pyrazolo-as-triazines have been screened for tumour-inhibitory activity against sarcoma S 180 in mice and a methylcholanthrene-induced tumour in rats. The antitumour activities of ethyl 4-aminopyrazolo[3,2-c]-as-triazine-3-carboxylate (Ig), 6-acetyl- and 6-iodoacetyl-3-methyl-4-methylenepyrazolo[3,2-c]-as-triazine (IIa and IIb respectively) against sarcoma S 180 exceed the inhibitory activity of 6-mercaptopurine against the same tumour.
Germination rate of spores of Bacillus megaterium
Authors: HAMBLETON R , RIGBY G J 
Published: April 2011

Abstract
THE most commonly accepted criteria of bacterial spore germination are loss of heat resistance, acquisition of stainability by simple stains and a change in absorbance (Wynne & Foster, 1948; Powell, 1951; Pulvertaft & Haynes, 1951; Levinson & Sevag, 1953). To these might be added a decrease in resistance to certain germicides. Although it has been suggested that some of these changes occur simultaneously (Campbell, 1957), most of the evidence for this is qualitative rather than quantitative.
The effects of the addition of manganese dioxide to media on the viability of bacteria damaged by x-rays, phenol and radiomimetic agents
Authors: HARRIS N D , WHITEFIELD M 
Published: April 2011

Abstract
Suspensions of two strains of Escherichia coli were counted before and after damage by phenol, X-rays and radiomimetic substances on nutrient agar which had been treated in various ways with manganese dioxide. The medium after some treatments gave increased counts with cells damaged by phenol and dimethyl busulphan and with undamaged cells, the strains responding rather differently. The beneficial action of manganese dioxide was not due to the breakdown of peroxides in the medium and may be due to the adsorption of toxic substances from the medium.
The effect of peptone on the inactivation of a bacteriophage by chemical antimicrobial agents
Authors: BROWN W R L , THOMAS A H 
Published: April 2011

Abstract
BECAUSE of their intracellular parasitic nature, infectious virus particles are almost invariably closely associated with substances derived from the host organism. In the chemical disinfection of virus contaminated material, the possible interference in the action of the inactivating agent by extraneous organic matter is therefore of particular importance. Little quantitative information on such effects is available however. Peptone reduces the activity of formaldehyde, phenol and sodium hypochlorite against Bacillus subtilis spores (Bullock & Rawlins, 1950, 1954) and it has been used here to illustrate the effect of non-viral organic matter on the chemical inactivation of a bacterial virus.
A method for the evaluation of some oral prolonged-release forms of dexamphetamine in man, using urinary excretion data
Authors: BECKETT A H , TUCKER G T 
Published: April 2011

Abstract
ALTHOUGH urinary excretion studies (Campbell, Nelson & Chapman, 1959; Chapman, Shenoy & Campbell, 1959; Shenoy, Chapman & Campbell, 1959) have been used as a technique to evaluate prolonged-release dosage forms of amphetamine, the significance of the results is in doubt because of the use of non-specific assay methods and the failure to control urinary pH. The use of radioactive material has indicated the similarity between a dose of 5 mg amphetamine three times a day and a 15 mg prolonged release preparation (Rosen, Tannenbaum, Ellison, Free & Crosley, 1965).
The metabolism and excretion of lignocaine in man
Authors: BECKETT A H , BOYES R N , APPLETON P J 
Published: April 2011

Abstract
The urinary excretion of lignocaine and monoethylglycinexylidide (megx) has been studied in man. The finding that megx is a major metabolite of lignocaine in man is discussed in relation to studies in animals reported by other workers. An analogue computer model was constructed to simulate the metabolism and excretion of lignocaine. By varying the model parameters it was possible to obtain good agreement between the calculated and empirical excretion data for both lignocaine and its metabolite megx. Because of this good agreement, the computer was used to predict body levels of the compounds after a dose of lignocaine.
Comparative anatomy of the leaves of Voacanga schweinfurthii Stapf and Voacanga africana Stapf
Authors: NEWCOMBE F , PATEL B A 
Published: April 2011

Abstract
There is a marked similarity in the anatomical structures of the leaves of the closely related species Voacanga schweinfurthii and V. africana which are here described and compared. The evidence suggests that these two species should be considered as a single species.
Histamine gastric ulceration and its prevention by degraded carrageenan: the effect of aminoguanidine sulphate
Authors: ANDERSON W , SOMAN P D 
Published: April 2011

Abstract
Pretreatment of the guinea-pig with intravenous aminoguanidine sulphate, a drug believed to inhibit histaminase, changes the gastric ulcer response following a dose of histamine acid phosphate (2·5 mg/kg) which elicits a submaximal ulcer response, to that of a dose (5 mg/kg) which normally elicits a maximal gastric ulcer response. A reduction in the volume and acidity of secretion also occurs. Intraduodenal administration of degraded carrageenan prevents this action of aminoguanidine. Conversely, in the presence of aminoguanidine, carrageenan fails to protect against histamine ulceration.
Radial voidage variation in randomly-packed beds of spheres of different sizes
Authors: RIDGWAY K , TARBUCK K J 
Published: April 2011

Abstract
The packing arrangement of the particles in a tablet die, before pressing, has no hitherto been considered as a variable in the tabletting process. Because of the complexity of this subject, the present investigation has been restricted to monosized and binary mixtures of spheres in a cylindrical container. The container could be revolved at speeds in excess of 1,000 rpm so that the thickness of an annular layer of water could be measured. From this, the voidage at any radial position could be found. The plot of voidage against distance from the cylindrical wall is a wave form which is damped out after about 5 particle diameters. For packings of monosized spheres the oscillations are regular. There appear to be two kinds of binary mixtures, those in which the particle sizes are similar, and those where the diameter ratio is greater than 0·4. The voidages calculated by suitably weighting the values for each component are in agreement with the measured voidages of the first kind but not with those of the second. Because there is an initial distribution of voidage, it is concluded that there must be some radial movement of the particles during the compacting operation.
Some angular properties of magnesia and their relevance to material handling
Authors: JONES T M , PILPEL N 
Published: April 2011

Abstract
By measuring the angular characteristics of magnesia over a range of particle sizes from 30–3000 μ, it has been possible to determine the factors which influence the shapes of heaps, cones and wedges of the material, formed under a variety of experimental conditions. The relevance of the measurements to quality control, flow-ability, hopper and chute design and material handling is discussed.
Cortisone acetate crystal forms
Authors: CARLESS J E , MOUSTAFA M A , RAPSON H D C 
Published: April 2011

Abstract
Infrared spectroscopy and differential scanning calorimetry data are given for the characterisation of three anhydrous and two hydrated crystal modifications of cortisone acetate. All forms revert to the same form on heating to 200°. The amount of hydration estimated from thermal analysis varies from half to one molecule of water per molecule of cortisone acetate. Methods for the preparation of the five forms are described emphasising the importance of solvent composition, particularly its water content. Interconversion of these forms under various conditions such as grinding, contact with water and heat treatment is discussed.
Enzymatic decyanation of cyanocobalamin in rat tissues
Authors: CIMA L , LEVORATO C , MANTOVAN R 
Published: April 2011

Abstract
Cyanocobalamin is decyanated in vitro to hydroxocobalamin by rat liver and kidney. This appears to be due to an enzyme system which we have called “cyanocobalamindecyanase”. The enzyme is in the soluble fraction of the cells; it requires reduced cozymases and flavins and has an optimum pH of 7.2 under anaerobic conditions. This is consistent with the fact that conversion of cyanocobalamin to hydroxocobalamin and/or its reduced forms (B12r, B12s) involves a reductive process in the earliest stage of the biosynthesis of coenzyme B12.
Synthesis and antiprotozoal activity of some nitro(nitroaryl)imidazoles
Authors: ELLIS G P , EPSTEIN C , FITZMAURICE C , GOLBERG L , LORD G H 
Published: April 2011

Abstract
A series of 5(4)-nitro-4(5)-nitroarylimidazoles has been synthesized and their in vitro antifungal and antiprotozoal activities have been studied. The compounds may be prepared by dinitration of an arylimidazole or by mononitration of either an aryl-nitroimidazole or a (nitroaryl)imidazole. In some of the compounds the ring nitrogen atom has been substituted. Several compounds exhibit high in vitro antitrichomonal activity against Trichomonas vaginalis and T. foetus, and a moderate activity against Histomonas meleagridis and Entamoeba histolytica. The chemical structure and antimicrobial activity of these and other imidazoles previously studied are briefly discussed.
Probable conformations of the analgesically active basic anilide N-[(2-benzylmethylamino)propyl]-propionanilide
Authors: CASY A F , HASSAN M M A 
Published: April 2011

Abstract
A spectroscopic (ultraviolet, infrared and nuclear magnetic resonance) study of N-[(2-benzylmethylaminp)propyl]propionanilide hydrochloride is reported and probable conformations of this molecule (in which the phenyl group and amide function are non-planar, the protonated basic centre lies close to the amido-nitrogen atom, and the secondary methyl group is removed from the region above the aromatic plane) proposed on the basis of the spectroscopic results. Differences in analgesic stereospecificity and basic group structure between enantiomorphs of methadone and N-[(2-benzylmethylamino)propyl]propionanilide are discussed in terms of the probable conformations of the two analgesics.
Molecular interactions of caffeine with o-, m- and p-iodobenzoic acids and o-, m- and p-fluorobenzoic acids
Authors: DONBROW M , BEN-SHALOM H 
Published: April 2011

Abstract
The solubilities of o-, m- and p-iodo- and fluorobenzoic acids in aqueous solutions of caffeine increase linearly with caffeine concentration due to complex-formation. Insoluble complexes are formed by the o- and m-acids and soluble ones by the p-acids. Approximate 1:1 stability constants have been evaluated from the phase diagrams and their values are considered in relation to possible mechanisms of complex-formation.
Viscosity of phospholipid sols
Authors: PERRIN J , SAUNDERS L 
Published: April 2011

Abstract
The viscosities of lysolecithin sols in water were found to be Newtonian at the concentrations investigated. A Couette viscometer was used. In the mixed sols containing both lysolecithin and lecithin, thixotropy was absent at all ratios and only the sol with a high lecithin fraction showed some non-Newtonian behaviour. The axial ratio of the mixed micelles calculated by the Simha method varies with the lecithin/lysolecithin ratio, rising to a maximum when the phospholipid mixture is of one mole lecithin to two moles lysolecithin. This phenomenon is probably due to the packing of the various hydrophobic groups in the micelle.
Uncoupling of oxidative phosphorylation by glycyrrhetic acid, fusidic acid and some related triterpenoid acids
Authors: WHITEHOUSE MW , DEAN P D G , HALSALL T G 
Published: April 2011

Abstract
Some new derivatives of 18α- and 18β-glycyrrhetic acid and oleanolic acid were tested for their ability to inhibit phosphorylation coupled to succinate oxidation in rat liver mitochondria. Glycyrrhetic acid is a potent uncoupler of oxidative phosphorylation (approaching 2,4-dinitrophenol in potency); uncoupling activity is dependent upon each of the following functional groups: 3-hydroxy, 11-oxo and 30-carboxyl groups. Inversion of the configuration at C-18 (D/E ring junction) or replacement of the 11-oxo-12-ene system in ring C by the 9(11),12-diene system in glycyrrhetic acid abolished uncoupling activity. By contrast, the hemisuccinates (3-O-carboxypropionyl derivatives) of 18α-glycyrrhetic acid and of the 18β-9,12-diene acid were moderately potent uncoupling agents but less active than 18β-glycyrrhetic acid. The uncoupling activity of these hemisuccinates could not be attributed to the carboxypropionyl group alone. Structural analogues of various glycyrrhetic acid derivatives prepared from oleanolic acid (with the carboxyl group at C-28) were less active in uncoupling oxidative phosphorylation than the corresponding compounds in the glycyrrhetic acid series (with the carboxyl group at C-30). The uncoupling activity of some derivatives of two naturally occurring tetracyclic triterpenoid acids, polyporenic acid A and fusidic acid, was also investigated and found to largely depend upon their chemical structure. The possible application of these compounds as drugs in man is discussed.
Interaction of anti-inflammatory drugs with serum proteins, especially with some biologically active proteins
Authors: Mizushima Y , Kobayashi M 
Published: April 2011

Abstract
The interaction of clinically established anti-inflammatory drugs with some proteins has shown these drugs to strongly inhibit heat coagulation of whole serum at a concentration attainable in the sera of patients. Phenylbutazone and sodium salicylate do not inhibit the biological activity of three biologically active and labile serum proteins, namely, necrotizing factor, heterogenous serum and complement. However, they do influence the effect of heat on these proteins. The relation between this drug action in vitro and the possible mode of action of the proteins in vivo is discussed.
The effect of a non-ionic surfactant upon the antifungal activity of benzoic acid
Authors: Humphreys K J , Richardson G , Rhodes C T 
Published: April 2011

Abstract
The effect of a non-ionic polyoxyethylene surfactant upon the fungicidal activity of benzoic acid has been investigated by a viable count method. The results show that theories equating antimicrobial activity to the concentration of non-micellar preservative are inadequate. The significance of these findings is discussed and some possible additional factors involved in the fungicidal process indicated.
The preparation and properties of (+)- and (−)-guanoxan
Authors: Stenlake J B , Breimer D D , Smail G A , Stafford Anne , Bowman W C 
Published: April 2011

Abstract
(±)-2-Aminomethyl-1, 4-benzodioxan has been resolved into its optically active isomers: (+)- and (-)-guanoxan have been synthesized from these. The pharmacological effects of racemic-guanoxan and of the two optical isomers have been compared on the isolated central ear artery of the rabbit, on the pithed rat in which pressor responses were evoked by stimulation of the thoraco-lumbar sympathetic outflow, and on the pre- and post-ganglionically stimulated nictitating membrane of the cat. The two isomers were equipotent in producing adrenergic neuron blockade. Initial catecholamine release was weak in the cat, but occurred more powerfully in the rabbit ear artery and in the rat. Ability to produce this effect resided mainly with the (+)-isomer. α-Adrenoreceptor blocking activity was detectable in the rat and was produced mainly by the (+)-isomer suggesting that its stereochemical configuration corresponds to that of D-(-)-noradrenaline. Ganglion blockade was an unimportant action of the compounds, but both isomers possessed weak atropine-like activity in the rat.
The effect of alloxan diabetes upon adjuvant-induced arthritis in the rat
Authors: Best R , Spencer P S J 
Published: April 2011

Abstract
THE relation between inflammation and carbohydrate metabolism has been the subject of several investigations using acute inflammatory models such as the anaphylactoid reaction in the rat (Adamkiewicz & Adamkiewicz, 1959; 1960) and true anaphylaxis in the rat and mouse (Kraus, 1964; Gulbenkian, Yanell Grasso & Tabachnick, 1967; Dhar, Sanyal & West, 1967). These acute inflammatory reactions are depressed by the hyperglycaemia produced by alloxan (Adamkiewicz & Adamkiewicz, 1959; 1960), by 2-deoxyglucose (Goth, 1959), by glucose loading (Dhar & others, 1967) and by glucagon (Lefebvre & Van Cauwenberge, 1962).
Using the model of “adjuvant arthritis” in the rat, produced by the injection of Freund's adjuvant (Pearson, 1956), Kellett (1965) showed that this chronic arthritic condition was also suppressed when alloxan diabetes was induced in rats before an injection of adjuvant. The syndrome of adjuvant arthritis occurs in two phases, firstly an acute inflammatory oedema at the injection site which is followed after a latent period of about ten days by a secondary, chronic polyarthritis involving all limbs and the tail.
Because of the biphasic course of the inflammation, and the possible dependence of the chronic phase on the prior appearance of an adequate initial phase, we decided to investigate the effect of alloxan diabetes induced at various times during the development of the adjuvant arthritic syndrome.
Synthesis and pharmacological action of some N-alkyl morpholines and their salts
Authors: Beckett A H , Hunter W H , Kourounakis P 
Published: April 2011

Abstract
The preparation is described of some 2-hydroxy-2- and 4-alkylmorpholines by ring closure of the corresponding phenacyl hydroxyalkylamines. The influence of structure upon the ring closure reaction is examined and the weak pharmacological action of the title compounds on leptazol convulsions, the autonomic nervous system and in the mouse hot-plate test is discussed in relation to the reversed esters of pethidine.
The effect of acetylsalicylic acid, phenylbutazone and indomethacin on the binding of 11-hydroxysteroids to plasma proteins in patients with rheumatoid arthritis
Authors: Stenlake J B , Davidson A G , Jasani M K , Williams W D 
Published: April 2011

Abstract
Plasma concentrations of total and unbound 11-hydroxysteroids in patients with rheumatoid arthritis have been determined using a fluorimetric method before and after administration of acetylsalicylic acid, phenylbutazone and indomethacin. Unbound 11-hydroxysteroids were measured in plasma ultrafiltrates obtained using the Toribara apparatus. Enhancement and quenching of fluorescence by acetylsalicylic acid, phenylbutazone, and indomethacin, and heparin used as an anticoagulant in the blood samples, have been shown to be absent. The results show that acetylsalicylic acid, phenylbutazone and indomethacin given in recommended therapeutic doses for periods of one week have no significant effect on plasma protein-binding of 11-hydroxysteroids.
The effect of anti-inflammatory drugs on the protein-binding of 11-hydroxysteroids in human plasma in vitro
Authors: Stenlake J B , Williams W D , Davidson A G , Downie W , Whaley K 
Published: April 2011

Abstract
The effect of acetylsalicylic acid, ibufenac, indomethacin, oxyphenbutazone and phenylbutazone on the protein-binding of 11-hydroxysteroids in vitro at concentrations in excess of normal has been examined in human blood bank plasma, in plasma from women in the third trimester of pregnancy, and in plasma from patients after injections of tetracosactide. Phenylbutazone, ibufenac and indomethacin do not significantly affect the protein-binding of 11-hydroxysteroids. Oxyphenbutazone causes a decrease in the proportion of unbound 11-hydroxysteroids and acetylsalicylic acid produces an increase of unbound 11-hydroxysteroids.
The absolute configurations of the alkaloids of Physostigma venenosum seeds
Authors: Longmore R B , Robinson B 
Published: April 2011

Abstract
The absolute configuration of physostigmine has been established by correlating the configuration of its C-3a atom with that of the asymmetric carbon atom in (+)-3-ethyl-3-methoxycarbonyl-3-methylpropionic acid. Comparison of the optical rotatory dispersion spectra of physostigmine, Na-norphysostigmine, geneserine, physovenine and eseramine have shown that all five alkaloids have the same absolute configurations.