bluuebunny/crossref_metadata_2025_split huggingface dataset:
Water vapour transmission properties of applied polymer films
Authors: BANKER GILBERT S , GORE ASHOK Y , SWARBRICK JAMES 
Published: April 2011

Abstract
The rates of moisture uptake by film-coated tablet matrices containing calcium chloride have been determined as a function of polymer coat formulation, film coat thickness and calcium chloride content of the matrix. The more hydrophilic polymer film formulations were less effective in reducing the rate of moisture uptake by the tablet matrices. A linear relation was observed between rate of moisture uptake and film thickness, in contrast to the log-log relationship obtained in previous work using the same systems cast as free films. Decreasing the calcium chloride content of the matrix caused an overall lowering of the moisture uptake rate. The results indicate that the water vapour transmission characteristics of these polymer film systems are not the same when assessed using the rate of moisture uptake of tablets coated with these films as when using the rate of water vapour transmission through the free films. It is suggested that films should not be accepted or rejected solely on the basis of transmission rates across free films but that due consideration should be given to the more meaningful moisture uptake rates of the film-coated dosage form.
The metabolism of ethionamide and its sulphoxide
Authors: JOHNSTON J P , KANE P O , KIBBY M R 
Published: April 2011

Abstract
The fate of orally administered ethionamide (2-ethyl-4-thiocarbamoylpyridine) and ethionamide sulphoxide in man, rats, mice and dogs has been examined. Though spontaneous interconversion between the two antituberculosis drugs does not take place, there was extensive interconversion in vivo, both appearing in the blood within 15 min of dosing irrespective of which compound was administered. Species differences were evident in both the rate of metabolism and in the ethionamide: ethionamide sulphoxide ratio. Apart from this interconversion, ten probable urinary metabolites were detected. These consisted of six fluorescent and four non-fluorescent metabolites, three of the latter being identified as 2-ethylisonicotinamide, 2-ethylisonicotinic acid and inorganic sulphate. A scheme is proposed to cover part of the common metabolic route of the two drugs.
Ionization constants and water solubilities of some aminoalkylphenothiazine tranquillizers and related compounds
Authors: GREEN A L 
Published: April 2011

Abstract
A simple graphical method is described for deriving the ionization constants of poorly soluble organic bases from the pH dependence of the water solubility. Ionization constants and water solubilities of 13 aminoalkylphenothiazines and related drugs have been determined using this procedure. Potent tranquillizing activity in this group of compounds is shown to be associated with a low water solubility at blood pH.
Analgesically active basic anilides: stereospecificity and structure of the basic group
Authors: CASY A F , HASSAN M M A 
Published: April 2011

Abstract
The synthesis of (RS)-, (R)- and (S)-N-(2-dimethylaminopropyl)propionanilide and the benzylmethylamino- analogues of methadone and isomethadone is described. The hot-plate activities in mice of the (S)- enantiomorphs of both the dimethylamino- and benzylmethylaminopropionanilides are greater than those of the corresponding (RS)- and (R)- forms, while the methadone and isomethadone analogues are inactive in the same test. These results support the view that 3-amino-1,1-diphenylpropyl- and basic anilide - analgesics differ in their modes of binding to the analgesic receptor site.
An in vitro model for soluble drug absorption
Authors: PERRIN JOHN 
Published: April 2011

Abstract
A physico-chemical model is proposed to simulate the transfer of a drug through a lipoidal membrane. The drug is transferred from a buffer of a pH found in the gut, through an immiscible organic liquid acting as the membrane, to a buffer of the plasma pH (7.4). The transfer of salicylic acid and amidopyrine obeys the theoretical equations. The apparatus used has the advantage that there is little or no danger of emulsion formation because of the lack of disturbance at the interface and the ease of removing samples for analysis.
Pharmacological properties of tetrahydropapaveroline
Authors: SANTI R , FERRARI M , TÓTH C E , CONTESSA A R , FASSINA G , BRUNI A , LUCIANI S 
Published: April 2011

Abstract
Tetrahydropapaveroline (thp) exerts β-sympathomimetic effects similar to those of isoprenaline. On guinea-pig isolated atria, thp elicits positive inotropic and chronotropic activities which are not abolished by previous reserpinization of the animals; on isolated mammalian heart these effects are associated with an increase in coronary flow. In the dog, thp increases myocardial contractile force and rate, elicits a hypotensive effect and stimulates respiratory activity in normal and reserpinized animals; when injected intra-arterially the drug causes vasodilatation. All the effects are prevented by the β-adrenergic blocking agents propranolol, dichloroisoprenaline and pronethalol. Structure-activity relationships between tetrahydroisoquinoline derivatives and their open-ring phenylethylamine congeners, which are closely related to sympathomimetic drugs, are discussed.
Some pharmacological effects and chemical properties of N-propargylnoratropine
Authors: DECSI L , VÁRSZEGI M K , NÁDOR K 
Published: April 2011

Abstract
N-Propargylnoratropine has been prepared from noratropine, and its structure proved by hydrogenation followed by alkaline hydrolysis. Some pharmacological effects of this compound have been compared with atropine. The central and peripheral cholinolytic activity is some 50% lower than that of atropine. There is a fourfold increase in the analgesic-disorientating action of atropine.
Chemical and pharmacological observations on some Hebe species
Authors: GRADY JUNE , LEWIS J J , MARTIN-SMITH M , MUIR T C , SUBRAMANIAN G 
Published: April 2011

Abstract
Examination of oven-dried leaves and twigs of four species of Hebe indigenous to New Zealand—H. stricta, H. odora, H. bollonsii and H. corriganii—has revealed D-mannitol and condensed tannins to be major constituents. Identification of some of the minor constituents, namely alkanes, fatty acids and aliphatic alcohols was achieved by means of gas-liquid chromatography. Pharmacological studies with the condensed tannin fractions of H. stricta and H. odora have indicated that the reputation of H. stricta as a constipatory agent is attributable to tannins; this agrees with earlier assumptions.
The mechanism of inhibition by salicylate of the pentose phosphate pathway in the human red cell
Authors: SMITH M J H , STURMAN J A 
Published: April 2011

Abstract
Salicylate inhibits the pentose phosphate pathway of glucose metabolism in human red cell haemolysates. The site of inhibition is concerned with glucose 6-phosphate and 6-phosphogluconate dehydrogenases and the mechanism of inhibition involves competition with nadp.
The rheology of some oil-in-water emulsions stabilized by condensed complex films
Authors: TALMAN F A J , DAVIES P J , ROWAN E M 
Published: April 2011

Abstract
The rheology of emulsions containing oleyl, lauryl or cetostearyl alcohol as the oil-soluble component has been examined. As the concentration of fatty alcohol was increased, three main types of behaviour were found. These could not be explained by the particle size distribution, phase weight ratio or internal phase viscosity. It is suggested that migration of oil-soluble component and subsequent formation of viscous gels in the aqueous phase accounted for the observed behaviour. The effects of temperature, type of oil phase and chemical constitution of water-soluble components, have also been examined.
Influence of dextrose on the viability of Bacillus subtilis
Authors: RICHARDSON G 
Published: April 2011

Abstract
Dextrose causes an increase in viable count of Bacillus subtilis and the effect is greater for spores than vegetative cells. The proportion of spores in which germination is initiated is not influenced by dextrose. During germination the ability of dextrose to affect the viable count is completely lost but re-appears as the germinated spore changes into a dividing vegetative cell. When spores are incubated in broth before plating in nutrient agar there is an increase in viable count followed by a fall before the increase in count due to division is detected. When plated in dextrose agar this initial rise is not seen and there is a fall in count before onset of division. The magnitude of the increase in count caused by dextrose is dependent on the method of plating. For maximum recovery of viable organisms the combination of roll-rube method with dextrose agar is to be preferred to surface plating with or without dextrose in the counting medium.
The effects of posterior pituitary hormones on isometric tension and isotonic shortening of the pig myometrium
Authors: KNIFTON A 
Published: April 2011

Abstract
Isotonic recording showed that uteri in the luteal stage of the oestrus cycle were more sensitive to oxytocin and vasopressin than those in the follicular stage. The uterine horn was more sensitive than the cervix. A comparison of isotonic and isometric recording revealed that the former exaggerated the response to oxytocin. Under isometric conditions there was no difference in sensitivity to oxytocin between progesterone-dominated and oestrogen-dominated uteri, but both were more sensitive than immature uteri. Tension developed in response to oxytocin was greatest in oestrogen-dominated, less in progesterone-dominated and least in immature uteri.
Acetylcholine in extracts and perfusates of urinary bladder
Authors: CHESHER G B 
Published: April 2011

Abstract
Tissue extracts of the urinary bladder of the rat, cat and guinea-pig contain an acetylcholine-like substance which is considered to be stored predominantly in post-ganglionic nerve fibres. An acetylcholine-like substance was liberated into the fluid bathing the isolated bladder of the guinea-pig and its output was increased 200-fold after transmural stimulation. The acetylcholine-like substance, both from bladder extracts (rat, cat and guinea-pig) and perfusates (rat), was found at the same Rf value as acetylcholine chloride when separated by paper chromatography in three solvent systems. It is concluded that the substance was acetylcholine.
A modification of a method for the evaluation of topical anaesthesia in the earthworm
Authors: SUSKEVICH JAMES , CAMPBELL ARTHUR H , LORD GEOFFREY H 
Published: April 2011

Abstract
The method of Block, Potts & Finney (1964) for the evaluation of local anaesthetic activity using the response of the earthworm tail to hydrochloric acid has been found to give false negative results with control solutions. This was because the acid progressively damaged and thus desensitized the tail. This has been overcome by arranging the test so that no tail is immersed in the acid more than three times during an assay.
The influence of anaesthetic agents on the formation of methaemoglobin induced by aniline in cats
Authors: McLEAN S , ROBINSON J , STARMER G A , THOMAS J 
Published: April 2011

Abstract
Administration of anaesthetic agents modifies the methaemoglobin formation induced by aniline in cats. The maximum amount of methaemoglobin is reduced, so too is the rate at which the methaemoglobin disappears. Studies with phenylhydroxylamine indicate that these changes are due to anaesthetics modifying the metabolism of aniline to phenylhydroxylamine rather than modifying the action of phenylhydroxylamine on systems within the red blood cell. The microsomal metabolism inhibitor SKF 525A has no effect on methaemoglobin formation induced by aniline.
The effect of various environmental factors on cocaine and ephedrine toxicity
Authors: PETERSON DONALD I , HARDINGE MERVYN G 
Published: April 2011

Abstract
The effect of environmental factors on the toxicity of ephedrine and cocaine has been examined and the results compared with those obtained with amphetamine. Ambient temperatures were identified at which these drugs have an “aggregation effect”, and isolated mice treated with ephedrine or cocaine were then forcibly exercised and the effect of increased motor activity on body temperature and mortality compared with the results obtained by grouping the animals together. In general, the toxicity of either drug is increased by a rise in ambient temperature. Both drugs produce an aggregation effect and forced exercise increases the toxicity of each drug as much as does grouping. In all parameters tested the effects of ephedrine and cocaine resemble qualitatively those of amphetamine, but are less potent. In mice given certain central nervous system stimulants the aggregation effect may be due to hyperpyrexia associated with increased spontaneous motor activity resulting from a greater response to external stimuli.
Effects of reserpine on the sensitivity of rat isolated uteri preparations to oxytocic drugs
Authors: KHAN I , QURESHI Z 
Published: April 2011

Abstract
Stimulant activity of the isolated uteri of female virgin rats to acetylcholine, 5-hydroxytryptamine, and oxytocin was examined quantitatively (4-point assay method) in anoestrus, induced oestrus (diethylstilboestrol 10μg/100 g body weight injected subcutaneously), reserpinized and stilboestrol-treated reserpinized animals. Each group had 30 animals. Reserpine was administered intraperitoneally in two doses each of 1 mg/kg body weight on the first and third days of dioestrus. The sensitivity to acetylcholine, 5-hydroxytryptamine and oxytocin of the uteri in induced oestrus was increased by 20, 86 and 730 times respectively. In the group of animals receiving reserpine alone the experiment could not be made due to persistant spontaneous activity (even up to 2 hr) of the uterine tissue. In the stilboestrol-treated reserpinized group, the sensitivity to all the oxytocic drugs was as low as in anoestrous tissue. Thus, stilboestrol injection failed to increase the sensitivity of the rat uteri to oxytocic drugs or to produce changes in the vaginal smear pattern. The possibility of progesterone being present in the tissue due to persistance of corpora lutea after reserpine is put forward.
Micelles as simple models of drug receptors
Authors: BECKETT A H , KIRK G , VIRJI A S 
Published: April 2011

Abstract
Some interactions of optically active N-alkyl-NN-dimethylalanine hydrobromide (alkyl betaine) micelles, representing model flexible drug receptors, with simple “drug” molecules, represented by a number of optically active amino-acids, choline derivatives and a dipeptide have been examined. Comparisons of these “drug-receptor” interactions have been made using a refractive index technique and an explanation of the difference in the degree of adsorption of different “drug” molecules at identical micelle surfaces is advanced.
A method for measurement and statistical analysis of large numbers of experimental tracings
Authors: CHRISTIANSON A H , DINNEEN L C , JAMES G W L , PERKINS A C 
Published: April 2011

Abstract
An accurate and rapid method of digitizing large numbers of experimental tracings is possible using a Pencil Follower (D-Mac). Its use in conjunction with a computer has meant that data, hitherto virtually unmanageable, can be subjected to full statistical analysis. An example of its application is cited.
Adrenoceptive receptors in the duodenum, aorta and atria of the rabbit
Authors: HILL ARNOLD J , KOHLI J D 
Published: April 2011

Abstract
pA10 values for the α-receptor blocking drug phentolamine against adrenaline, noradrenaline and phenylephrine were determined in rabbit aorta and duodenum, and for the β-receptor blocking drug propranolol, against adrenaline, noradrenaline and isoprenaline in rabbit atria and duodenum. The values for phentolamine against different amines were found to be similar, varying by less than half a log unit, between or within the tissues, as were the values for propranolol. These data provide quantitative evidence that α-receptors in the aorta and duodenum are similar, as are the β-receptors in the atria and duodenum, even though both types of receptor serve divergent functions in different tissues.
The biliary metabolites of butylated hydroxytoluene in the rat
Authors: LADOMERY L G , RYAN A J , WRIGHT S E 
Published: April 2011

Abstract
The biliary metabolites from intravenous and intraperitoneal doses of small amounts of [14C]butylated hydroxytoluene have been separated and estimated. The metabolites recognized were the alcohol (II), aldehyde (III) and acid (IV) together with small amounts of the diphenyl ethane (VI). Three other metabolites appear to be present in relatively large amounts. The pattern of metabolites in bile and urine has been compared. It is suggested that the relatively low excretion of the acid (IV) in the urine compared to bile is due to a selective reabsorption of this compound after biliary excretion.
Solubility and viscosity relations in the system ascorbic acid—water—polysorbate 80
Authors: NIXON J R , CHAWLA B P S 
Published: April 2011

Abstract
The solubility of ascorbic acid in dispersions of polysorbate 80 has been examined. Over a large region of the solubility range liquid crystal exists, bounded by isotropic liquid phases. Excess solubilizate separates out as crystalline material. The rheological properties are complex. Within the isotropic phases the viscosity is Newtonian, but as soon as liquid crystal is produced pseudoplastic or thixotropic flow occurs. In the centre of the liquid crystal region, there were concentrations exhibiting a “yield” value followed by relaxation before the usual thixotropic loop.
Some pharmacodynamic effects of the babesicidal agents quinuronium and amicarbalide
Authors: EYRE P 
Published: April 2011

Abstract
The intravenous injection of a therapeutic dose of quinuronium methylsulphate (1 mg/kg) causes a fall in blood pressure in sheep, which is partly prevented by mepyramine and abolished by atropine. Larger doses of quinuronium cause more marked hypotension and inhibition of respiratory movement, which are not affected by atropine. Quinuronium strongly increases the amplitude of contraction of the isolated rabbit heart. This effect is not antagonized by atropine or mepyramine. Contractions of plain muscle in the guinea-pig and sheep, and hypersecretion of gastric acid in the rat and of saliva in the sheep were all produced by quinuronium. The responses to acetylcholine were potentiated by quinuronium, an effect which was abolished by atropine. Amicarbalide isethionate by comparison was weakly active. The drug causes no change in blood pressure, smooth muscle contraction or salivary secretion, but stimulates gastric secretion and partially inhibits the actions of acetylcholine in these preparations.
Evaluation of potential antirheumatic drugs in vitro using lymphocytes and epithelial cells. The selective action of indoxole, methyl glyoxal and chloroquine
Authors: WHITEHOUSE M W 
Published: April 2011

Abstract
Anti-inflammatory steroids and non-steroid drugs rapidly inhibit the incorporation of radioactivity from tritiated uridine and thymidine into the nucleic acid fraction of cultured epithelial cells and lymphocytes obtained from sheep, rats, rabbits and chickens. Acidic (uncoupling) drugs were also found to inhibit protein synthesis in these particular cells, and protein and nucleic acid synthesis in other cells which were steroid-insensitive, DNA synthesis in epithelial cells and lymphocytes was inhibited by methyl glyoxal (pyruvaldehyde). Chloroquine selectively inhibited thymidine incorporation by the epithelial cells. Indoxole was a potent inhibitor of the metabolism of circulating lymphocytes incubated in protein-free media. These findings may indicate why some of these drugs suppress adjuvant arthritis in rats.
The fate of [14C]thalidomide in the pregnant hamster
Authors: HAGUE D E , FABRO S , SMITH R L 
Published: April 2011

Abstract
The embryotoxicity and fate of [14C]thalidomide in the pregnant European golden hamster have been investigated. Daily administration of thalidomide (1 or 2 g/kg orally) to pregnant hamsters on days 4–12 inclusive of pregnancy was not embryotoxic. [14C]Thalidomide (150 mg/kg) administered on the 204th hr of pregnancy is well absorbed and about 84% of the 14C is excreted in the urine and 9% in the faeces in the 3 days after dosing. The urinary 14C consists of thalidomide (3% of dose), α-(o-carboxybenzamido)glutarimide (26%), 2- and 4-phthalimidoglutaramic acids (8%), 2-phthalimidoglutaric acid (0.2%) and 2- and 4-(o-carboxybenzamido)-glutaramic acids plus 2-(o-carboxybenzamido)glutaric acid (27%). 14C is present in the embryo and the relative concentrations of radioactivity in the embryo and plasma are about the same at 4, 12 and 24 hr after dosing. At 4 hr after dosing the embryo contains mainly thalidomide, but at 12 hr this has largely disappeared and the 14C consists of seven hydrolysis products. The lack of embryotoxicity of thalidomide in the hamster is thus not due to an inability of the teratogen to penetrate to the conceptus.
Influence of the route of administration on the toxicity of some cholinesterase inhibitors
Authors: NATOFF I L 
Published: April 2011

Abstract
The acute median lethal doses of a series of cholinesterase inhibitors have been estimated in mice for different routes of administration Differences in the LD50 values obtained for intraperitoneal and oral routes (“hepatic” routes) and subcutaneous and intravenous routes (“peripheral” routes) suggest that the availability of the compound for metabolism by the liver is a major factor in their toxicity.
The metabolism of 5,5‘-methylenedisalicylic acid in various species
Authors: Davison Clarke , Williams R T 
Published: April 2011

Abstract
Commercial methylenedisalicylic acid has been shown to be grossly impure. Pure 5,5′-methylendisalicylic acid (4,4′-dihydroxydiphenylmethane-3,3′-dicarboxylic acid) has been prepared and labelled with 14C. The fate of the pure compound in the rat, mouse, hamster, rhesus monkey, rabbit, guinea-pig and chicken has been investigated. The compound is excreted entirely unchanged in the urine and faeces in all the above species and no metabolites have been found. The biliary excretion of the injected compound is high (50–60%) in the rat and dog and low (5%) in the guinea-pig and rabbit. In the monkey, rabbit and guinea-pig, the compound is excreted almost exclusively in the urine. In the rat about 50% of the dose is excreted in the faeces. In the mouse and hamster, the main route of excretion is the urine, about 10% appearing in the faeces.
Estimation of the stability of dry horse serum cholinesterase by means of an accelerated storage test
Authors: Cole B R , Leadbeater L 
Published: April 2011

Abstract
The thermal inactivation of dry horse serum cholinesterase was found to obey first order kinetics over the temperature range 38–140°. Rogers' (1963) accelerated storage test was applied to this reaction and gave estimates of the rate coefficients and energy of activation of the inactivation reaction which agreed with the values determined in isothermal experiments. The stability of the enzyme preparation at 38° predicted by means of the accelerated storage data coincided with that found by isothermal storage of the enzyme at 38°.
The distribution of salicylate in mouse tissues after intraperitoneal injection
Authors: Sturman J A , Dawkins P D , McArthur N , Smith M J H 
Published: April 2011

Abstract
The concentrations of salicylate and its principal metabolites were measured in blood, liver, brain, kidney, heart, spleen, diaphragm and skeletal muscle after the intraperitoneal injection of a fixed amount of radioactive salicylate and varying doses of unlabelled salicylate. The patterns of distribution of salicylate in the various organs with time were similar, the peak level being attained in 30–60 min after injection. Salicylate was eliminated from the blood after 8 hr but persisted in liver in measurable amounts up to 24 hr.