bluuebunny/crossref_metadata_2025_split huggingface dataset:
The analgesic properties of some 14-substituted derivatives of codeine and codeinone
Authors: Buckett W R , Farquharson Muriel E , Haining C G 
Published: April 2011

Abstract
The effects of 14-hydroxylation and subsequent 14-acylation on the toxicity and analgesic activity of codeine, codeine-6-acetate, codeinone, and Δ7-deoxycodeine have been examined in rats and mice. Acute toxicity was reduced in each instance by the introduction of a 14-hydroxy group and was not generally enhanced by its esterification. 14-Acetoxycodeine was approximately equal to morphine in potency and esterification at the 14-position of hydroxycodeine with other straight chain aliphatic acids containing up to 5 carbon atoms failed to enhance analgesic potency further. 14-Benzoylation of either 14-hydroxycodeine or 14-hydroxycodeinone had little effect on analgesic activity but the introduction of a methylene group between the carboxyl group and the phenyl ring enhanced potency considerably in each case. Increasing the number of carbon atoms from 2 to 5 in the 14-acyl groups of esters of 14-hydroxycodeinone and 14-hydroxy-Δ7-deoxycodeine led to a gradual increase in analgesic activity. In rats the n-valeryl ester of 14-hydroxy-Δ7-deoxycodeine was estimated to have 75 times the potency of morphine.
The anti-anaphylactic activity of theophylline and some related xanthine derivatives
Authors: Firth A , Smith W G 
Published: April 2011

Abstract
Theophylline and theobromine, but not caffeine and xanthine, protect sensitised guinea-pigs against anaphylactic shock induced by aerosolised antigen. There is an inhibition of release of slow reacting substance of anaphylaxis and some reduction in histamine release. The lung lipid changes associated with anaphylactic shock are prevented by pre-treatment with theophylline.
Method of graphical analysis of 2 + 2 and 3 + 3 biological assays with graded responses
Authors: Warner B T 
Published: April 2011

Abstract
Three examples of 2+2 and 3+3 biological assays with graded responses are analysed graphically. The method described has the advantage that only two “general purpose” nomograms are necessary for the analysis of assays with a wide range of ratios of successive doses and numbers of observations; assays with block restrictions may also be analysed. The accuracy of the method is discussed. An appendix gives the theory of the method and of the construction of the nomograms.
Absorption of ephedrine onto sulphonic acid cation-exchange resins
Authors: Chaudhry N C , Saunders L 
Published: April 2011

Abstract
Detailed studies of the kinetics of absorption of ephedrine onto the sulphonic acid cation-exchange resins have been made and most of the results have been interpreted by the particle diffusion theory of Boyd, Adamson & Myers (1947). The rate constant has been found to be inversely proportional to the square of particle radius and also dependent on the solution concentration, the temperature and the cross-linking of the resin. Absorption of ephedrine onto the 9% cross-linked (C.L.) resin proceeds to its capacity from ephedrine solution and not from ephedrine hydrochloride solution when experiments are made in closed tubes; with 13.5% C.L. resin, absorption does not proceed to capacity even after 2 months. The rate constant of absorption of ephedrine onto the sodium form of the resin is low as compared with the hydrogen form. In most cases diffusion coefficients have been calculated.
Sorption of water vapour and surface activity of ghatti gum
Authors: Elworthy P H , George T M 
Published: April 2011

Abstract
The sorption of water vapour by three fractions of sodium ghattate has been studied at 25° and 40°. The results were fitted by Brunauer, Emmett & Teller plots at low relative vapour pressures. Calculations of the differential heats and entropies of sorption gave initially exothermic ΔH̄ values and negative ΔS̄ values. As the sorption proceeded the signs of the thermodynamic properties became positive The mechanism of sorption onto different parts of the macromolecules was discussed.
The surface tension of one sodium ghattate fraction was measured in water, 0.05 and 0.5 N sodium chloride solution, as a function of concentration, using the sessile drop method. The presence of salt enhanced the surface activity. A structure for the adsorbed film is suggested.
Some 2-Iminoselenazolidin-4-ones and related compounds
Authors: Comrie A M , Dingwall D , Stenlake J B 
Published: April 2011

Abstract
A series of 2-iminoselenazolidin-4-ones, selenazolidine-2,4-diones and some 2-alkylidenehydrazones have been synthesised. Wide-range screening for biological activity failed to reveal any compounds of promise.
Some possible causes of pharmacological activity in blank eluates following the separation of sympathomimetic catecholamines by paper chromatography
Authors: Roberts D J 
Published: April 2011

Abstract
Eluates prepared from paper chromatograms at Rf values and under experimental conditions that were expected to eliminate the possibility of contamination with catecholamines were shown to inhibit the rat uterus and to cause a fall in the mean arterial blood pressures of anaesthetised rats. These isoprenaline-like actions have been shown to be due to inadequate removal of the phenolic developing solvent and to the use of sodium dihydrogen phosphate solutions as eluants. Attempts to establish qualitative and quantitative relationships between the chromatography blank and isoprenaline have failed, and it is concluded that these factors could not alone be responsible for the isoprenaline-like substance reported to occur naturally in various species of mammal.
The solubilisation and inactivation of preservatives by non-ionic detergents
Authors: Evans W P 
Published: April 2011

Abstract
A novel potentiometric method, which depends on the pH changes which occur when an acidic material is solubilised, has been used to determine the solubilisation of the weakly acidic preservative, p-hydroxybenzoic acid, in a non-ionic detergent. From the pH changes observed, the partition coefficient, Km, for the distribution of the un-ionised acid between the micellar and the aqueous phase has been calculated and found to be 2.8 × 103. Specific interaction between the acid and the detergent. to form a complex is shown not to be important. It is suggested that the arguments against specific interaction apply generally to other preservatives and non-ionic detergents.
The site of action of sympathomimetic amines on the circular muscle strip from the guinea-pig isolated ileum
Authors: Harry J 
Published: April 2011

Abstract
The circular muscle strip of the isolated ileum of the guinea-pig, treated with the anticholinesterase mipafox (100 μg/ml) responds to doses of methacholine or carbachol with contractions that are inhibited by previous doses of noradrenaline, adrenaline or isoprenaline in that order of potency. Piperoxane antagonised the inhibitory action of adrenaline, but not that of aminophylline. Dichloroisoprenaline did not antagonise the action of adrenaline on the circular muscle strip. It is concluded that the site of action of the sympathomimetic amines on the circular muscle of the guinea-pig ileum is located at postganglionic neuro-effector junctions in the smooth muscle.
Hydroxylation in vitro of pharmacologically active phenothiazine derivatives
Authors: Robinson Ann E , Beaven Vida H 
Published: April 2011

Abstract
The hydroxylation of promazine, chlorpromazine, chlorproethazine, triflu-promazine and promethazine by a rat liver preparation is described. It is concluded that promazine is converted to 3-hydroxypromazine by this system.
Note on the cardiac effects of nystatin
Authors: Arora H R K 
Published: April 2011

Abstract
Nystatin, a polyene antifungal antibiotic, induces systolic arrest of the isolated hearts of the frog, rat or rabbit. In the frog, heart failure induced by raising venous pressure was antagonised and the cardiac outflow was increased. Coronary flow in the perfused heart of the rat or rabbit was decreased.
Effects of tyramine on a spinal reflex in the anaesthetised chick
Authors: Bowman W C , Callingham B A , Osuide G 
Published: April 2011

Abstract
The effects of tyramine on polysynaptic spinal reflexes in anaesthetised chicks and cats have been studied. Very large intravenous doses of tyramine depressed the reflexly evoked contractions of skeletal muscles by an action exerted in the spinal cord. Since tyramine is normally present in the central nervous system, its function may be to exert some inhibitory controlling influence on muscular activity.
Gamma-irradiation of spores of Bacillus subtilis
Authors: Cook A M , Roberts T A 
Published: April 2011

Abstract
Freeze-drying from a 5% aqueous solution of glucose produced a marked protection of spores of Bacillus subtilis subjected to spent fuel gamma-irradiation over the range 2·5–12·5 × 105 rads. Freeze-drying from aqueous suspension produced no protection. Irradiation in 5% aqueous glucose and in aqueous suspension gave log % survivor/dose regressions with similar slopes.
Hypoglycaemic agents
Authors: Hayman D F , Petrow V , Stephenson O 
Published: April 2011

Abstract
Various 3-substituted derivatives of 1-(p-vinylbenzenesulphonyl)urea, 1-[p-(2-chloroethyl)benzenesulphonyl]urea and 1-[p-(2-bromoethyl)benzenesulphonyl]urea are described. Several of the compounds possess noteworthy hypoglycaemic activity on oral administration in rabbits. In contrast, several related 5-substituted derivatives of 2-[p-(2-chloroethyl)benzenesulphonamido]-1,3,4-thiadiazoles and -1,3,4-oxadiazoles were virtually inactive.
Spectrophotometric method for the estimation of guanethidine
Authors: Bose B C , Vijayvargiya R 
Published: April 2011

Abstract
A spectrophotometric method for the estimation of guanethidine sulphate, based on the development of blue colour in alkaline medium after reaction with lithium and sodium molybdophosphotungstate B.P. reagent, is described. The method is more sensitive and rapid than the existing British Pharmacopoeia methods. Both powder and tablets can be estimated by this method.
Urethane anaesthesia and pituitary-adrenal function in the rat
Authors: Spriggs T L B , Stockham M A 
Published: April 2011

Abstract
Urethane anaesthesia produced a prolonged hypersecretion of ACTH as shown by plasma and adrenal corticosterone and adrenal ascorbic acid changes. There was also a concurrent depletion of the adrenaline content of the adrenal gland. Adrenal demedullation did not prevent the steroid changes induced by the anaesthetic. Hyperactivity of the pituitary-adrenal axis for 24 hr in the urethane-anaesthetised rats did not prevent further alteration of steroid levels in response to a stress.
Inactivation of a bacteriophage by chemical antibacterial agents
Authors: Cook A M , Brown W R L 
Published: April 2011

Abstract
An extinction method has been used to examine the inactivation of coliphage T6r by a number of chemical antibacterial agents. A marked difference in the effect of concentration on inactivation efficiency has been shown for different agents, chloramine-T and formaldehyde having concentration exponents of approximately 2 and 3 respectively; crystal violet, cetrimide and phenol having concentration exponents of approximately 11, 13 and 15 respectively. It is suggested that a low concentration exponent is associated with inactivation of the phage by an effect on the protein coat of the particle and a high concentration exponent with an effect on its internal structure.
A phytochemical investigation of Trigonella corniculata Linn.
Authors: Atal C K , Sood S P 
Published: April 2011

Abstract
The extraction of ground seeds of Trigonella corniculata with light petroleum has yielded triacontane and 22,23-dihydrostigmasterol. Further extraction of the seeds with ethanol yielded choline and betaine. Trigonelline, the major alkaloid of Trigonella foenum-graecum was not found.
Determination of methyl salicylate in pharmaceutical preparations
Authors: Stevens S G E , Warren B 
Published: April 2011

Abstract
A method based on gas-liquid chromatographic technique is described for the determination of methyl salicylate in pharmaceutical preparations. 10% carbowax 20M is used as a stationary phase to resolve mixtures containing amyl, ethyl and methyl salicylates, menthol and camphor. The determinations are based on the area triangulation method against a diphenyl reference standard.
The effect of Polysorbate (Tween) 80 on the growth rate of Pseudomonas aeruginosa
Authors: Brown M R W , Richards R M E 
Published: April 2011

Abstract
Problems associated with growth rate measurement for Pseudomonas aeruginosa have been investigated. There is an apparent change in the rate of growth at an early stage when determined spectrophotometrically. This change is associated with cell clumping. The presence of polysorbate 80 in the culture medium eliminated this effect. The reproducibility of the growth rate measurement has been established.
The relationship between analgesic activity, acute toxicity and chemical structure in esters of 14-hydroxycodeinone
Authors: Buckett W R 
Published: April 2011

Abstract
Acylation of 14-hydroxycodeinone with long chain unbranched fatty acids produced compounds of varying analgesic potency, maximal activity being in 14-n-heptoyl-oxycodeinone. In 14-phenylalkyloxy derivatives maximal analgesic potency was found in 14-cinnamoyloxycodeinone. All codeinone derivatives studied had approximately one-third the duration of morphine in mice. Intravenous and subcutaneous toxicities in mice were generally similar in compounds causing death by convulsions, but differed widely in those causing death by respiratory depression.
A simple method for the evaluation of local anaesthetic activity using earthworms
Authors: Block B P , Potts D J , Finney R S H 
Published: April 2011

Abstract
Earthworms are immersed in local anaesthetic solution and tested for anaesthesia at 1 min intervals by dipping their tails into weak acid. The time of onset of anaesthesia is used as a measure of anaesthetic activity. The method is simple, inexpensive and has an end-point which is unmistakable.
Some observations on the effect of lubrication on the crushing strength of tablets
Authors: Shotton E , Lewis C J 
Published: April 2011

Abstract
The effect of mean compaction pressure, base particle size, lubricant particle size, and lubricant concentration, on crushing strength of tablets has been determined for crystalline aspirin, hexamine, sucrose and sodium chloride, and simple granulations of sucrose and of hexamine. Magnesium stearate powder was used as a lubricant. The lubricant decreased the strength of all tablets, the reduction being greatest for the crystalline materials. Variation of lubricant particle size had no effect on strength, and the behaviour of the granulations was not predictable from the characteristics of the crystalline materials. The results are compared with those of other workers.
The assay of nux vomica and its preparations
Authors: Perry H M , Sheppard M L 
Published: April 2011

Abstract
A method is proposed for the extraction of strychnine and brucine, from nux vomica and some of its preparations. An ammoniacal suspension of the drug is extracted with chloroform in a downward displacement liquid-liquid extractor. The strychnine and brucine are then extracted from the chloroform with normal sulphuric acid and the strychnine determined spectrophotometrically. In general the results are in good agreement with those obtained by official methods and the method effects a considerable saving of time.
Preparation and biological activity of some complexes of trypanocidal phenanthridinium compounds
Authors: Groves M J , Wilmshurst E C 
Published: April 2011

Abstract
The preparation and in vivo testing is described of complexes of some phenanthridinium trypanocides with polysaccharides and polymeric materials possessing strong anionic groups. The laminarin sulphate complex of Prothidium bromide [2-amino-7-(2-amino-6-methyl-4-pyrimidylamino)-9-p-aminophenylphenanthridium 10,1′-dimethobromide] shows enhanced prophylactic activity in mice challenged with Trypanosoma congolense (F.N.). When tested in cattle in East Africa the complex produced less local reaction at the site of injection but prophylactic activity was similar to that obtained with the equivalent dose of Prothidium bromide itself. Possible reasons for these results are discussed.
Reproducibility of extinctions measured on the slopes of absorption curves
Authors: Ismail M , Glenn A L 
Published: April 2011

Abstract
Errors in setting the wavelength scale of an ultra-violet spectrophotometer cause an increase in the variance of extinctions measured on the slope of an absorption curve. For a given instrument and operator, the coefficient of variation of extinctions measured on a steep slope was ten times the normal value for zero slope. A method is described for obtaining reasonably precise estimates of (E/), where “S” refers to the displacement of the wavelength scale. The coefficient of variation bears a linear relationship to (E), which is relevant to the choice of wavelengths for Vierordt’s method.
Alkaloids of the leaves of Rauwolfia vomitoria Afz.
Authors: Patel M B , Poisson J , Pousset J L , Rowson J M 
Published: April 2011

Abstract
Leaves of Rauwolfia vomitoria, collected in Nigeria, contained at least six alkaloids, three are indole derivatives (aricine, tetrahydroalstonine, isoreserpiline) and three are isomers of α-oxindole type (carapanaubine, rauvoxine, rauvoxinine). Rauvoxine and rauvoxinine are new alkaloids. The leaves contained no reserpine.
Effect of adrenalectomy on cotton pellet granuloma formation in the rat
Authors: Ashford A , Penn G B 
Published: April 2011

Abstract
The development of granulomas over 3 days was inhibited in adrenalectomised rats when cotton pellets were implanted on the day of adrenalectomy and was potentiated when the pellets were implanted 7 days after adrenalectomy. The initial inhibitory effect of adrenalectomy was not observed when the granulomas were allowed to remain in situ for 7 days instead of 3 days and was completely reversed by treatment with corticosterone.
Cytological aspects of the mode of action of chlorhexidine diacetate
Authors: Hugo W B , Longworth A R 
Published: April 2011

Abstract
Electron microscopic examination of ultra-thin sections of Escherichia coli cells treated with various concentrations of chlorhexidine diacetate reveal two effects. In low drug concentrations many cells lose electron dense material leaving behind empty shells, in higher concentrations the appearance of the cytoplasm is significantly affected. These results are discussed in the light of biochemical findings under identical conditions.
The role of the nervous system in local inflammatory responses
Authors: Fearn H J , Karady S , West G B 
Published: April 2011

Abstract
Inflammation produced in rats by three means has been investigated. The response produced by the external application of xylol seemed to be the result of stimulation of the axon reflex in the area of skin where the substance was applied; it was prevented by chronic denervation of the sensory nerves. The inflammatory response produced by dextran involved the release of 5-hydroxytryptamine; it was prevented by the prior treatment with specific antagonists. The inflammatory response produced by heat treatment did not involve the axon reflex and appeared to be the result of another mechanism, probably involving bradykinin.
The significance of an isoprenaline-like metabolite in the interpretation of the responses of blood vessels in skeletal muscle to adrenaline
Authors: Roberts D J 
Published: April 2011

Abstract
A depressor substance, which resembled isoprenaline in Rf value, was demonstrated after chromatography of plasma collected from chloralose-anaesthetised cats during the blood pressure responses to intravenous injections of adrenaline, but the results obtained did not substantiate the hypothesis of a functional metabolite. The amount of vasodilatation that the “metabolite” would have caused in the skeletal muscles of the hind limb could not, for example, be correlated with the increases in blood flow produced by the original intravenous doses of adrenaline. The fact that adrenaline was largely vasoconstrictor in acutely denervated hind limbs was taken to indicate that the original vasodilator effects were of reflex nervous origin. It is suggested that the afferent source of this and related reflexes involves the stimulation of chemoreceptors as opposed to mechanoreceptors and that increases in flow through denervated muscles in response to adrenaline are caused by a direct action on the walls of the blood vessels.
Macusine B: Further pharmacology
Authors: Leonard B E 
Published: April 2011

Abstract
Macusine B reduced the induction time and potentiated the barbiturate sleeping time of mice, possibly as a consequence of the hypothermia produced by the alkaloid. There was no evidence to suggest that macusine B affects the synthesis or metabolism of noradrenaline, dopamine, 5-hydroxytryptamine or γ-aminobutyric acid in the rat brain, nor was there any evidence to suggest that it affected the binding of noradrenaline and 5-hydroxytryptamine within the brain. There is an indication that macusine B may act on central adrenergic receptors. The slight depression of the behavioural activity which occurs in rats and mice after the injection of macusine B was probably due to the hypothermia induced by the alkaloid.
On sympathetic regulation of carbohydrate metabolism in the liver
Authors: Vizi E S , Pogátsa G , Káldor A 
Published: April 2011

Abstract
Glycogenolysis in the liver produced by isoprenaline was inhibited by β-receptor blocking agents using the perfusion technique. Dichloroisoprenaline also inhibited spontaneous glucose release, as did α-receptor stimulation by noradrenaline.
Histamine gastric ulceration in the guinea-pig. Some observations on a new method
Authors: Anderson W , Soman P D 
Published: April 2011

Abstract
Consistent gastric ulceration can be produced in suitable strains of guinea-pig, after high duodenal ligation under pentobarbitone anaesthesia, by the subcutaneous injection of a relatively low dose of aqueous histamine acid phosphate. The ulceration coincides with a dose of histamine which produces sub-maximal secretion volume and which is greater than that producing the maximum secretion. The method does not require antihistamine cover, and it is shown that antihistamines may complicate the true histamine response by the stomach. The results provide evidence that this type of ulceration follows the action of gastric juice on a functionally impaired mucosa.
Radiation-protection of Serratia marcescens by a thiolsulphonate related to cysteamine
Authors: Owen T C , Parker M S , Stern G M 
Published: April 2011

Abstract
A thiolsulphonate, 2-aminoethyl 2-aminoethanethiolsulphonate (also known as cystamine disulphoxide) affords significant protection to the micro-organism Serratia marcescens against the lethal effects of X-rays. The thiolsulphonate breaks down extensively at pH7, but the degree of protection given by it is much greater than can be accounted for by the action of decomposition products and is considered to be characteristic of the compound itself.