bluuebunny/crossref_metadata_2025 huggingface dataset:
The Effects of Two Phenylacetic Acid Derivatives on the Analgesic Action of Morphine in Mice
Authors: Medaković M , Banić B
Published: April 2011

After intracerebral injection in mice, the analgesic effect of morphine depended on the dose. Two phenylacetic acid esters, CFT 1201 (diethylaminoethylphenyldiallyl acetate) and CFT 1208 (diethylaminoethylphenylallyl acetate), injected intraperitoneally, potentiated the analgesic action of 0·5 μg. of morphine, injected into the posterior portion of the brain 90 min. later. When the phenyl acetates were injected (50 μg.) into the brain, they potentiated the analgesic action of morphine, injected subcutaneously (10 mg./kg.) 80 min. later. The results show that the inhibitors of the hepatic microsomal enzymes may affect the action of analgesics by an action on the central nervous system.
A Note on the Toxicity and Solvent Properties of Dimethyl Sulphoxide
Authors: Brown V K , Robinson J , Stevenson D E
Published: April 2011

Dimethyl sulphoxide has good solvent properties for a wide range of chemicals, and a low toxicity to mammals. The acute oral LD50 for rats is about 20ml./kg. and for chickens about 12·5 ml./kg. Rats tolerate up to 10 daily doses of 10 ml./kg. weight. Dimethyl sulphoxide is therefore a useful solvent for chemical compounds under toxicological evaluation.
Phosphatidylethanolamine and Lysophosphatidylethanolamine
Authors: Robins D C
Published: April 2011

Phosphatidylethanolamine and Lysophosphatidylethanolamine belong to a group of phospholipids generally termed cephalins. The phospholipids are universally distributed among living organisms and are thought to be essential components of cell membranes. From the quantities of lipoidal and protein material found in cell membranes (Danielli and Stein, 1956) together with surface tension and related studies (Danielli and Harvey, 1935; Danielli and Davson, 1935), the membranes are considered to consist of a bimolecular leaflet of lipids with a unimolecular layer of protein adsorbed onto the polar surface.

The course of investigation of the cephalin fraction has not been reviewed in recent years, and here is discussed the general scope of the work in this field, under the headings of preparation, structure, synthesis and physical properties.
On the Stability of Adrenaline in Injections: A Comparison of Chemical and Bioassay Methods
Authors: Backe-Hansen K , Aarnes E Drottning , Venneröd A M , Jensen K Briseid
Published: April 2011

The stability of adrenaline in some injections has been investigated by chemical assays based on determinations of adrenochrome and of adrenolutine, while the rat blood pressure method and the rat uterus inhibition method served as biological control procedures. The colorimetric method, in which adrenaline is oxidised to adrenochrome by means of potassium ferricyanide in acid solution, proved unable to detect any deterioration of adrenaline in procaine and adrenaline injections. The corresponding fluorimetric method, in which the adrenochrome formed is rearranged to adrenolutine by addition of strong alkali, gave results which agreed well with the biological results. In injections, adjusted to pH 3 with hydrochloric acid, adrenaline was stable for at least 20 months at 4° in solutions heated at 120° for 20 min., at 100° for 20 min. or unheated. Replacement of the hydrochloric acid by sodium metabisulphite (pH 3·6) prevented the discoloration. In injections of procaine and adrenaline, adjusted to pH 3 with hydrochloric acid, the adrenaline content decreased over the 20 month period, and was most pronounced in the solutions that had been heated before storage. Sodium metabisulphite significantly increased the stability of adrenaline in these injections and also prevented any colour formation.
The Isolation of Hordenine and Norsecurinine from Securinega Virosa (Baill.). The structure of Norsecurinine
Authors: Iketubosin G O , Mathieson D W
Published: April 2011

From the ground roots of Securinega virosa, hordenine and a new alkaloid (norsecurinine) have been isolated. The structure of the latter alkaloid has been elucidated.
An Active Glycoside from Albizia Species and its Action on Isolated Uterus and Ileum
Authors: Lipton A
Published: April 2011

An active oxytocic principle was extracted from Albizia gummifera (Lipton, 1959) by continuous percolation of the dry bark with methanol. Further purification was by dialysis, fractional extraction and precipitation with organic solvents, and by chromatography on alumina. The concentration of activity achieved was 200 times that of the dried bark, measured in vitro on strips of uterus. The active principle is a saponin, giving on hydrolysis an unsaturated triterpene acid (probably C30H48O5), and four sugars, glucose, rhamnose, xylose and arabinose. The principle has a powerful action on isolated uterine tissues from different species, resistant to atropine, antihistamines and brief boiling in aqueous or alcoholic solution, but it fails to excite guinea-pig ileum even in high concentrations. The material, for which the name ‘albitocin’ is proposed, is thought to be potentially valuable in the study of smooth muscle, particularly uterine muscle. The use of these plants by African native doctors, and their possible implication in the high incidence of uterine rupture in Uganda is discussed.
Refractometric Determination of the Critical Micelle Concentration of Non-Ionic Surface-Active Agents
Authors: Donbrow M , Jan Z A
Published: April 2011

The critical micelle concentrations (CMC) values of some non-ionic surfactants have been determined by refraction and are compared with the results reported earlier by other methods. The slope values have been calculated below and above the CMC and an equation developed to predict the slope below the CMC for any member of the homologous series. The values appear to conform with those expected theoretically from atomic refraction data.
Some cyclic hydroxamic acids
Authors: Coutts R T , Noble D , Wibberley D G
Published: April 2011

The preparation of certain quinolines, quinazolines, quinoxalines, benzoxazines and benzothiazines containing the cyclic hydroxamic grouping is described. In vitro antibacterial activities showed that no compound had a broader spectrum of activity than the known 1,2-dihydro-1-hydroxy-2-oxoquinoline.
Analysis of August rat liver for calcium, copper, iron, magnesium, manganese, molybdenum, potassium, sodium and zinc
Authors: Everett J L , Day C L , Bergel F
Published: April 2011

The concentrations of Ca, Cu, Fe, Mg, Mn, Mo, K, Na and Zn in “August” pure line rat livers has been determined by emission spectroscopy, polarography and flame photometry. Differences were shown to exist between normal, regenerating and neoplastic livers, especially in their calcium, iron and manganese contents.
Further pharmacological screening of some West Indian medicinal plants
Authors: Feng P C , Haynes L J , Magnus K E , Plimmer J R
Published: April 2011

Tabulated results are presented for the systematic pharmacological examination of a further 61 Jamaican medicinal plants.
The antibacterial activity of a complex of iodine and a non-ionic surface-active agent
Authors: Hugo W B , Newton J M
Published: April 2011

The antibacterial activity of a complex of iodine and cetomacrogol against Escherichia coli and Staphylococcus aureus has been compared with a system prepared by diluting an iodine solution in ethanol and potassium iodide. Known numbers of bacteria were mixed with known concentrations of iodine and viable counts were made at intervals thereafter. The activity of both preparations was the same at equal iodine concentrations. Killing, when it occurred, was rapid, the relation between the iodine concentration and the dry weight of the bacterial suspension apparently being the controlling feature. The presence of serum reduced the activity, the reduction being greater for Staph. aureus than for E. coli. Temperatures from 20–37° had no effect whilst reducing the pH to 4, or below, caused a marked increase in the activity.
Note on the detection of hexoestrol, stilboestrol, dienoestrol and the p-hydroxy metabolites of phenobarbitone and phenytoin in urine
Authors: Tompsett S L
Published: April 2011

A procedure for the identification of the synthetic oestrogens, p-hydroxypheno-barbitone and 5-(p-hydroxyphenyl) 5-phenylhydantoin in urine by use of two dimensional paper chromatography is described.
Identifying the names and dosage of drugs
Authors: Poulton E C
Published: April 2011

Printing the different doses of a drug (morphine sulphate) larger or in different colours on labels was found to increase the rate at which they could be discriminated from each other by students. Rate of discrimination was measured by the mean time taken both to sort packs of labels, and to search among a matrix of labels. Printing the different doses of an antibiotic preparation (Pro-stabillin-A.S.) in large numerals of different colour made them as quick to discriminate from each other as were different coloured labels. It is believed that changes of this kind in printing could ease the job of finding the required medical preparation, and might reduce the number of instances in which the wrong preparation is given in error.
The stability, staining and corrosive properties of an iodine-non-ionic surface-active agent complex
Authors: Hugo W B , Newton J M
Published: April 2011

The stability of concentrated and dilute solutions of an iodine-cetomacrogol complex and the staining of fabrics and the corrosion of metals it produced, have been compared at the same available iodine concentration, with a system based on weak iodine solution B.P. The available iodine content of the complex decreased on storage, but this loss was associated with the production of an equivalent amount of hydrogen iodide, such that the total iodine content of the system remained constant. The reaction was accelerated by an increase in temperature, but was neither a photochemical nor an oxidative decomposition. The complex was not subject to the large losses of solvent which occurred with the potassium iodide-ethanol system, and in dilute solution was generally more stable; both systems being more stable in acid conditions. Dilute solutions of electrolytes, as found in hard waters, had little effect on the stability of either type of dilute solution except where they caused the pH to rise, but potassium salts produced a characteristic precipitation of the complex, which resulted in a loss of available iodine. The technique of testing the permanency of staining indicated that the complex often produced the less permanent stain, but it was not completely devoid of staining properties. The complex was less corrosive towards certain metals when tested by a static total immersion test, but when the attack was severe as with aluminium and copper, there was little difference between the two iodine systems in their corrosive action.
Note on a micromethod for the estimation of ascaridole
Authors: Wahba S K , Youssef N Z , Amin S W , Girges K N
Published: April 2011

A micro stoichiometric method for the determination of ascaridole in a pure state and in oil of chenopodium is described. The determination is made either by direct or indirect titration of stannous chloride solution. A blank standardisation for the stannous chloride solution should be carried out consecutively.
The action of sympathomimetic amines on circular and longitudinal smooth muscle from the isolated oesophagus of the guinea-pig
Authors: Bailey Diana M
Published: April 2011

The responses to sympathomimetic amines of circular and longitudinal preparations of smooth muscle from the isolated oesophagus of the guinea-pig have been investigated. Evidence is provided for the existence of α-excitatory and β-inhibitory adrenergic receptors in both circular and longitudinal smooth muscle preparations.
Pharmacological properties of isoidide dinitrate
Authors: Halliday J E , Clark S C
Published: April 2011

Isoidide dinitrate is a more active vasodepressor agent in anaesthetised animals than either of its geometric isomers, isosorbide dinitrate and isomannide dinitrate. Isoidide dinitrate also has the greatest vasodilator action of the three isomers on the vascular system of the dog hind leg and is a more potent hypotensive agent than isosorbide dinitrate in hypertensive rats. The greater activity of isoidide dinitrate may be attributable to its higher oil: water partition coefficient or enhanced drug-receptor interaction resulting from the spatial positions of the nitrate groups or both factors. No evidence was found for involvement of adrenergic receptors in responses of vascular or intestinal smooth muscle to isoidide dinitrate.
Absolute configuration and parasympathetic action: Pharmacodynamics of enantiomorphic and diastereoisomeric esters of β-methylcholine
Authors: Ellenbroek B W J , Nivard R J F , Van Rossum J M , Ariéns E J
Published: April 2011

The parasympathomimetic and atropine-like actions of enantiomorphic esters of β-methylcholine and various esters of choline or β-methylcholine containing an asymmetric centre in the acid moiety have been studied. The potent parasympathomimetic drugs have a configuration identical with that of muscarine, suggesting a close affinity with the receptor. There is a gradual change from agonist to antagonist with increasing molecular size of the acid moiety, antagonism beginning with the butyric ester. Optimal affinity as a mimetic in the lower homologues is obtained with the acetic ester. Maximum affinity as an antagonist is obtained with the ester of the bulky hexahydrobenzilic acid. The configuration of the choline part is irrelevant for high atropine-like potency in the compounds derived from β-methylcholine. Clear differences in affinity are found, however, between stereoisomers of potent antagonists containing an asymmetric centre in the acid moiety, provided the asymmetric carbon atom does not bear isosteric groups. It is concluded that the atropine-like agents, although being competitive antagonists of the parasympathomimetics at best cover the agonistic receptor area only partially.
Observations on the pharmacology of halquinol
Authors: KAUL C L , LEWIS J J
Published: April 2011

Halquinol non-specifically depresses tone and motility in isolated intestinal smooth muscle and reduces intestinal motility in intact animals. These properties may be involved in its therapeutic effects.
Interaction between imipramine-like agents and catecholamine-induced hyperthermia
Authors: Jori A , Garattini S
Published: April 2011

Imipramine-like drugs potentiate the hyperthermic response obtained by infusion of noradrenaline, adrenaline and isoprenaline. In addition to this effect, desipramine increases the hyperthermic response induced by L-dopa (in monoamine oxidase blocked rats), reserpine (immediately after intravenous injection) and dexamphetamine. On the contrary, other types of hyperthermia, such as the one induced by phenethylamine in monoamine oxidase treated rats, and that by yeast, were not increased by desipramine. These results are discussed in relation to the mechanism of action of antidepressant drugs.
The viability of spores of some Bacillus species
Authors: Richardson G
Published: April 2011

The percentage of spores of Bacillus subtilis capable of giving rise to macro-colonies (“viability”) has been determined. Under optimum conditions (heat-activation and inclusion of dextrose in the counting medium) about 30% of spores formed colonies. This figure appeared to increase to about 70% on prolonged cold storage (0–10°). The viability of spores decreased with increase in the manganese content of the sporulation medium. Spores of four other species of Bacillus examined were not heat-activatable and were unaffected by the dextrose content of the counting medium. They showed viabilities of 40–75%.
The effects of growth conditions on the yield and quality of essential oil of Mentha piperita
Authors: O’Connor Christopher
Published: April 2011

The results of a factorial experiment designed to study the effects of nitrogen, phosphorus and potassium, alone and in combination, on the yield of green herb, and on the yield and composition of the essential oil of Mentha piperita are reported. The experiment was made on reclaimed peatbog in Ireland. The main conclusion is that there is a significant increase in the yield of essential oil when nitrogen is added in high concentration. This also results in a decrease in the menthol content of the oil. Superphosphate also reduces the percentage menthol content of the oil. Mixtures of all three fertilisers reduce the percentage oil yield.
Comparative assays of some nitrofurans in urine
Authors: Jones B M , Ratcliffe R J M , Stevens S G E
Published: April 2011

Polarographic and microbiological methods for the determination of nitrofurantoin and of N-(5-nitro-2-furfurylideneamino)-2-imidazoline-one (NF 246) in urine are described. In these the limit of detection is 1 μg/ml by the polarographic and 5 μg/ml by a cup plate microbiological technique. No preliminary separation of the drugs is required. The polarographic method is to be preferred, since it is a more sensitive assay and results can be obtained within an hour of receiving the sample.
The analysis of methisazone
Authors: Deavin J C , Mitchell D H
Published: April 2011

The physical and chemical properties of methisazone (1-methylindoline-2,3-dione 3-thiosemicarbazone) are described. Iodimetric titration is suggested as being the most convenient method of assay. Each molecule of methisazone reacts with eight atoms of iodine and the mechanism of this reaction is discussed. Methisazone was examined for impurities by thin-layer chromatography and details are given of the technique employed. Reference is made to the change in light absorption of methisazone solutions when exposed to light.
Adjuvant effect of aluminium monostearate paraffin gels on antitoxin response
Authors: Coles C L J , Heath Kathleen R , Hilton Marjorie L , Lees K A , Muggleton P W , Walton C A
Published: April 2011

Clostridium welchii Type D toxoid has been dispersed in aluminium monostearate-hydrocarbon gels. When these are injected subcutaneously in laboratory animals the antitoxin response is influenced by the method of preparation of the gels. The level and duration of the antitoxin titre in the blood is related directly to the viscosity of the vaccine preparations. Six months after injection, the residual antitoxin titre produced by the most successful treatments was still as good as the peak titre obtained from simple aluminium hydroxide adsorbed vaccine.
A new method for the determination of emulsion stability by dielectric constant measurement: a preliminary report
Authors: Kaye R C , Seager H
Published: April 2011

The creaming of emulsions of liquid paraffin in water stabilised by cetomacrogol 1000 has been studied in a specially designed capacitance cell. Before visual separation of the emulsion is detectable, changes in emulsion composition in the upper part of the cell result in a measurable decrease of dielectric constant. Differences in the creaming rates of a number of emulsions are easily detected and the rate of change of dielectric constant with time is dependent on globule size.
Interaction of aluminium with bacteria isolated from wounds
Authors: Bradley T J , Fish F , Parker M S
Published: April 2011

The effect of aluminium as metal foil and as a weak solution of potassium aluminium sulphate on the growth of Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli and Proteus vulgaris, has been examined over a range of pH values. Aluminium foil, and an aluminium metal film deposited by evaporation on a bonded cellulose fabric, failed to inhibit the growth of the organisms on agar plates. In contact with saline metal foil yielded trace amounts of aluminium in solution but no detectable amounts of aluminium were found in human serum which had been in prolonged contact with aluminium metal. Staph, aureus and Ps. aeruginosa were adsorbed from aqueous suspension by aluminium surfaces. Below pH 5 the growth of these organisms was inhibited by low concentrations of aluminium in aqueous solution. Preliminary measurements of the uptake of aluminium by these sensitive organisms have been made.
The seed haemagglutinins of some Phaseolus vulgaris L. cultivars
Authors: Toms G C , Turner T D
Published: April 2011

The haemagglutinating properties of Phaseolus vulgaris L. vars Canadian Wonder, Masterpiece, Mont D’or, Navy Pea and Red Kidney seed extracts against erythrocytes of the A1A2BO and D(Rho) human blood groups have been investigated. Under some conditions, Navy Pea extract reacted preferentially with erythrocytes possessing the A1 and B antigens, but the remaining extracts showed no blood group selectivity. The agglutination reactions are discussed, and it is suggested that Navy Pea seed contains a non-specific agglutinin and an anti-A1 + B agglutinin.
The temperature coefficient of some bactericides in oil: water dispersions
Authors: Bean H S , Heman-Ackah S M
Published: April 2011

The temperature coefficient of a bactericide in oil: water dispersion changes with the nature of the oil and the phase: volume ratio. The variations in the temperature coefficient are due to temperature effects on the availability of the bactericide in the aqueous phase, and at the oil: water interface of the dispersions. Failures in the preservation of oil:water formulated products encountered during storage in different climates may be due to such underlying phenomena which are not considered in the initial stages of formulation.
The effect of benzoic acid, phenol and hydroxybenzoates on the oxygen uptake and growth of some lipolytic fungi
Authors: RIVERS STELLA M , WALTERS V
Published: April 2011

Oxygen uptake by lipolytic fungi on arachis oil is in the order Aspergillus flavus (brown) > A. niger > Rhizopus arrhizus > Rh. cohnii > A. flavus (green). Respiration is stimulated by low concentrations of benzoic acid, hydroxybenzoates and phenol, but with higher concentrations it is inhibited. Concentrations which give relatively low oxygen uptake are also fungistatic. The factors governing partitioning in oil-water systems are used to calculate the inhibitory concentration of benzoic acid in the aqueous phase.
The in vivo metabolism of isomeric methoxyoxindoles
Authors: BECKETT A H , MORTON D M
Published: April 2011

Isomeric methoxyoxindoles are metabolised by rats, guinea-pigs and rabbits to phenolic metabolites by O-demethylation and hydroxylation. This has been shown by comparison of the physical characteristics of the metabolites with those of standard synthetic hydroxyoxindoles. Negligible O-demethylation of methoxyoxindoles occurs with rat or guinea-pig liver microsome preparations, when compared with those of rabbit, but significant O-demethylation occurs with rat liver slices.
Solubilisation of preservatives: interaction of benzoic acid with short-chain glycol ethers in water and in aqueous polysorbate 80 solution
Authors: DONBROW M , JACOBS JOHN
Published: April 2011

Using a potentiometric titration technique, ethylene glycol mono-ethers (Me, Et, n-Bu, Ph) and diglycol mono-ethers (Me, Et) have been shown to cause elevation of pH in benzoic acid-sodium benzoate solutions. The butyl glycol ether is shown to form micelles; critical micelle concentration values are given and the “loss” of benzoic acid from aqueous solution is considered. In mixtures with polysorbate 80, the glycol ethers increase the uptake of benzoic acid by the micelles.
Rheological investigation of a thixotropic lotion
Authors: WOODMAN M , MARSDEN ANN
Published: April 2011

Various methods of characterising the thixotropic properties of an oil in water lotion are described. Stress relaxation behaviour, which can be expressed over a range of shear rates by a single empirical equation, is shown to be more informative than the measurement of hysteresis loops. Relaxation rate depends upon previous shear treatment which suggests that more than one process occurs during breakdown.
Replenishment by 5-hydroxytryptophan of the amine stores in the central 5-hydroxytryptamine neurons after depletion induced by reserpine or by an inhibitor of monoamine synthesis
Authors: CORRODI H , HÖKFELT K FUXE T
Published: April 2011

A combined biochemical and histochemical analysis of central 5-hydroxytryptamine distribution has produced further evidence to support the theory that 5-hydroxytryptophan is specifically taken up and decarboxylated in 5-hydroxytryptamine neurons of rat brain. After treatment with an inhibitor of monoamine synthesis, α-propyldopacetamide, but not after treatment with reserpine, the intraneuronal 5-hydroxytryptamine stores could be replenished by injected 5-hydroxytryptophan. This appears to indicate that the uptake-storage mechanism of amines in the 5-hydroxytryptamine neurons is intact after α-propyldopacetamide. Pretreatment with a monoamine oxidase inhibitor, nialamide, allowed repletion of the intraneuronal 5-hydroxytryptamine stores by 5-hydroxytryptophan even after treatment with reserpine. This further stresses the importance of monoamine oxidase in regulating the amine levels of the 5-hydroxytryptamine neurons.
Mechanism of the vasoconstrictor action of isoprenaline on an isolated artery preparation
Authors: GAY W S , RAND M J , WILSON J
Published: April 2011

It was not possible to demonstrate a vasodilator action of isoprenaline using the isolated artery segment from the rabbit ear. However, in high doses isoprenaline produced vasoconstriction. This vasoconstrictor response was blocked by α-receptor antagonists but not by β-receptor antagonists, except in high, non-specific doses. The response was not reduced by pretreatment of the rabbits with reserpine or by cocaine. The vasoconstriction produced by isoprenaline in this preparation therefore appears to be due to a direct action on the α-adrenotropic receptors.
The role of the adrenal glands and of α- and β-adrenergic receptors in bronchodilatation of guinea-pig lungs in vivo
Authors: JAMES G W LYNN
Published: April 2011

Adrenaline, aminophylline, isoprenaline, noradrenaline, papaverine and phenylephrine exerted non-specific bronchodilator effects in guinea-pig lungs in vivo. The descending order of bronchodilator potency was isoprenaline > adrenaline > noradrenaline > phenylephrine. These agents also exerted a bronchoconstrictor effect, the descending order of bronchoconstrictor potency being phenylephrine > noradrenaline > adrenaline > isoprenaline. Bronchodilator activity could be antagonized by either α- or β–adrenergic receptor antagonists. The bronchodilator action of aminophylline, papaverine, phenylephrine and noradrenaline was partly mediated via the adrenal gland.
Uptake and storage of catecholamines in rabbit brain after chronic reserpine treatment
Authors: DAHLSTRÖM A , FUXE K , HAMBERGER B , HÖKFELT T
Published: April 2011

The brains of rabbits treated chronically with small doses of reserpine have been examined by the histochemical fluorescence method for dopamine, noradrenaline and 5-hydroxytryptamine. Measurements were made 4 and 24 hr after the last reserpine injection both in vivo and in vitro. Evidence has been obtained that the small functionally-important pool of amine can be directly visualized in the fluorescence microscope. It was found to be present intraneuronally, probably localized to amine storage granules. The degree of functional recovery was correlated with the recovery, as shown by the increased fluorescence, of a small intraneuronal pool of amine and with the ability of amine storage granules to take up monoamines.
Blockade of bradykinin-induced nociception in the rat as a test for analgesic drugs with particular reference to morphine antagonists
Authors: BLANE G F , Macfarlane I R , Reed G
Published: April 2011

A rat test, recently outlined by Deffenu & others for the evaluation of analgesic drugs and using intra-arterially administered bradykinin as the nociceptive stimulus, has been applied to varied categories of analgesic drugs including, for the first time, morphine antagonists. For purposes of comparison, data obtained with the same drugs using established techniques are also given. The use of the bradykinin-antagonism test as a laboratory model with which to investigate drugs of potential therapeutic value in man is discussed and compared particularly with the mouse phenylquinone-induced writhing test. Attention is drawn to the possibility of correlating the effect of drugs on bradykinin-induced pseudo-affective responses in animals with human pain.
The excretion of [14C] butylated hydroxytoluene in the rat
Authors: LADOMERY L G , RYAN A J , WRIGHT S E
Published: April 2011

The excretion of small doses of [14C]labelled butylated hydroxytoluene has been examined in the rat. Parenteral doses are excreted slowly in urine and faeces over 4 days. Biliary excretion is rapid. The biliary radioactivity is absorbed readily from the gut and a rapid enterohepatic cycle has been found to operate over at least 96 hr.
Mechanism of amphetamine accumulation in the isolated perfused heart of the rat
Authors: Thoenen H , Hürlimann A , Haefely W
Published: April 2011

Rat hearts were perfused with 10 to 1,000 ng/ml of (±)-[3H]amphetamine. The time course of accumulation and the maximal tissue/medium ratio (T/M) were identical for all concentrations studied. The maximal T/M varied between 5 and 6 and was reached after 5 min of perfusion. The accumulation of amphetamine was not inhibited by cocaine or noradrenaline. It was not impaired by combined inhibition of aerobic and anaerobic energy metabolism and it was not dependent on the intactness of sympathetic nerve endings, indicating that the greater amount of amphetamine was located extraneuronally. The diminished accumulation of amphetamine following reduction of temperature or sodium concentration of the perfusion fluid most probably reflects impaired tissue perfusion resulting from vascular constriction. The time course of accumulation and decay of amphetamine is compatible with a rapidly reversible phase-distribution of this amine possibly related to its relatively high lipophilic properties. The possible significance of phenolic hydroxyl groups in membrane transport and diffusion of phenethylamines is discussed.
The response of an isolated artery to sympathomimetic amines
Authors: Campbell I K , Farmer J B
Published: April 2011

The rabbit ear central artery preparation responded with contractions to noradrenaline, dopamine, tyramine, octopamine, phenylethylamine, β-phenylethanolamine and periarterial sympathetic nerve stimulation. Noradrenaline, dopamine and nervous stimulation gave monophasic responses. Tyramine and octopamine gave biphasic responses consisting of an initial fast contraction followed by a second contraction of slow onset and long duration. Phenylethylamine and phenylethanolamine also gave biphasic responses, but the second contraction was of quick onset and short duration of action and often merged with the first contraction. Cocaine, superior cervical ganglionectomy and reserpinization reduced the second phase of the contraction to tyramine, octopamine and phenylethylamine. The second phase of the response to phenylethanolamine was reduced by reserpine but not by cocaine or denervation.
The effects of physiological concentrations of noradrenaline on the coronary resistance of isolated perfused hearts of the cat, dog and monkey
Authors: Proctor E
Published: April 2011

The effects of “physiological” concentrations of noradrenaline on the coronary resistance of isolated, perfused hearts of the cat, dog and monkey were determined. At the lowest active concentrations of noradrenaline (2–4 ng/ml), the preparations always responded with an increase in coronary resistance associated with an un-recordable or minimal myocardial response. As the concentration increased, the effect of the amine on the coronary resistance became biphasic. There was an initial transient increase followed by a more prolonged decrease in resistance associated with a significant myocardial response. These results support other evidence that the direct action of noradrenaline on the coronary vessels is one of vasoconstriction, and that the decrease in resistance associated with larger concentrations of noradrenaline is secondary to the myocardial stimulation, perhaps by way of vasodilating metabolites. Lack of agreement of results may well arise due to the use of concentrations of noradrenaline which also affect the myocardium.
A note on the determination of particle size by dielectric measurement
Authors: Kaye R C , Seager H
Published: April 2011

An incremental method for the determination of particle size distribution by dielectric constant measurement is described. The results obtained for griseofulvin and phenothiazine agree well with those obtained by Andreasen's method. The technique is suitable for the size-grading of low-conducting powder suspensions.
A note on the absorption of 3-methoxy-N-methyl-morphinan hydrochloride from the rat stomach
Authors: Fiese G , Perrin J H
Published: April 2011

(+)-3-Methoxy-N-methylmorphinan, a base with a pKa of 7·97 is absorbed from the rat stomach at pH 2·0, in a manner which suggests passive diffusion rather than a specialized transport process to be the mechanism.
Potentiation of ethanol by Coprinus atramentarius in mice
Authors: Genest K , Coldwell B B , Hughes D W
Published: April 2011

Assessment of toxic manifestations and sleeping times in mice shows that the mushroom Coprinus atramentarius potentiates the action of ethanol when administered orally from 3 to 16 hr before a sub-lethal dose of ethanol. Administration of this mushroom 24 hr before, immediately after or 3 hr after the ethanol causes no potentiation. No similar effect was observed with Coprinus comatus.
Peripheral and central components in the hyperthermic effect of desipramine in reserpinized rats
Authors: Bernardi D , Paglialunga S , Jori A
Published: April 2011

Pithed rats show a decrease of body temperature which is not affected by reserpine, cocaine or desipramine. Noradrenaline decreases the rate of fall of body temperature and this effect is enhanced by pretreatment with cocaine or desipramine. Reserpine with desipramine or with cocaine also produces a decreased rate of fall of body temperature. But if reserpine is given 18 hr before pithing, desipramine is without effect although noradrenaline and 2,4-dinitrophenol produce a calorigenic response. The hyperthermic effect of desipramine in reserpinized rats is also decreased by spinal transection. Lumbar transection is less effective than cervical transection. It is concluded that the integrity of the central nervous system is required for the development of the hyperthermic effect of desipramine in previously reserpinized rats.
The effect of ascorbic acid on the cerebral and adrenal catecholamine content in the male rat
Authors: Izquierdo Juan A , Jofré Isabel J , Acevedo Cristina
Published: April 2011

The intraperitoneal administration of ascorbic acid (500 mg/kg) to rats produces a significant decrease in the concentration of dopamine, and an increase in noradrenaline, in the cerebral hemispheres, cerebellum, diencephalon, mesencephalon and medulla oblongata. The only change in the concentration of adrenaline was a decrease observed in the cerebral hemispheres. Ascorbic acid produces an increase in the concentration of ascorbic acid in the brain; this rise was not observed in the adrenal medulla where the concentrations of catecholamines were also unchanged.
Concentric cylinder creep investigation of pharmaceutical semi-solids
Authors: Warburton B , Barry B W
Published: April 2011

The rheological examination of pharmaceutical preparations has not often taken into account the contributions of viscoelasticity. Many semi-solids have been treated as liquids and observed in continuous shear. The present paper describes a concentric cylinder creep apparatus designed to enable viscoelastic parameters to be measured. A resumé of current theory is given and some experimental data analysed.
Subcellular distribution of some phenothiazines in blood platelets of rabbit
Authors: Solatunturi Erkka , Ahtee Liisa
Published: April 2011

Platelets incubated in plasma containing 5 times 10−5 and 3 times 10−4 M chlorpromazine, desmonomethylchlorpromazine or chlorpromazine sulphoxide were homogenized and fractioned by differential centrifugation. After fractionation most of the accumulated chlorpromazine and desmonomethylchlorpromazine were found in the particulate fractions, while most of the chlorpromazine sulphoxide was in the supernatant. The phenothiazines studied had a certain affinity for that fraction containing most of the platelet 5-hydroxytryptamine (5-HT). These phenothiazines released half of the platelet 5-HT without altering its intracellular distribution. The distribution of 5-HT was affected only by concentrations of chlorpromazine and desmonomethylchlorpromazine which released nearly all of the platelet 5-HT.
Aspects of the epimerization of certain tetracycline derivatives
Authors: Hussar Daniel A , Niebergall Paul J , Sugita Edwin T , Doluisio James T
Published: April 2011

The epimerization of several tetracycline derivatives was examined at several pH values using varying conditions of temperature and buffer strength. Rate coefficients for the epimerization of tetracycline and demethylchlortetracycline are reported and factors associated with the epimerization of chlortetracycline and oxytetracycline are discussed. Under the conditions used calcium had no effect on the rate of epimerization and copper promoted degradation other than epimerization.
Hypoglycaemic activity of 1,1‘-biadamantylaryl sulphonylureas
Authors: Pala G , Coppi G , Mantegani A , Bianchi C
Published: April 2011

Replacement of the 1-adamantyl group with a 1,1′-biadamantyl group in the N-adamant-1-yl-N'-arylsulphonylureas leads to compounds having the same or a doubled hypoglycaemic activity. The new biadamantyl derivatives exert a delayed onset of action compared with that of the corresponding adamantane derivatives. The most promising, 3,3′-di(N'-p-toluenesulphonylureido)-1,1′-biadamantyl (Compd No. 1) and 3,3′-di(N'-p-methoxybenzenesulphonylureido)-1,1′-biadamantyl (Compd No. 3) are only slightly toxic and appear not to have other pharmacological activity.
Dissolution and crystal growth in aqueous suspensions of cortisone acetate
Authors: Carless J E , Moustafa M A , Rapson H D C
Published: April 2011

The change in particle size distribution of cortisone acetate in aqueous (saline) suspensions has been examined using the Coulter Counter. Rate of growth under standardized conditions was calculated as increase of diameter per unit time. Solubility of a water-unstable crystal form has been shown to be greater than that of the stable form. Discussion of the results reveals that crystal growth is mainly initiated by polymorphic transformation. Lattice energies, heats of wetting and solution of the different crystal forms are thought to be the rate controlling factors.
Effects of the NN‘-triethyl analogue of suxamethonium on neuromuscular transmission
Authors: Dowd H , Jennings S J , Marshall I G , Tracy B M
Published: April 2011

The effects of succinyltriethylcholine on neuromuscular transmission in the cat and chick, and on the output of acetylcholine from the isolated rat hemidiaphragm, are described. Succinyltriethylcholine exhibits an initial post-junctional non-depolarizing blocking action. A secondary prejunctional inhibitory action on acetylcholine output, is due to succinyltriethylcholine rather than to the hydrolysis products. The compound also exhibits a facilitatory action which may be due to anticholinesterase activity.
The effects of drugs on circular muscle strips from the isolated ileum of the rabbit
Authors: Tweeddale M G
Published: April 2011

Circular muscle strip preparations were contracted by high concentrations of acetylcholine, methacholine or carbachol, but not by other smooth muscle stimulants. The responses to acetylcholine were antagonized by muscarinic blocking agents but not by ganglion-blocking drugs or local anaesthetics. Anticholinesterases induced violent and prolonged activity which was unaffected by repeated washing, by atropine or by local anaesthetics. The insensitivity to acetylcholine and the anomalous responses to anticholinesterases and to the stimulant drugs are discussed. It is suggested that there is some basic difference between the pharmacological responses of the two layers of the mammalian small intestine.
The partially inhibited growth of Escherichia coli in the presence of some antibacterial agents
Authors: Rye R M , Wiseman David
Published: April 2011

Cultures of Escherichia coli were partially inhibited by treatment with tetracycline, phenol, phenylmercuric acetate or cetyltrimethylammonium bromide. The effects of these agents were investigated by measuring the cell size distributions after growth had occurred in the presence of sufficient ampicillin to suppress cellular division. Tetracycline and phenol inhibited cultures by a uniform decrease in the rate of growth of all of the cells; cetyltrimethylammonium bromide completely inhibited the growth of some of the cells whilst having no effect on the remainder; phenylmercuric acetate probably affected all the cells but inhibited each individual to a different extent. The implications of these results are discussed in terms of a general growth rate equation.
The solubilities of the lower testosterone esters
Authors: James K C , Roberts Mrs M
Published: April 2011

The solubilities of the formate to valerate esters of testosterone have been determined in water and several organic solvents. The aqueous solubilities decrease logarithmically as the homologous series is ascended, but the acetate is less soluble than anticipated in the organic solvents. The variation in solubility from ester to ester can be predicted in the organic solvents from thermodynamic data, and is a reflection of the differences in melting point. The melting point differences are explained from the space group dimensions and the area of α to α face contact in the crystals.
A note on insulin tolerance during mebanazine treatment
Authors: Adnitt P I
Published: April 2011

In contrast to previous findings, mebanazine, a hydrazine monoamine oxidase inhibitor, administered for 21 days had no effect on insulin sensitivity in the rabbit. Insulin sensitivity was increased in mebanazine pretreated 24 hr starved rats but unchanged in mebanazine pretreated fed rats. Muscle and liver glycogen in the rat was unaffected by mebanazine treatment.
Water-in-oil solubilized vaccine adjuvants
Authors: Coles C L J , Hepple J R , Hilton Marjorie L , Walton C A
Published: April 2011

The solubilization of water and toxoid solutions in oils by non-ionic surface-active agents has been examined. Water-in-oil solubilized adjuvant formulations of vaccines containing Clostridium welchii type D toxoid as antigen have been tested in laboratory animals. The antitoxin titres in rabbit serum induced by the most successful formulation were as high 14 weeks after a single dose, as the peak titres after two doses of a simple aluminium hydroxide adsorbed vaccine. The vaccines are clear and of low viscosity which facilitates accurate measurement and handling by syringe.
Routine detection and identification in urine of stimulants, analgesics, antihistamines, local anaesthetics and other drugs, some of which may be used to modify performance in sport
Authors: Beckett A H , Moffat A C
Published: April 2011

MANY sporting authorities throughout the world proscribe, in addition to the stimulants, other classes of drugs, e.g. the narcotics and phenothiazine tranquillizers. Present gas-liquid chromatographic procedures for the routine detection in urine of all these classes of drugs suffer from the disadvantage of using a variety of operating conditions (see for example Kazyak & Knoblock, 1963, who listed retention time data for 59 compounds using a single SE-30 column and temperatures from 115–250°, and also Street, 1967).

The work of Beckett, Tucker & Moffat (1967) on stimulants is therefore now extended, using two isothermal GLC systems, to obtain retention data for 74 additional compounds. This allows the analysis of 116 compounds to be made using only three isothermal GLC systems. Drugs, other than those which may be used to modify performance in sport, are included since sportsmen may use them for medical reasons, e.g. phenacetin in analgesic preparations or a local anaesthetic for injury, and these may interfere with the dope control test.
Solubilities of testosterone propionate in non-polar solvents at 100°
Authors: Bowen D B , James K C
Published: April 2011

THE solubilities of the formate to valerate esters of testosterone in non-polar solvents at 25° were determined by James & Roberts (1968) who also compared them with ideal mole fraction solubilities (X2), calculated from the equation,

(Hildebrand & Scott 1962). ΔHF is the heat of fusion of the solute and TM the melting point. Changes in solubility as the homologous series is ascended were predicted by equation (1), but the individual experimental results did not agree with the calculated values. ΔHF was calculated from the heat of fusion at the melting point, ΔHFM, by correcting for the differences in heat capacity of the solid and the supercooled liquid between TM and T. The correction was estimated with a differential scanning calorimeter by extrapolating the liquid enthalpy line back to 25° and measuring the area between the extrapolation and the enthalpy line of the solid. The method was considered questionable, however, because it assumed that the enthalpy line of the supercooled liquid decreased linearly over the whole range of temperature. This theory is tested below by comparing the measured and calculated solubilities of testosterone propionate at a temperature just below its melting point, where the heat capacity correction is small and ΔHFM can be used for ΔHF.

The solvents examined by James & Roberts (1968) had smaller molar volumes than the testosterone esters, and it was suggested that the difference in molar volume between solute and solvent could prevent the random distribution assumed by regular solution theory. Prediction of solubility would thus improve as the molar volume of the solvent approached that of the solute. The test is applied below by determining the solubility of testosterone propionate in a range of solvents.
The effect of pH and sodium metabisulphite on the stability of physostigmine sulphate solutions to heat and ionizing radiation
Authors: Fletcher G , Davies D J G
Published: April 2011

A method which assays the alkaloid in the presence of its breakdown products has been used to investigate the effects of heating and exposure to ionizing radiations on the degradation kinetics of aqueous physostigmine solutions. Maximum stability at 90***° is between pH 2·2 and 3·0. Sodium metabisulphite retards the degradation of physostigmine when exposed to gamma irradiation, but has no effect on the degradation by heat.
Some limitations of continuous shear methods for the study of pharmaceutical semi-solids
Authors: Davis S S , Shotton E , Warburton B
Published: April 2011

The limitations of the Ferranti Shirley viscometer are reviewed and discussed. An experimental study of four pharmaceutical materials indicates that the apparatus is restricted to a qualitative use for semi-solids because of effects due to evaporation, sweep time selection and shear fracture. When the above effects are gross, the rheograms demonstrate obvious peculiarities. If they are slight, they could escape unnoticed physically and yet lead to incorrect interpretation. The rheograms obtained for such materials are not reproducible for a once sheared sample and hence their quantitative interpretation would be meaningless. Transient tests or oscillatory studies are suggested as alternative methods of examination.
Thixotropy and rheopexy of propyliodone suspensions in arachis oil: Effect of median particle size
Authors: Chawla B S
Published: April 2011

Propyliodone oily injection B.P. exhibits thixotropy under high shear rates and rheopexy under low shear rates. The rate and the degree of rheopectic build-up of structure are influenced by the particle size, the effect increasing as the median particle size is reduced.