bluuebunny/crossref_metadata_2025 huggingface dataset:
A Note on the Influence of Chlorpromazine and Diethazine on the Stores of Catecholamine in the Adrenal Glands and Aortic Walls of Rats
Authors: Davis Ruth A , Kaul C L , Lockett Mary F
Published: April 2011

Stores of catecholamines accumulated in the adrenal glands and in the walls of the aortae of rats during treatment with diethazine or chlorpromazine. Diethazine failed to antagonise the release by reserpine of tissue stores of catecholamines and increased tissue sensitivity to the pressor effects of tyramine, probably because release of catecholamines from tissue stores by tyramine is enhanced. Chlorpromazine antagonised the release of adrenal medullary amines by reserpine and delayed the restoration of these stores after depletion.
The Influence of Environmental Changes on the Cardiotoxicity of Isoprenaline in Rats
Authors: Balazs T , Murphy J B , Grice H C
Published: April 2011

The influence of environment on the cardiotoxicity of isoprenaline has been examined in rats. Animals kept for 3 months in individual cages exhibited an increased sensitivity compared to their community caged controls when either mortality or the severity of the heart lesion was considered. Animals exposed to cold for one week showed a 1,000–10,000 times increased sensitivity to isoprenaline compared to their controls. A probable mechanism of sensitisation is discussed.
Potential Reserpine Analogues: Part III Derivatives of 4-ethoxycarbonyloxy-3,5-dimethoxy-benzoic acid, 3-dimethylaminobenzoic acid, p-hydroxybenzanilide and N-(3,4-dimethoxyphenethyl)-3(or 4)-hydroxycyclohexane carboxyamide
Authors: Chodnekar M S , Sharp L K , Linnell W H
Published: April 2011

4-Ethoxycarbonyloxy-3,5-dimethoxybenzanilide (I), 3-dimethylamino-benzanilide (II), N(3,4-dimethoxyphenethyl)-4-ethoxycarbonyloxy- 3,5-dimethoxybenzamide (III), N-(3,4-dimethoxyphenethyl)-3-dimethylaminobenzamide (IV), 4-(3,4,5-trimethoxybenzoyloxy)- benzanilide (V), 4-(4-ethoxycarbonyloxy-3,5-dimethoxybenzoyloxy)- benzanilide (VI), 3-acetoxy-N-(3,4-dimethoxyphenethyl)cyclohexane- carboxyamide (VII), 3-anisoyloxy-N-(3,4-dimethoxyphenethyl)cyclo- hexanecarboxyamide (VIII), N-(3,4-dimethoxyphenethyl)-3-veratroyl- oxycyclohexanecarboxyamide (IX), N-(3,4-dimethoxyphenethyl)-3- trimethoxybenzoyloxycyclohexanecarboxyamide (X), and N-(3,4-dimethoxyphenethyl)-4-trimethoxy benzoyloxycyclohexanecarboxyamide (XI) have been prepared. Eight of the compounds, I-VII and X, were compared with reserpine for their ability to potentiate barbiturate hypnosis in mice and to deplete the 5-hydroxytryptamine content of rat brain. None of them lowered the brain 5-hydroxytryptamine content but several showed barbiturate potentiation. Compound V was the most potent of the series in producing potentiation of barbiturate hypnosis, being about one tenth as action as reserpine.
A Method for the Estimation of Adrenaline and Noradrenaline in Urine
Authors: Atkinson R , Wynne N A
Published: April 2011

A method for the estimation of adrenaline and noradrenaline in urine is described. The catecholamines are adsorbed on aluminium oxide and eluted with acid. The adrenaline and noradrenaline are estimated separately after oxidation with manganese dioxide at different pH values and conversion to the trihydroxyindole derivative for fluorimetric estimation. A mean recovery of 82 per cent (±5 per cent S.D.) was obtained for total amines estimated as noradrenaline, adrenaline recovery was 83 per cent (±6 per cent S.D.) and noradrenaline recovery was 80 per cent (±6 per cent S.D.). The results were in good agreement with biological assay results.
The Bacteriostatic Actions of Tetracycline and Oxytetracycline
Authors: Jones J G , Morrison G A
Published: April 2011

The bacteriostatic actions of tetracycline and oxytetracycline on cultures of A. aerogenes in glucose-mineral salt media have been studied. Both antibiotics show two modes of action, one of which is non-operative under aerobic conditions and is ascribed to an interference with the disposal of hydrogen in unaerated cultures. The other mode of action can be accounted for by an interference with the synthesis of protein. Quantitative measurements of the dependence of the degree of inhibition on the pH and the concentration of magnesium ions are in accord with attributing inhibitory power solely to the non-ionic molecular forms of the antibiotics. The possible contributions of the two modes of action to the cytotoxic action are discussed.
The urinary metabolites of 5-(2-diethylaminoethyl)-3-phenyl-1,2,4-oxadiazole
Authors: Silvestrini B , Catanese B , Corsi G , Ridolfi P
Published: April 2011

The urine of mice, rats, dogs, and men treated with 5-(2-diethylaminoethyl)-3-phenyl-1,2,4-oxadiazole has been examined for metabolic products of the drug. So far, a neutral oxadiazole derivative, which has tentatively been assigned the formula of 3-phenyl-5-hydroxyethyl-1,2,4-oxadiazole, diethylamine and small amounts of unchanged drug have been isolated.
The adsorption of iodine from solution by micro-organisms and by serum
Authors: Hugo W B , Newton J M
Published: April 2011

The uptake of iodine by baker’s yeast, serum, E. coli and Staph. aureus from aqueous dilutions of an iodine non-ionic surface-active agent complex was compared with that from aqueous dilutions of an ethanol and potassium iodide solution. The form of adsorption isotherms depended upon the iodine system and the substrate. A characteristic of all isotherms was the high affinity at low iodine concentrations. Except where high ethanol concentrations remained, uptake was greater from the ethanol: potassium iodide dilutions. The pH of the iodine system also influenced the uptake, the effect varying with the iodine system and the substrate.
The effects of blocking agents upon the isolated vas deferens of the guinea-pig stimulated by the hypogastric nerve
Authors: Morrison A B , Parkes M W
Published: April 2011

When the guinea-pig isolated vas deferens preparation was stimulated by its hypogastric nerve, the responses obtained at different frequencies of stimulation were all reduced proportionately by guanethidine, bretylium, reserpine and pentamethonium. The difference between guanethidine and bretylium in affecting the responses to nervous stimulation at different frequencies of the cat nictitating membrane reported by Boura & Green was not observed with this preparation. Papaverine reduced responses to high frequencies of stimulation more than those to low frequencies. Amphetamine also reduced responses to all frequencies uniformly except in the smallest doses used, which potentiated the responses to high frequencies; these doses reversed the reduction in response by guanethidine, bretylium and reserpine. Preparations stimulated between parallel electrodes responded similarly to those stimulated by the hypogastric nerve.
Antibacterial properties of 5-nitro-2-furylglyoxylidene derivatives
Authors: Buckett W R , Kidd D
Published: April 2011

5-Nitro-2-furylglyoxal has been prepared and nine new derivatives synthesised. These showed similar in vitro antibacterial activity to the corresponding 5-nitro-furfurylidene analogues. The antibacterial activity of the 5-nitro-2-furylglyoxylidenes could not be demonstrated in the serum or urine of rats after oral administration.
Hypoglycaemic agents: variants of tolbutamide
Authors: Hayman D F , Jackman G B , Petrow V , Stephenson O , Wild A M
Published: April 2011

Further new variants of tolbutamide (and two new imidazolines) are described.
The flow properties of magnesia
Authors: Pilpel N
Published: April 2011

A study has been made of the effect of particle size and particle size distribution on the angle of repose of granulated magnesium oxide. Particles smaller than about 100 μ diameter produce a substantial increase in the angle of repose: this has been explained in terms of frictional and van der Waal’s cohesive forces.
Factors influencing the action of glycine on Escherichia coli in nutrient broth and in hypertonic medium
Authors: Russell A D , John R V
Published: April 2011

The effect of various glycine concentrations in nutrient broth and in a hypertonic nutrient medium against E. coli at various temperatures has been examined. Optimum spheroplast formation was found to occur in bacteria which were in the logarithmic growth phase. Glycine has no action on the viability of non-growing bacteria.
Activity of eledoisin, other polypeptides and ergometrine on the uterus in situ of rabbit and other animal species
Authors: Fregnan G B , Glässer A H
Published: April 2011

The oxytocic activity of eledoisin on the uterus in situ of different animal species has been studied and compared with other oxytocic drugs. Eledoisin stimulated the rabbit uterus at doses as low as 0·01-0·1 μg/kg i.v. but had no significant oxytocic action on the uterus of cat, rat, and guinea-pig. It is, however, more active on the vascular than on the non-vascular smooth muscle preparations of the same animal species. The oxytocic activity of oxytocin and ergometrine, on the other hand, has been confirmed on almost all the animal species studied in doses which did not significantly alter the blood pressure (at least in the rabbit).

In the rabbit the oxytocic effect of ergometrine but not that of eledoisin and oxytocin was abolished by the adrenolytic drugs dibenzyline, piperoxan and hydergine. Hypertensin also stimulated almost all the uteri tested, whilst bradykinin was not active in the doses used.
Effects on anaesthetised animals of an oxytocic glycoside extracted from certain species of Albizia
Authors: Lipton A
Published: April 2011

The actions on anaesthetised guinea-pigs, rabbits, cats and monkeys of a glycoside, “albitocin”, obtained from Albizia gummifera, and some other species of Albizia, used by East African witchdoctors to accelerate labour and induce abortion, are described. On intravenous injection there is a transient fall in systemic blook pressure and an increase in uterine activity, with the pregnant uterus exhibiting greater sensitivity. Both responses occur in the presence of atropine and antihistamines, and in monkeys after bilateral vagotomy and hexamethonium, but a prolonged small rise in blood pressure occurs on intraperitoneal injection of the drug. Electrocardiograph records in rabbits and monkeys exhibit no consistent acute or chronic changes in the electrical activity of the heart resulting from the injection of the drug even in lethal doses, almost up to the time of death.
Some effects of altering onium substituents on the internitrogen distance in ganglionic and neuromuscular blocking agents
Authors: Elworthy P H
Published: April 2011

The conductances of butaethonium chloride and bromide, hexaethonium chloride and bromide, and hexadecaethonium iodide have been measured in water at 25°. The limiting equivalent cationic conductances have been interpreted to give a measure of the internitrogen distances, which are larger than in the corresponding methonium compounds, being 5.7–6.7 Å for butaethonium, 6.5–8.7 Å for hexaethonium, and 13.6–14.9 Å for hexadecaethonium. The changes of potency observed on changing the onium substituents are attributed to changes in internitrogen distance and of molecular geometry.
A preparation of the spinal cat by an anterior approach
Authors: Zarro Vincent J , Dipalma Joseph R
Published: April 2011

A method for preparation of the spinal cat through an anterior approach is described. It has certain advantages over the classical posterior approach and is particularly useful in preparations for studying the superior cervical ganglion or nictitating membrane since the entire procedure may be carried out through the same exposure.
Anthelmintic constituents of ferns
Authors: Blakemore R C , Bowden K , Broadbent J L , Drysdale A C
Published: April 2011

Extracts, oils and some individual phloroglucinol compounds prepared from the fern Dryopteris dilatata and Dryopteris filix-mas were tested for taeniacidal activity against the dwarf tapeworm Hymenolepis nana. In D. dilatata activity is concentrated in the phloroglucinol compounds (mainly aspidin, phloropyrone and aspidinol) of which aspidin is the most potent. In D. filix-mas the mixed phloroglucinol compounds (mainly flavaspidic acid and aspidinol) are active, but no more so than the total ether extract. Flavaspidic acid seems to be the most active phloroglucinol constituent of the fern. Desaspidin which occurs in a third fern, Dryopteris austriaca, is more potent than either aspidin or flavaspidic acid. A method of detecting phloroglucinol compounds by thin-layer chromatography is described.
Stability of heparin solutions
Authors: Pritchard J
Published: April 2011

Heparin injection B.P., adjusted to a pH between 7.0 and 8.0, preserved with 0.15% chlorocresol, is a relatively stable biological product and may be expected to retain its potency for up to 15 years if stored at 4°, over 7 years at room temperature and 6–8 years at 37°. The stability is markedly reduced if the pH of the solution falls below 6.0, so that a rapid and marked loss in potency can be expected if heparin is sterilised in, or mixed for any length of time with, solutions of dextrose, owing to the low pH of these solutions.
Urinary excretion kinetics of amphetamine in man
Authors: Beckett A H , Rowland M
Published: April 2011

The urinary excretion of amphetamine has been examined in 11 male subjects after oral administration of (+)- and (–)- amphetamine sulphate. The excretion of unchanged drug was shown to be dependent upon urinary pH. Excretion of amphetamine, when the urine was maintained alkaline or acid, was measured in seven subjects. The implications of these results, especially in the evaluation of dosage forms, are discussed.
Impairment of sympathetic nerve responses by dopa, dopamine and their α-methyl analogues
Authors: Farmer J B
Published: April 2011

Dopa and dopamine reduced the response of the nictitating membrane to postganglionic sympathetic nerve stimulation in cats pretreated with the monoamine oxidase inhibitor pargyline. A similar reduction could be obtained with α-methyldopa and α-methyldopamine in untreated cats. The sensitivity of the membrane to injected noradrenaline, α-methylnoradrenaline or adrenaline was not reduced. The possible mechanism of the anti-hypertensive action of monoamine oxidase inhibitors and α-methyldopa is discussed in the light of these findings.
The anticoagulant activity of carrageenan
Authors: Anderson W , Duncan J G C , Harthill J E
Published: April 2011

λ-Carrageenans and κ-carrageenans from samples of Chondrus crispus, carrageenan from Polyides rotundus and degraded carrageenan from Eucheuma spinosum have anticoagulant activity on intravenous injection in the rabbit. Anticoagulant activity appears to be caused by a general reaction with plasma protein. The undegraded carrageenans are acutely toxic on intravenous injection and form insoluble complexes with fibrinogen in neutral solution. Degraded carrageenan is very much less toxic and, like heparin, forms soluble complexes with fibrinogen. The λ-carrageenans from C. crispus have higher sulphate content, consistently prolong the clotting time more, and are more toxic than the corresponding κ-carrageenans. The differences in sulphate content between the various λ-carrageenans, and between the carrageenans from the other seaweeds tested, do not correspond directly with differences in anticoagulant action and toxicity.
Pharmacological studies on modaline sulphate (W 3207)
Authors: Jori A , Carrara C , Paglialunga S , Garattini S
Published: April 2011

Modaline sulphate (W 3207) has pharmacological effects which probably belong both to the group of monoamine oxidase inhibitors and the imipramine-like drugs. It differs from the monoamine oxidase inhibitors by producing an increase in body temperature in fully reserpinized animals. It differs from imipramine-like drugs in not potentiating the hyperthermic effect of isoprenaline. The effects of modaline are probably related to the formation of a metabolite because they are prevented by the administration of SKF 525 A.
A comparison of the anti-anaphylactic properties of ethanolamine and hydrocortisone
Authors: Goadby P , Smith W G
Published: April 2011

Both ethanolamine and hydrocortisone potentiate the anti-anaphylactic activity of mepyramine in actively sensitised guinea-pigs subjected to anaphylactic shock by exposure to aerosols of antigen solution. The effects of these two substances have now been compared. After intramuscular injection, the peak effect with ethanolamine occurred 1 hr later whereas with hydrocortisone it occurred 18 hr later. Both substances were also effective, after 45 min and 12 hr respectively, as aerosols. The optimum intramuscular dose of ethanolamine was 10 mg/kg and that of hydrocortisone 100 mg/kg. After aerosol administration, optimum effects were observed when 5% solutions of either drug were used.
Synthesis of 1,3,3-trimethyl- and 1,2,3,3-tetramethyl-5-(methyl- and dimethyl-carbamoyloxy) indolines and their methiodides
Authors: Ahmed M , Robinson B
Published: April 2011

The title compounds have been synthesised for testing as anticholinesterases.
Antitrichomonal activity of 1-[(2, 4-dinitropyrryl)-ethyl]-2-methyl-5-nitroimidazole and related compounds
Authors: Brown George W. , Wellerson Ralph , Kupferberg Alfred B
Published: April 2011

A series of 1-substituted dinitropyrroles was tested for trichomonacidal activity. The shorter the substituent the greater was the in vitro activity. No relationship was found between in vivo activity and substituent length. A comparison of the trichomonacidal activities of 1-[(2,4-dinitropyrryl)-ethyl]-2-methyl-5-nitroimidazole (ORF-2245) and 1-(2-hydroxymethyl)-2-methyl-5-nitroimidazole (8823 R.P.) was made. ORF-2245 exhibited activity equal to or greater than 8823 R.P. except in the treatment of established infections where its limited activity was attributed to poor absorption from the gut. Absorption, however, was apparently sufficient to combat or prevent the low-grade infections.
Actions of hemicholinium and triethylcholine on responses of guinea-pig colon to stimulation of autonomic nerves
Authors: Rand M J , Ridehalgh Angela
Published: April 2011

Hemicholinium caused a failure of responses of the guinea-pig colon to stimulation of extrinsic parasympathetic and sympathetic nerves: failure of the parasympathetic responses occurred the more readily. In seven of 20 experiments, hemicholinium did not block the inhibitory response to sympathetic nerve stimulation but the latent period between the start of a train of stimuli and the first sign of relaxation was prolonged after repeated stimulation in the presence of hemicholinium in all 20 experiments. Triethylcholine caused failure of responses of the guinea-pig colon and a reduction of responses of rabbit ileum to sympathetic nerve stimulation. Choline sometimes reversed the blocking action of hemicholinium on responses to parasympathetic and sympathetic nerve stimulation.
Some pyrrolidines and azacycloheptanes related to reversed esters of pethidine
Authors: Casy A F , Birnbaum H , Hall G H , Everitt B J
Published: April 2011

The preparation of some N-substituted 3-phenylpyrrolidin-3-ols and their derivatives is described, and the hot-plate analgesia activities in mice of these compounds and related azacycloheptane derivatives reported. The effect of changes in ring size upon the analgesic activities of 4-phenylpiperidine derivatives is discussed.
Nitroethylenes and related compounds as trichomonacides and candidacides
Authors: Clitheroe Ann , Green D , Jansen A B A , Phillips P C , Rule A W
Published: April 2011

Several of the compounds examined, particularly certain β-nitrostyrenes and di(2- vinyl)benzenes, were highly active in vitro against both Trichomonas vaginalis and Candida albicans, which are commonly found together in vaginitis. The urinary recovery of the compounds after oral administration, however, suggested that the drugs had not gained access to the circulation in amounts sufficient to ensure a worthwhile effect against the organisms and, moreover, they proved irritant to vaginal mucosa.
Note on the estimation of ibufenac in serum
Authors: Adams S S , Cliffe E E
Published: April 2011

A method for the estimation of ibufenac (4-isobutylphenylacetic acid) in serum is described. The acidified serum is extracted with ether and the drug estimated by quantitative paper chromatography.
Cardiovascular and autonomic effects of fenfluramine hydrochloride
Authors: Franko Bernard V , Honkomp Leroy J , Ward John W
Published: April 2011

Fenfluramine hydrochloride (N-ethyl-α-methyl-3-trifluoromethylphenethylamine hydrochloride; AHR-965) administered orally or intravenously to anaesthetised or unanaesthetised dogs, caused a predominant rise in arterial blood pressure, tachycardia, an increase in myocardial contractile force and cardiac output, and an enhanced total peripheral resistance. Fenfluramine was qualitatively like dexamphetamine in its cardiovascular effects; however dexamphetamine was 10 to 20 times more potent as a pressor agent.
Note on derivatives of 2,5-diphenylfuran
Authors: Bavin P M G
Published: April 2011

Aminoalkyl derivatives of 2,5-diphenylfuran have been prepared and shown to be general central nervous system depressants.
An investigation of the pharmacology of macusine B
Authors: Leonard B E
Published: April 2011

Macusine B, an alkaloid isolated from Strychnos toxifera, blocks α-adrenergic receptors and stimulates β-receptors in vivo and in vitro. It partially blocks the response of the isolated rabbit heart and the cat blood pressure to tyramine. Macusine B is a competitive inhibitor of 5-hydroxytryptamine on the guinea-pig ileum and also blocks the action of this spasmogen on the rat uterus.
The compaction of some solid lubricant materials
Authors: Lewis C J , Train D
Published: April 2011

Samples of −100 mesh powders of stearic acid, palmitic acid, sodium stearate, potassium stearate, lithium stearate, calcium stearate, magnesium stearate, zinc stearate, zinc oleate, boric acid and a synthetic wax, were compacted and the die reaction determined using a “moving-die” technique. The shear strength of the compacts measured in a punch penetration test, with the exception of boric acid and zinc stearate, was independent of the compaction pressure above 500 kg/cm2. Solid discs of stearic acid and palmitic acid possessed the same shear strength as the powder compacts; discs of synthetic wax and zinc stearate gave higher values than the corresponding powder compacts. Values of shear strength calculated from measurements of die reaction were higher than values obtained in the shear strength test, but show good agreement with the results calculated by other workers from sliding friction experiments. Shear strength values for compacts of boric acid and discs of synthetic wax, talc crystal, and graphite, indicate that these materials are unlikely to be such good lubricants as stearic acid or its salts.
A note on the absorption and excretion of 14C-labelled thalidomide in pregnant mice
Authors: NICHOLLS P J
Published: April 2011

After oral administration of 14C-labelled thalidomide to pregnant mice, similar concentrations of the drug are found in several maternal tissues and in the placenta and foetus. Thalidomide and one of its hydrolysis products, α-(o-carboxybenzamido)-glutarimide, have been identified in the foetus.
Specific stimulation of gastric acid secretion by a pentapeptide derivative of gastrin
Authors: BARRETT A M
Published: April 2011

The effects of gastrin, a synthetic pentapeptide (N-t-butyloxycarbonyl-β-Ala. Try. Met. Asp. Phe. NH2; I.C.I. 50,123) and histamine on the secretion of gastric acid have been compared in a perfused stomach preparation using anaesthetised rats. The pentapeptide was shown to possess similar secretory activity to that of gastrin but to be 11 times less potent on a molar basis. It produced acid secretions similar to those produced by histamine when compared in several different ways. Unlike histamine, the pentapeptide was without significant effect on blood pressure or haematocrit in maximally stimulating doses.
The effects of polyoxyethylene compounds on the hydrolysis of chlorbutol
Authors: ANDERSON R A , SLADE A H
Published: April 2011

The rates of hydrolysis of chlorbutol are reduced by surface-active agents, but not by polyethylene glycols. The ratio of the rate-constant in simple aqueous systems to that in systems containing surface-active agents can be predicted if the distribution coefficient for chlorbutol between the micellar pseudo-phase and the aqueous phase is known and is independent of concentration.
Effect of metal ions on the lysis of yeast cells by cationic dyes and surfactants
Authors: RIEMERSMA J C
Published: April 2011

Uranyl ions and thorium ions are effective in preventing cytolysis by Toluidine Blue and Azure A because they interfere with dye uptake by the cells. Neither uranyl nor thorium ions prevent the uptake of cetrimide or cetylpyridinium chloride. Cetylpyridinium chloride is capable of releasing previously bound uranyl ions from the cell surface. Anionic groups belonging to lipid constituents of the cell membrane may be involved in the uptake of uranyl and thorium ions as well as in the binding of dye and surfactants cations respectively. Possible cytolytic mechanisms involving polar interactions at the cell surface with lytic cations are discussed.
Decarboxylation and demethylation of some phenolic benzoic acid derivatives by rat caecal contents
Authors: SCHELINE RONALD R
Published: April 2011

Rat caecal contents decarboxylate phenolic benzoic acid derivatives when a free hydroxyl group is in the para position but the presence of substituents adjacent to this group or the carboxyl group reduce or abolish the reaction. Compounds containing a hydroxyl group in the ortho or meta position but lacking one in the para position are not decarboxylated. Some methoxy-derivatives are demethylated. The possible relationship between these findings and urinary phenols is discussed.
A note on the use of the isolated stomach preparation of the Syrian golden hamster
Authors: MIKOŚ E
Published: April 2011

The sensitivity of the isolated stomach strip of the Syrian golden hamster to some neurohormones has been assessed. Acetylcholine (5 × 10−9 g/ml), histamine (10−8 g/ml), bradykinin (10−9 g/ml) and angiotensin (10−9 g/ml) contracted the preparation. The action of bradykinin and angiotensin was probably direct although some results for angiotensin suggested a neurogenic component. The sensitivity of this preparation to angiotensin or bradykinin is only a little less than that of the ascending or descending colon of the rat.
Phase relationships in the simple coacervating system isoelectric gelatin: ethanol: water
Authors: Nixon J R , Khalil Saleh A H , Carless J E
Published: April 2011

The influence of molecular weight on coacervation in the system iso-electric gelatin: ethanol: water has been studied. The minimum concentration of ethanol required to produce coacervation decreased as the molecular weight of the gelatin increased. Analysis of the coacervate phase showed that the ethanol content was approximately constant and independent of both the molecular weight of the gelatin and the total concentration of ethanol in the system.
The “nicotinic” and “muscarinic” receptors of the urinary bladder of the guinea-pig
Authors: Chesher G B , James Barbara
Published: April 2011

The action of acetylcholine and nicotine on the urinary bladder of the guinea-pig has been examined using three techniques of physiological denervation. Nicotine was neurogenic and equiactive concentrations of acetylcholine were myogenic. Whilst acetylcholine has both “muscarinic” and “nicotinic” effects on the guinea-pig bladder, the concentration required to stimulate the nicotinic receptors was approximately 100 times that required for the muscarinic receptors. These results indicate that the nicotinic receptors are confined to nervous tissue, and do not support the suggestion that there might be non-neuronal nicotinic receptors in the bladder musculature of the guinea-pig. The possibility of a non-cholinergic component in the post-ganglionic parasympathetic fibres to the bladder should still be considered.
Spectroscopic examination of the solubilisation of benzoic acid by a non-ionic surfactant
Authors: Donbrow M , RHODES C T
Published: April 2011

Ultraviolet and nuclear magnetic resonance spectroscopy have been used to examine the location of benzoic acid within the cetomacrogol micelle. Evidence has been obtained that the solubilised benzoic acid is probably located at the junction of the hydrocarbon nucleus and oxyethylene palisade layer, supporting the hypothesis advanced earlier on the basis of potentiometric observation.
The flow of granular magnesia
Authors: Jones T M , Pilpel N
Published: April 2011

Investigations of the flow rates of loosely packed magnesia have shown that the general equation developed by Jones & Pilpel (1966)

can be applied to single component and multicomponent mixtures in the size range 0·003 to >0·2 cm. The increase in flow rate caused by mixing coarse and fine particles has been related quantitatively to the size of the particles by the general expression

This can be used to calculate the composition for maximum flow in multicomponent mixtures. The mechanism of action of glidants is discussed in the light of the experimental results and a distinction is made between glidants which improve the flow of granulations and those which improve the flow of cohesive powders.
Water vapour transmission properties of free polymer films
Authors: Banker Gilbert S , Gore Ashok Y , Swarbrick James
Published: April 2011

The water vapour transmission properties of selected hydrophilic, lipophilic, and mixed hydrophilic-lipophilic polymer systems, cast as free films, have been examined as a function of time, film thickness, plasticiser concentration, and film formulation. An inverse linear relationship was established between the logarithm of the water vapour transmission rate (Rwvt) and the logarithm of film thickness in the presence of the various plasticiser concentrations for the three systems studied. The lipophilic n-butyl methacrylate films were found to be less permeable to moisture than either the hydrophilic hydroxypropyl cellulose or mixed methyl hydroxypropyl cellulose-ethyl cellulose films. The butyl methacrylate films closely follow Fickian diffusion, whereas the permeability constants of the other two films increased linearly with film thickness over the range of thicknesses studied. These phenomena are discussed with respect to the relative attractions these films have for water vapour.
The effect of butylated hydroxytoluene, butylated hydroxyanisole and octyl gallate upon liver weight and biphenyl 4-hydroxylase activity in the rat
Authors: CREAVEN P J , DAVIES W H , WILLIAMS R T
Published: April 2011

When a diet containing butylated hydroxytoluene at levels of 0·01 to 0·5% is fed to growing male rats for 12 days, body weight is not affected, but liver weight is increased. The activity of liver microsomal biphenyl 4-hydroxylase is also increased by these concentrations of butylated hydroxytoluene except the lowest level of 0·01% (100 ppm). Butylated hydroxyanisole at 0·1 and 0·25% of the diet did not affect liver weight or the enzyme activity, but at 0·5% it caused some increase in enzyme activity but not in liver weight. At the level of 0·5%, butylated hydroxytoluene given for a single day caused an increase in liver weight which was observed two days later and persisted for three days after which time the liver weight did not differ from controls. Enzyme activity was not significantly altered by 0·5% butylated hydroxytoluene fed during a single day. Octyl gallate fed at 0·5% of the diet for 9 days did not affect liver weight or enzyme activity. High fat diets with or without 0·01% butylated hydroxytoluene fed for 12 days did not increase liver weight, but did increase biphenyl 4-hydroxylase activity.
The effect of 6-azauridine on the contractile responses of the isolated ileum of the guinea-pig to drugs and to coaxial stimulation
Authors: ŜEFERNA I , LOUKOMSKAYA N , KADLEC O , JANKŮ I
Published: April 2011

Small concentrations of 6-azauridine augmented the contractions of the guinea-pig isolated ileum to acetylcholine, nicotine, histamine, barium chloride and to coaxial stimulation. High concentrations partially inhibited all the responses. After prolonged contact with high concentrations of 6-azauridine, the anti-spasmogenic effect persisted long after washing out the compound. The acetylcholine output did not change under these conditions. Comparison of the actions of 6-azauridine with those of papaverine is made and the possible mechanisms of action are discussed.
Anticonvulsant and some neuropharmacological properties of 2-methyl-3-o-tolyl-6-chloro-4(3H)-quinazolone and related compounds
Authors: MEHTA V L , MALHOTRA C L
Published: April 2011

Three 2-methyl-3-o-tolyl-4(3H)-quinazolone derivatives and five 3-p-bromophenyl-4(3H)-quinazolone derivatives were screened for oral anticonvulsant, analgesic and hypothermic properties. The anticonvulsant properties were assessed using a modified maximal electroshock seizure test and the leptazol threshold test. 2-Methyl-3-o-tolyl-6-chloro-4(3H)-quinazolone, being the compound with the greatest anticonvulsant action, was examined in more detail. It is about 1 1/2 times more potent than phenytoin sodium against electroshock induced convulsions, and its potency ratio with phenobarbitone is 1·2 to 1. Against leptazol-induced convulsions, it is 10 times more potent than troxidone. Its sedative-hypnotic properties are much less than those of phenobarbitone sodium and it also has a much weaker potentiating action on phenobarbitone-induced hypnosis. There is no reduction in the spontaneous motor activity of normal and amphetamine-stimulated rats at its ED50 dose level. None of the compounds possesses any analgesic or hypothermic properties.
The dissolution of aspirin and aspirin tablets
Authors: MITCHELL A G , SAVILLE DOROTHY J
Published: April 2011

An attempt has been made to standardize the “beaker” method of measuring in vitro dissolution rates of tablets against published data for aspirin. An unexpected problem arose when it was found that samples of commercial aspirin have different intrinsic dissolution rates. The form of aspirin used in tablet manufacture is likely therefore to be of significance from the viewpoint of in vivo dissolution and drug availability.
A note on some changes in the physical properties of Escherichia coli after heat treatment
Authors: HARRIES DIANN , RUSSELL A D
Published: April 2011

Suspensions of Escherichia coli in water at 50, 55, 60 and 100° showed an increase in extinction and nephelometer readings, the rate of increase depending on the temperature. This is considered to represent varying degrees of alteration in bacterial cytoplasmic protein. No such increases at any temperature occurred with cells held in 0.9% w/v sodium chloride. Lysozyme induced no lysis in cells which had been heated in water or in saline.
A quantitative analysis of the antagonism of intravenous noradrenaline by thymoxamine or phentolamine on the blood pressure of the conscious cat
Authors: BIRMINGHAM A T , AKUBUE P I , SZOLCSÁNYI J
Published: April 2011

The blood pressure of the unanaesthetized cat was recorded from a nylon catheter inserted permanently into the aorta via the right carotid artery and intravenous injections were made into a nylon catheter tied permanently into the right external jugular vein. For noradrenaline there was a linear relation between log dose and blood pressure rise. The α-blocking agents thymoxamine and phentolamine lowered the blood pressure and decreased the pressor response to noradrenaline. Quantitative analysis of the results by three different graphical methods revealed that for the first dose of blocking agent the antagonism was complex but had the characteristics associated with mixed non-competitive and uncompetitive antagonism. For further cumulative doses of blocking agent, the antagonism had the characteristics of competitive antagonism. It is concluded that a first dose of α-blocking agent has an effect on the dynamics of a noradrenaline-induced blood pressure rise in the conscious cat which is complex and could in part be due to the initial effect of the blocking agent in lowering the blood pressure and in part to the activity of the vasomotor compensatory reflexes. After α-blockade has been initiated, the characteristics of the antagonism are, like those in the anaesthetized cat, those of competitive antagonism.
The accumulation of [3H]noradrenaline in the adrenergic nerve fibres of reserpine-treated mice
Authors: CARLSSON A , WALDECK B
Published: April 2011

Mice, pretreated with reserpine, were given [3H]noradrenaline (3H-NA) intravenously and were killed 30 min later. Only small amounts of 3H-NA were recovered from the hearts. The monoamine oxidase inhibitor nialamide in a dose of 10 mg/kg increased the 3H-NA recovered from the hearts of reserpine-treated animals severalfold. In higher doses, however, this effect of nialamide was no longer observed. When 3H-NA was replaced by [3H]α-methylnoradrenaline, nialamide only reduced the amount of amine recovered from the hearts. The balance between the opposing actions of nialamide depended on dosage, time interval and temperature in a manner suggesting that the inhibitory influence was due to accumulation of endogenous amines in the adrenergic nerve fibres. Bretylium and harmaline also preserved 3H-NA in reserpine-treated animals whereas iproniazid, pheniprazine, pargyline and tranylcypromine did not do this. Moreover, pargyline blocked the ability of nialamide to enhance 3H-NA accumulation. The uptake of 3H-NA observed after monoamine oxidase inhibition in the hearts of reserpine-treated mice was almost completely blocked by pretreatment with desipramine or protriptyline, potent blockers of amine uptake by adrenergic nerve fibres.
Infrared studies of hydantoin and its derivatives
Authors: ELLIOTT T H , NATARAJAN P N
Published: April 2011

Infrared absorption spectral characteristics of hydantoin and its akyl, aryl and aralkyl derivatives are reported. The major peaks of comparative significance are discussed in detail.
Impurities in halothane: their identities, concentrations and determination
Authors: CHAPMAN J , HILL R , MUIR J , SUCKLING C W , VINEY D J
Published: April 2011

The following impurities arising during the manufacture of a proprietary halothane have been identified by gas chromatographic, mass spectrometric, nmr and infrared techniques: 2-chloro-, 2,2-dichloro-, 2-bromo-, 2,2-dibromo-, 2,2-dibromo-2-chloro- and 2-bromo-2,2-dichloro-1,1,1-trifluoroethanes, 1,1,2-trichloro-1,2,2-trifluoroethane, 1,2-dichloro-1,1-difluoroethane, 2-bromo-2-chloro-1,1-difluoroethylene, bromodichlorofluoromethane, chloroform, trans-2-bromo-1,1,1,4,4,4-hexafluorobut-2-ene and the trans and cis isomers of 2-chloro- and 2,3-dichloro-1,1,1,4,4,4-hexafluorobut-2-enes. Gas chromatographic methods using chlorinated biphenyl, dinonyl phthalate and polyethylene glycol as liquid phases have been developed for their determination at the ppm level.
Routine detection and identification in urine of stimulants and other drugs, some of which may be used to modify performance in sport
Authors: BECKETT A H , TUCKER G T , MOFFAT A C
Published: April 2011

A general procedure for the analysis in urine of basic drugs (and their metabolites), some of which may be misused as stimulants in sport, has been developed. The techniques used include gas-liquid and thin-layer chromatography and linked gas-liquid chromatography—mass spectroscopy. It is recommended that international control of drug-taking in sport be based primarily upon urine analysis by gas-liquid chromatography systems and also derivative formation followed by gas-liquid chromatography. The principles outlined in the procedure can be applied in a much wider forensic context.
Noradrenaline-phospholipid interactions
Authors: CUTHBERT A W , CALLINGHAM B A , WARREN SYLVIA , PAINTER ELISABETH
Published: April 2011

The uptake of (±)-[3H]noradrenaline from an aqueous phase to an ether phase containing dissolved lecithin has been measured. No differences between the behaviour of (+)- or (—)-noradrenaline in this system could be detected. The biological implications of this finding are discussed.
The configuration of β-eucaine and β-isoeucaine
Authors: PERKS F , RUSSELL P J
Published: April 2011

The configurations of the two isomers, β-eucaine (benzamine hydrochloride B.P.C. 1954) and β-isoeucaine have been deduced. As a result of a study of the nuclear magnetic resonance spectra and of catalytic hydrogenation and oxidation, the α-form has been assigned an equatorial hydroxyl group on C-4 and the β-form an axial hydroxyl group in this position.
Apparatus for studying the disintegration of tablet coatings
Authors: ANDERSON W , SAKR A
Published: April 2011

A new apparatus has been designed to assess rates of disintegration of tablet coatings and the availability of coated tablet contents. Random movement of the coated tablet in a known volume of mildly turbulent disintegrating fluid at a standard temperature is achieved in a perforated Perspex drum made to revolve slowly in the fluid which moves up and down in its container at the same time. The procedure eliminates the tendency for coatings to stick together or to the grid during a test, which is seen with present pharmacopoeial designs and which causes large variability in the results.
A note on a micro and a semimicro method for the assay of ephedrine
Authors: KARAWYA M S , WAHBA S K , KOZMAN A R
Published: April 2011

Two colorimetric methods for the assay of ephedrine are proposed. One is a semi-micro method in which the intensity of red colour produced by the oxidation of ephedrine with hydrogen peroxide is measured. The other is a micro method in which measurement is made of the intensity of the brown colour of the respective copper dithiocarbamate, produced by interaction of ephedrine, carbon disulphide and ammoniacal copper sulphate, the limit of sensitivity being 100 μg. Both methods gave reproducible results when used to assay ephedrine in pharmaceutical preparations. Results were compared with those from the Egyptian pharmacopoeial method.
Inhibitory activity of 8β-carbobenzyloxyaminomethyl-1, 6-dimethyl-10α-ergoline towards stimulant effects by 5-hydroxytryptamine and amphetamine on liver fluke, Fasciola hepatica, in vitro
Authors: Beretta C , Locatelli A
Published: April 2011

The powerful and long lasting anti-5-hydroxytryptamine effects of 8β-carbo-benzyloxyaminomethyl-1–6-dimethyl-10α-ergoline (mce) have been tested on the spontaneous rhythmical activity of Fasciola hepatica, in vitro. The stimulant effects of both 5-ht and amphetamine on this preparation were totally blocked for at least 2 hr by 0·01 μg/ml of mce. One mole of mce counteracts the effects of about 2 × 101 mole of 5-ht or amphetamine. A few other drugs exert inhibitory activity on this preparation but at far higher doses. A comparison between the data obtained for mce and for bromolysergic acid diethylamide (bol) reveals that mce is a more potent inhibitory drug than bol and that, moreover, it is characterized by total lack of depressant or paralysant effects.
Distribution of prostaglandins E1, E2, F1α and F2α, in some animal tissues
Authors: Karim S M M , Hillier K , Devlin Jean
Published: April 2011

A survey of the distribution of prostaglandins E1, E2, F1α and F2α in fourteen tissues from the dog, cat, rat, rabbit, guinea-pig and chicken has been made. One or more of these prostaglandins are present in varying amounts in most tissues with PGE2 PGF2α occurring most commonly.
The effect of emulsifier concentration on the rheological properties of acacia emulsions
Authors: Shotton E , Davis S S
Published: April 2011

The effect of potassium arabate concentration on the rheological properties of liquid paraffin emulsions has been examined over a range of emulsifier concentrations and volume fractions. The emulsions were of small particle size. Aggregation of the emulsions occurred when the volume fraction (ø) was in the region of 0·33–0·43, the exact value of ø depending on the emulsifier concentration. The aggregated emulsions demonstrated irreversible shear thinning and hysteresis loops were obtained. The aggregation only occurred during the emulsification process and was due to a macro-molecular bridging mechanism. The emulsifier concentration influenced aggregation and thereby influenced the rheological properties of the emulsions by two opposing mechanisms. It decreased the volume fraction at which aggregation first occurred (øagg), through its influence on particle size, but increased øagg through its effect on the degree of contraction of the acacia molecule.
A note on the solubility of griseofulvin
Authors: Elworthy P H , Lipscomb F J
Published: April 2011

The solubility of griseofulvin in heptane, water and benzene over the temperature range 15–45° is reported together with the thermodynamic properties for solution of the antibiotic in these solvents.
The solubility of sulphadiazine in water-dimethylformamide mixtures
Authors: Elworthy P H , Worthington H E C
Published: April 2011

Precise measurements of the solubility of sulphadiazine in water, dimethylformamide (DMF), and a range of mixtures of these solvents have been made at 20°, 30°, and 40°. The solubility of sulphadiazine in the mixtures increases with their DMF content. The partial molar heats and entropies of solution decrease with increasing DMF concentration.
A note on the evaluation of results from creep tests using a computer
Authors: Davis S S , Warburton B
Published: April 2011

The accuracy of line spectrum creep analysis depends ultimately on the accuracy with which the steady state compliance of the system with the longest retardation time can be derived. The presented treatment shows how the maximum theoretical value of the creep compliance may be calculated and describes an iterative method for obtaining the correct value using the least sum of squares.
A high content (−)-deguelin concentrate from a commercial derris resin by steady-state distribution
Authors: Brierley E , Smith H J
Published: April 2011

The isolation of a high content (-)-deguelin concentrate from a commercial derris resin using steady-state distribution is described. The separation was followed by noting the change in ratio of extinctions at two wavelengths.
Quantitative method for determining aminofurantoin
Authors: Umar M T , Mitchard M , Gorrod J W
Published: April 2011

A quantitative colorimetric procedure for the estimation of aminofurantoin is described. The red colour of the Schiff base produced by the reaction of dimethylaminobenzaldehyde with aminofurantoin, is stable after a period of 40 min for a further 20 min and can be measured at 582 mμ. Maximal colour is developed at room temperature (20°) under acid conditions (pH 2·0). This technique was found suitable for the determination of aminofurantoin in tissue homogenates. The formation of aminofurantoin as a probable metabolite of nitrofurantoin was investigated but its production was not confirmed.
Metabolic effects induced by the interaction of reserpine with desipramine
Authors: Jori A , Annoni F , Bianchetti A
Published: April 2011

The administration of desipramine to reserpinized rats induces an increase of body temperature without any change in blood glucose and liver or muscle glycogen. Instead there is an increase in the utilization of blood glucose after a glucose load and an increase of blood lactic acid. Plasma and brown adipose tissue free fatty acids are also increased. These findings are discussed in relation to the event linking the central stimulation induced by desipramine with the peripheral metabolic changes associated with the increase of body temperature.
Observations on the efficacy of oral hyoscine N-butyl bromide
Authors: Pennefather Jocelyn N , McCulloch Marian W , Rand M J
Published: April 2011

Hyoscine N-butyl bromide (Buscopan) antagonized the spasmogenic action of acetylcholine on guinea-pig isolated ileum, having a pA2 of 7·8. The drug also had intestinal antispasmodic activity in the anaesthetized cat after either parenteral or enteral administration. With the enterally administered drug larger doses were required, but the effects were longer lasting. Enterally administered in conscious dogs the drug sometimes produced a small increase in heart rate.