bluuebunny/crossref_metadata_2025 huggingface dataset:
The Flask Combustion Technique in Pharmaceutical Analysis: Iodine-Containing Substances
Authors: Johnson C A , Vickers C
Published: April 2011

The flask method for combustion of organic samples has been applied to a number of iodine-containing substances of pharmaceutical interest including the non-staining iodine ointments. The method is both rapid and simple and the accuracy and precision of the results obtained show that it is suitable for routine control purposes and possibly for consideration as an official assay procedure.
The Characterisation of Crystalline and Amorphous Aloin
Authors: Lister R E , Pride R R A
Published: April 2011

Tests are described showing the differences between amorphous aloin and that of the B.P. 1953. One of these tests might, with advantage, be incorporated in official publications to differentiate crystalline aloin from the relatively impure and less active amorphous aloin.
Polyhydroxy (Catecholic) Phenolic Acids—the Formation of m-Hydroxy- and Methoxy-Derivatives in Man
Authors: Tompsett S L
Published: April 2011

A method has been described for the determination of the methoxy group in phenolic compounds. Tannic and 3:4-dihydroxybenzoic acids when administered orally to man are excreted in appreciable quantities as 4-hydroxy 3-methoxybenzoic and m-hydroxybenzoic acids.
Chemotherapeutic Properties of Some New Quaternary Ammonium Salts
Authors: Hawking F , Terry R J
Published: April 2011

Several new quaternary ammonium salts have been tested for antifilarial activity against Litomosoides carinii, filarial parasite of the cotton rat. Many of these compounds are active in killing L. carinii; the most promising (BIQ 20) eicosane 1:20-bis(isoquinolinium iodide) and (BAC 20) eicosane 1:20-bis(4-aminocinnolinium iodide) possess an index (LD50 mice/minimum effective dose cotton rats) of 19 and 39 respectively. The compounds have a direct filaricidal action on the adult worms while the microfilariae are comparatively unaffected.
A Note on Glycerol Formal as a Solvent in Toxicity Testing
Authors: Sanderson D M
Published: April 2011

Twenty-nine organic solvents and emulsifying agents, selected for possible use as injection solvents in toxicity testing, have been submitted to a “range-finding” toxicity screening test on rats. As a result, glycerol formal was examined in greater detail. Glycerol formal is a good inert solvent for a wide range of organic chemicals. It produced no toxic effects or macroscopic pathology when 1500 mg./kg. was administered intraperitoneally to rats, or 1000 mg./kg. to mice or guinea pigs, or 4000 mg./kg. orally to rats, and at high doses the only specific effect found was narcosis. It was correspondingly innocuous subcutaneously or dermally, and was almost non-irritant to the eye surface. There was no detectable effect on the toxicity of parathion. Glycerol formal appears to be a useful addition to the range of solvents suitable for use in toxicity tests.
The Stability of Thioglycollate Solutions: Part II. Miscellaneous Factors Associated with the Oxidation and Stability
Authors: Cook A M , Steel K J
Published: April 2011

The rate of oxidation of thioglycollate in aqueous solution increases with increasing pH, but when dextrose is present, neutral solutions are oxidised more rapidly than alkaline solutions. The effect of sodium metabisulphite on the oxidation was indecisive. Boiling thioglycollate solutions evolved hydrogen sulphide. Heating old solutions of thioglycollate caused regeneration of the oxidised material but the extent of this regeneration was less than might have been expected. A yellow colour in some thioglycollate solutions is believed to be due to the action of alkali on the thioglycollic acid. The tetracarboxy acid occurring in samples of the acid was isolated. It is recommended that thioglycollate media be stored in air-tight containers at as low a temperature as possible.
Some Biological Properties of Dimethisterone “Secrosteron” a New Orally Active Progestational Agent
Authors: David A , Fellowes K P , Millson D R
Published: April 2011

Dimethisterone, 6α:21-dimethylethisterone possesses well-marked oral progestational properties with 11.6 times the activity of ethisterone in the Clauberg assay. It has an oral LD50 in mice of 7.65 g./kg., no apparent anabolic, androgenic properties and no significant effect on sodium, potassium or water excretion in saline loaded rats.
Some Physico-Chemical Studies on Salts of Long Chain Dicarboxylic Acids
Authors: Elworthy P H
Published: April 2011

Conductimetric studies on the dipotassium salts of acids of the type HOOC(CH2)nCOOH have been made on sebacic acid (K2, n = 8), dodecanedicarboxylic acid (K2, n = 12), and hexadecane dicarboxylic acid (K2, n = 16). The equivalent conductance-concentration curve for K2, n = 16 showed breaks at 11 and at about 33 mM 1.−1; diffusion studies indicated that the formation of small aggregates occurred at 10 mM 1.−1, the aggregates containing two molecules. The second concentration limit was believed to represent either a change in the electrical properties of the solute, or an increase in the amount of aggregate present. Certain tentative deductions about the length of the molecule in solution were made from the diffusion results.
Microchemical Identification of Some Atropine-Like Drugs
Authors: Clarke E G C
Published: April 2011

Crystal and colour tests are described for 48 atropine-like drugs.
The Antagonism of the Antibacterial Action of Mercury Compounds: Part I. The Antibacterial Activity of Mercuric Chloride
Authors: Cook A M , Steel K J
Published: April 2011

E. coli I was the most resistant of nine organisms tested to the bacteriostatic action of mercuric chloride. Incubation of peptone water or Lemco broth containing high concentrations of mercuric chloride produced a greyish-black sediment. The inclusion of dextrose in the medium increased the amount of mercuric chloride necessary for bacter-iostasis. The bacteriostatic values of the liquid and solid dilution methods differed, and the results of the liquid dilution method could be varied by alteration of the experimental technique. The bacteriostatic activity of mercuric chloride was greater at 37° than at 20°. The presence of culture medium has a protecting action on the organisms. Mercuric chloride prolongs the lag phase of E. coli I but its mechanism has not been investigated.
Comparative Toxicity Studies on Ten Antibiotics in Current Use
Authors: Bacharach A L , Clark Barbara J , Mcculloch Marian , Tomich E G
Published: April 2011

The acute toxicities of ten currently used antibiotics have been compared on two strains of mouse by four different routes.
The Preparation and Pharmacology of Some Phenolic Carbamates and Allophanates
Authors: Barnes J H , Chapman Marguerite V A , McCrea P A , Marshall P G , Walsh Pamela A
Published: April 2011

A series of alkyl-substituted phenyl carbamates has been screened for analgesic activity by two methods and the ED50 of a representative number has been determined by one of them. An attempt has been made to correlate the analgesic activity with chemical constitution and the following points emerge: (i) at least one m-alkyl group is essential for significant activity, (ii) where only one substituent is present, maximal activity occurs when this is ethyl, (iii) two o-substituents abolish the activity, (iv) 2,4,5-trimethylphenyl carbamate (compound 686) possesses the highest activity, (v) the most active compounds are in general also the most toxic, compound 688 being a notable exception, (vi) o-substitution by a group larger than methyl tends to reduce activity, (vii) substitution on the carbamate N, except by hydroxyl, strongly reduces the activity. The toxicity of some of the compounds could not be attributed to their anticholinesterase activity.
The Relation Between Chemical Structure and Uncoupling Activity in Congeners of Salicylate
Authors: Brostoff D V , Moses V , Smith M J H
Published: April 2011

The relation between chemical structure and uncoupling activity in congeners of salicylate has been studied by means of their effects on the oxygen consumption of a suspension of baker's yeast utilising a limited quantity of glucose. Salicylic acid, salicylaldehyde, 2-hydroxyacetophenone, salicylamide, 3-methylsalicylic and 1-hydroxy-2-naphthoic acids were found to show uncoupling activity.
The Formation of Histamine in the Rat
Authors: Telford J M , West G B
Published: April 2011

Factors affecting the determination of histidine decarboxylase activity in adult rat tissues have been studied. The optimal conditions vary from tissue to tissue, and the most potent sources of the enzyme are the pyloric part of the stomach, the liver and the duodenum, with less in the kidney. There is no relationship between the histidine decarboxylase activity of a rat tissue and the amount of histamine it contains.
Polyhydroxy (Catecholic) Phenolic Acids—-Studies of their Metabolism in Man
Authors: Tompsett S L
Published: April 2011

The urinary excretion of glycine and glutamine conjugates has been studied after the oral ingestion of some phenolic acids. The stability of such conjugates and also of the parent substances to various forms of acid hydrolysis has been made. Further observations on the 4-hydroxy-3-methoxy- and m-hydroxyphenolic acids present in human urine have been made.
Notes on the Origin and Significance of the Peroxide Value of Anhydrous Lanolin
Authors: Clark E W , Kitchen G F
Published: April 2011

Wool fat on the fleece has a high peroxide value because of autoxidation, this value falls greatly during washing of the wool and grease-recovery as a result of biological or chemical reduction. It increases again if anhydrous lanolin refined from this grease is bleached by oxidation. Peroxide values are useful as a measure of autoxidation only if values of the surface and lower layers are compared.
A Non-Corrodible Valve for Use in Automatic Control of Flow of Physiological Fluids
Authors: Hemes S A , Roberts J B
Published: April 2011

A valve made from non-corrodible materials, with the method of construction, relevant measurements, order of assembly and final adjustments is described.
The Pharmacognosy of the Root of Rauwolfia Ligustrina Roem. and Schult
Authors: Adderson J E , Evans W C , Trease G E
Published: April 2011

The morphological and anatomical characters of Rauwolfia ligustrina roots are described and compared with those of other Rauwolfia species. The characters of the stem, particularly in so far as they concern its detection when mixed with root, are recorded. Analytical studies on individual plants indicate that reserpine is confined almost entirely to the root-bark, the concentration rapidly decreasing towards the crown and becoming negligible in the stems. Samples of root from different localities may vary greatly in reserpine content.
A New Analeptic: 5,5-Diethyl-1,3-Oxazin-2,4-Dione (Dioxone): I. Toxicity and Convulsant Activity
Authors: Maffii G , Dezulian V M , Silvestrini B
Published: April 2011

Dioxone (5,5-diethyl-1,3-oxaziti-2,4-dione) is a new substance possessing convulsant properties qualitatively similar to leptazol and bemegride. Its convulsant properties have been studied quantitatively in mice and rats. By comparison with the other two analeptics, dioxone shows the highest ratio of lethal to convulsive doses. Dioxone is active orally in mice, rats and dogs. Experiments on spinal cats and rabbits have shown that it does not act on the spinal cord. In the decerebrated animals its effects appear limited and inconsistent. It has a relatively low toxicity, is well tolerated by rats and dogs when administered for up to 6 months either subcutaneously or orally.
The Antitussive Activity of Glycyrrhetinic Acid and its Derivatives
Authors: Anderson Doreen M , Smith W G
Published: April 2011

The antitussive activity of 18β-glycyrrhetinic acid has been investigated using chemical stimulation in the unanaesthetised guinea-pig and electrical stimulation in the lightly anaesthetised cat. Derivatives of glycyrrhetinic acid were active in both types of experiment indicating a central antitussive effect. Several derivatives had approximately the same potency as codeine when given subcutaneously to guinea-pigs; one of these, dicholine glycyrrhetinic acid hydrogen succinate, exhibited the same degree of activity after oral administration
A Note on the Antidiuretic Effect of Small Amounts of Isoprenaline in Rats
Authors: Farmer J B , Lockett Mary F
Published: April 2011

Small subcutaneous amounts of isoprenaline, 0.5–1.0 μg./100 g. weight, caused reduction in the rates of excretion of sodium, potassium and water, both in sham operated and in adrenalectomised rats, and also in unoperated rats in the presence and absence of mannitol diuresis. These effects of isoprenaline were attributed to enhanced reabsorption of sodium and water in the proximal tubules
The Biological Assay of Thyroactive Materials by the Goitre Prevention Technique
Authors: Wiberg G S , Stephenson N R
Published: April 2011

The goitre prevention technique was employed to measure the biological activity of synthetic and natural thyroproteins as well as L-thyroxine and L-triiodothyronine. These studies indicated that L-thyroxine could not be used as a reference standard for natural thyroid preparations since the log dose response lines were not parallel. However, L-thyroxine was a suitable reference standard for the biological assay of the synthetic iodinated proteins
The Oxytocic Activity of Dl-5-Hydroxytryptophan
Authors: Lovašen Ž , Supek Z , Randić M
Published: April 2011

Incubation of the isolated rat uterus with α-methyldopa or bromolysergic acid diethylamide produces a complete inhibition of oxytocic activity of 5-hydroxytryptophan
Antitrichomonal Agents Triazen Derivatives
Authors: Strube R E , Michaels R M
Published: April 2011

Six new triazens have been synthesised. One of these compounds, 3-(2′-diethylaminoethyl)-3-ethyl-1-(p-nitrophenyl)-triazen was active in mice against Trichomonas vaginalis but inactive against Trichomonas foetus
Micelle Formation by Lecithin in Some Aliphatic Alcohols
Authors: Elworthy P H , McIntosh D S
Published: April 2011

Lecithin has been studied in methanol, ethanol, butanol, and hexanol using light scattering and viscosity techniques. A new type of light scattering cell was employed. Micelles were present in all solvents, the micellar weights being 2,300; 7,100; 18,000, and 22,000 in the four alcohols respectively. It appeared that as the polarity of the solvent decreased, the micellar size increased. Dissymmetry measurements showed that no dimension of the micelles exceeded 270Å (λ/20), but high observed depolarisations showed that the particles were anisotropic. Viscosity measurements also gave an idea of the shape of the micelles, giving intercepts of plots of specific viscosity/solute volume fraction against solute volume fraction of 4.29, 4.26, 4.26, and 3.56 for the four alcohols respectively. Using the dimensions of the lecithin molecule, and the number of monomers present in the micelle, calculations of the theoretical viscosity intercept have been made for each solvent, and compared with values obtained experimentally
The Effect of Temperature on the Action of Penicillin on Escherichia Coli
Authors: Hugo W B , Russell A D
Published: April 2011

At least two lethal mechanisms operate when penicillin is allowed to act on growing cultures of E. coli. These effects may be observed by studying penicillin action at 44°
Analgesic Action of Chlorpromazine and Reserpine in Relation to that of Morphine
Authors: Leme J Garcia , Silva M Rocha e
Published: April 2011

An analgesic action of reserpine is reported in mice. This effect, detected by the hot-plate method, is of little, or only of moderate intensity, in the first 2 hr. after injection; maximal intensity is obtained 48–72 hr. after the injection of the drug, and then decreases gradually; after 144 hr. injected animals behave again like controls. The analgesic effect of reserpine seems to differ from that shown by morphine or that shown by chlorpromazine which is quicker in onset and disappears in a few hours. Reserpine potentiates the analgesic action of morphine. This potentiation can be observed 2 hr. after the injection of reserpine. The early potentiating period is followed by a later period of summation of effects. Since a short interval after the injection, reserpine does not exert any analgesic effect, but is able to potentiate morphine analgesia, this action has been regarded as a direct one; the later period of analgesia and summation of effects with morphine has been interpreted as an indirect action of the drug
The Response of the Pig Uterus to Oxytocin at Different Stages in the Oestrus Cycle
Authors: Knifton A
Published: April 2011

Knaus (1926) showed that the uterus of the pregnant rabbit was insensitive to doses of Pituitrin which were sufficient to elicit large contractions in the non-pregnant state. This effect was later shown to be due to the influence of progesterone. But this difference in response between pregnant and non-pregnant uteri did not hold for some other species; thus in the rat and guinea-pig, the uterus responds to posterior pituitary extract (Pituitrin) in the gravid and non-gravid state. The evidence is reviewed by Reynolds (1949).

Adams (1940) tentatively suggested that in the sow, progesterone increases the sensitivity of the myometrium to posterior pituitary extract (Pituitrin). The present investigation was carried out in order to examine further this apparent anomaly.
Local Anaesthetic Activity in Diethylaminoacetyl Derivatives of Substituted Benzylamines
Authors: Collins R F , Large B J
Published: April 2011

Six diethylaminoacetyl derivatives of general formula (III) are more potent than lignocaine as local anaesthetics. All cause erythema or necrosis of guinea-pig skin on intradermal injection except III, R = NH2, R' = H, and R = O(CH2)2Ph. This compound is several times more potent than lignocaine and in equipotent concentrations did not cause any tissue damage to skin on intradermal injection.
The Determination of Calcium in Heavy Magnesium Carbonate using Glyoxal Bis (2-Hydroxyanil)
Authors: Leonard M A
Published: April 2011

The selective and sensitive colour reaction between calcium ions and glyoxal bis (2-hydroxyanil) has been applied to the determination of 0·1 to 0·5 per cent of calcium in heavy magnesium carbonate. The method, which is simple and rapid, gives results which compare well with those by flame photometry.
Studies on Datura Leichhardtii Muell. Ex Benth.
Authors: Evans W C , Stevenson N A
Published: April 2011

The variation in the proportion of hyoscyamine and hyoscine in the aerial parts of Datura leichhardtii has been investigated. From the roots, the alkaloids 7-hydroxy-3, 6-ditigloyloxytropane, 3α-tigloyloxytropane and meteloidine have been isolated.
Sterilisation of Colchicine Injection
Authors: Smith G , Bullivant J M , Cox P H
Published: April 2011

Colchicine solutions for injection can be sterilised by heating at 115° for 30 min., or by heating at 98 to 100° for 30 min. in the presence of phenylmercuric nitrate 0·002 per cent, or by filtration. Solutions in multi-dose containers may be prepared using phenol 0·5 per cent, phenyhnercuric nitrate 0·001 per cent, or benzyl alcohol 1 per cent as bactericide. Sterilised solutions are stable for at least six months if protected from light.
The Instrumentation of a Rotary Tablet Machine
Authors: Shotton E , Deer J J , Ganderton D
Published: April 2011

A rotary tablet machine has been instrumented to measure the forces operating during the compression cycle. A radio link was used to transmit to a recording unit the effect of pressure on strain gauges attached to the punches. Sodium chloride and aspirin were compressed at various pressures and the results compared, using strength and porosity data, with tablets of the same materials prepared on an eccentric machine.
Chemical Studies of the Leaves and Inflorescences of Digitalis Purpurea L. and of Allied Species
Authors: Cowley P S , Rowson J M
Published: April 2011

The total glycoside content and the nature of the individual glycosides in the leaves and inflorescences of Digitalis purpurea, D. lanata, D. lutea, D. thapsi and D. ambigua have been studied. A similarity in the chemical composition of the leaves and inflorescences of each species has been demonstrated. The yield of glycosides from D. purpurea and from D. thapsi would be increased by harvesting the entire aerial parts of the second year plants.
An Experimental Determination of the Inter-Nitrogen Distance in Some Bis-Quaternary Ammonium Ganglionic and Neuromuscular Blocking Agents
Authors: Elworthy P H
Published: April 2011

The conductances in water of hexamethonium bromide and iodide, decamethonium bromide and iodide, hexadecamethonium iodide, and decaethonium iodide have been measured. The values of the limiting cationic conductances have been interpreted in terms of molecular shape, and the internitrogen distance for the above compounds calculated, using hydrodynamic relationships. The internitrogen distances found were 6·3 Å for hexamethonium, 9·5 Å for decamethonium, 13·5 Å for hexadecamethonium, and 10·2–13·5 Å for decaethonium. The effect of the hydrocarbon/water interfacial energy on the extended lengths of these molecules is discussed.
On the Relationship between the Effect of Phenol on the Oxygen Uptake and the Viability of Penicillium Notatum Spores
Authors: Chauhan N M , Rivers Stella M , Walters V
Published: April 2011

0·05 to 0·2 per cent phenol in Horowitz medium progressively reduces the oxygen uptake of Penicillium notatum spores. 0·08 per cent causes fungistasis and fungicidal action is evident at 0·15 per cent and higher concentrations. Exogenous respiration is less sensitive to phenol than spore germination. Measurement of oxygen uptake can not be used for quantitative evaluation of fungicidal action. The concentration exponent for the effect of phenol on oxygen uptake is −1·5.
Synthesis and Pharmacological Properties of Some Derivatives of p-Aminophenylethanolamine
Authors: Teotino U M , Friz L Polo , Steis G , Bella D Della
Published: April 2011

Synthesis of a series of N-alkyl derivatives of 2-amino-1-p-aminophenyl-ethanolamine has been described, and the results of pharmacological screening reported. The antagonistic action exhibited at the adrenergic β-receptors by the p-nitro- and p-amino-N-isopropyl derivatives and the outstanding spasmolytic and bronchodilator activity of 1-p-aminophenyl-2-s-butylaminoethanol have been pointed out.
Pressor Effects of Adrenaline, Noradrenaline and Reflex Vasoconstriction Sensitised by Low Concentrations of Ganglion Blocking Drugs
Authors: Mawji Sultan , Lockett Mary F
Published: April 2011

In cats, rats and pigeons, concentrations of hexamethonium, tetra-ethylammonium and pentolinium ions too low to influence transmission in autonomic ganglia potentiate the pressor effects of adrenaline, noradrenaline and of reflex vasoconstriction. These effects of the ganglion blocking drugs are not modified by spinalization or by acute adrenalectomy but are absent after pretreatment of an animal with reserpine or of a tissue by postganglionic sympathetic denervation. These concentrations of ganglion blocking drug increase the uptake of noradrenaline by the adrenal medulla, increase the total amine and the proportion of it present as adrenaline in this gland, fail to antagonise adrenal medullary depletion of catecholamine by reserpine and can reverse a pre-existing potentiation of the pressor effects of adrenaline and noradrenaline induced by cocaine.
in vitro and in vivo Properties of Aloxiprin: A New Aluminium Derivative of Acetylsalicylic Acid
Authors: Cummings A J , Martin B K , Wiggins L F
Published: April 2011

The rates of solution of aspirin from aloxiprin, an aluminium derivative of acetylsalicyclic acid, in buffer solutions of pH 2–8 were found to be lower than those of aspirin B.P., particularly in the more acid buffers.

The excretion of salicylate in the urine of 11 human subjects who received aloxiprin was more delayed than that from a corresponding dose of aspirin B.P. Little difference was found in the total amount of salicylate excreted in 24 hr.
Substituted Dithiocarbamates and Related Compounds as Trichomonacides
Authors: Michaels R M , Peterson L J , Stahl G L
Published: April 2011

A series of derivatives of dithiocarbamic acid and related compounds have been examined against Trichomonas vaginalis and Trichomonas foetus in vitro and in vivo in the mouse and the rat. The most active compound in vitro, sodium dimethyldithiocarbamate, caused a 90 per cent inhibition of growth of T. vaginalis and T. foetus at 0·07 μg./ml. The in vitro activity of the other compounds ranged from 0·17–1·5 μg./ml. There was no direct correlation of in vitro and in vivo activity. In the assay in mice, sodium 4-morpholinecarbodithioate was the most active compound against T. vaginalis. The CD 50 was 3·9 mg./kg. This compound would not cure rats infected intravaginally with T. vaginalis. In vitro there was an area of non-response in the dose-response curve of T. vaginalis to sodium 4-morpholinecarbodithioate and piperidine 1-piperidinecarbodithioate. When mice were infected with T. vaginalis, the infections were completely susceptible to treatment with low doses of sodium 1- pyrrolidinecarbodithioate and bis(dimethylthiocarbamoyl) sulphide, but not higher doses. Both of these phenomena, in vitro and in vivo, may have been due to differences in the solubility of various metal complexes formed by these compounds.
Studies in the Field of Diuretic Agents
Authors: Jackman G B , Petrow V , Stephenson O , Wild A M
Published: April 2011

New derivatives of 4-chloro-3-sulphamoylbenzoic acid and of 4-chloro-3-sulphamoylaniline are described along with some formally related quinazolones.
A Note on the Metabolism of o-(2-Ethoxyethoxy)-Benzamide to o-(Carbamoyl)Phenoxyacetic Acid in Man
Authors: Cummings A J
Published: April 2011

After the oral administration of o-(2-ethoxyethoxy)benzamide to man, the only metabolic product detected in the urine was o-carbamoylphenoxyacetic acid.
A Specific Method of Assay of Strong Solutions of Benzalkonium Chloride and Other Quaternary Ammonium Germicides
Authors: Brown E R
Published: April 2011

A method of assay of quaternary ammonium germicides in strong solutions or concentrated solid form is described. It can be used for solutions down to about 1 per cent in content. A known excess of iodide is added to the sample solution and the quaternary ammonium iodide is removed by shaking with chloroform. The excess iodide is titrated by an iodate method. When the chloroform extraction is made from a slightly alkaline solution only quaternary ammonium compounds are measured; if it is made from a slightly acid solution, non-quaternary cationic amine impurities are also included. The difference between assay results obtained from acid and alkaline extractions represents the non-quaternary amine content.
Surface-Active Betaines: N-Alkyl-Nn-Dimethylglycines and Their Critical Micelle Concentrations
Authors: Beckett A H , Woodward R J
Published: April 2011

A series of surface-active N-alkyl NN-dimethyl glycines (alkyl betaines) and their hydrochlorides have been prepared. Some physical properties of these compounds have been investigated. The critical micelle concentrations of the betaines have been determined by a surface tension, a refractive index, a dye solubilisation and an iodine method. An explanation of the differences in critical micelle concentrations between these amphoteric surfactants and corresponding anionic and cationic surfactants is proposed.
Phase Equilibria in Some Betaine-Benzaldehyde-Water Systems
Authors: Swarbrick J , Carless J E
Published: April 2011

The phase equilibrium diagrams for six betaine-benzaldehyde-water systems have been determined at 25°, with particular reference to those phases in which future oxidation studies are to be carried out. A progressive increase in the amount of benzaldehyde solubilised in aqueous betaine solutions was found on increasing the betaine chain length from 8 to 11 carbon atoms. Further increase in the betaine chain length from 12 to 16 carbon atoms brought about a progressive decrease in benzaldehyde solubility. These results are discussed in the light of the phases separating at these solubility limits.
The Effects of Guanethidine on the Noradrenaline Content of the Hypothalamus in the Cat and Rat
Authors: Dagirmanjian R
Published: April 2011

Single injections of guanethidine 15 mg./kg. i.p. did not lower the hypothalamic noradrenaline in cats, but, daily injections of 15 mg./kg. s.c. over a 7 day period consistently produced a decrease in the hypothalamic noradrenaline. Attempts to lower the hypothalamic noradrenaline in rats after single injections or daily injections of guanethidine were unsuccessful.
Some Physico-Chemical Studies of Lysophosphatidylethanolamine Sols
Authors: Robins D C , Thomas I L
Published: April 2011

The solubilities of lysophosphatidylethanolamine in some organic solvents have been determined. Surface tension measurements of aqueous sols showed it to have pronounced surface-active properties. There was a surface ageing effect which was followed by a rise in the surface tension. Possible explanations for these effects are given. The effects of concentration, pH, mono- and divalent salts on the surface activity have been investigated. The critical micelle concentration was in the range 0·001 to 0·002 per cent w/v. The isoelectric point was at pH 3·25. The stability of sols of the phosphatide in the presence of mono- and divalent salts has also been examined.
A Direct Titrimetric Method for the Determination of Some Organic Bases in Pharmaceutical Preparations
Authors: Johnson C A , King R E
Published: April 2011

A rapid titrimetric method using an extractive end-point has been developed for the determination of atropine, codeine, methadone and pethidine in pharmaceutical preparations. Chloroform is added to the organic base dissolved in pH 2·8 buffer solution so that the ratio of chloroform to aqueous phase lies between 2 to 1 and 4 to 1. Titration is carried out with sodium dioctylsulphosuccinate using Dimethyl Yellow screened with Oracet Blue B as indicator; at the end-point the chloroform phase changes colour from green to pink. The method is accurate to ± 1 per cent and has been applied to a number of injection, eye-drop, syrup and tablet preparations. Since little sample-preparation is required, most preparations may be assayed within 10 min., whilst the codeine content of complex compound tablets can be determined in 20 min.
Substituted Dihydroxybenzoic Acids as Possible Anti-Inflammatory Agents
Authors: Lightowler J E , Rylance H J
Published: April 2011

A series of substituted dihydroxybenzoic acids was prepared and examined for anti-inflammatory activity. The compounds which showed activity were derived from γ-resorcylic acid. The introduction of a halogen atom at positions 3 and 5 and a benzyl or methyl group at position 4 gave marked activity but also increased toxicity.
The Relative Potencies of Thyroxine and Liothyronine by Oral and Subcutaneous Administration in the Rat
Authors: Wiberg G S , Devlin W F , Stephenson N R , Carter J R
Published: April 2011

In goitre prevention assays in adult female rats, thyroxine was only one-fifth to one-sixth as active by mouth as by subcutaneous injection whereas liothyronine had about the same biological activity for the two routes of administration. These findings provide an explanation for the fact that thyroxine was one-sixth to one-seventh as active as liothyronine when injected subcutaneously but only one-twentieth to one-thirtieth as potent when the hormones were administered orally. Chemical examination of three commercially available thyroxine samples which were labelled as “chromatographically pure” revealed that one of them contained approximately 10 per cent liothyronine. The presence of this contaminant had a marked influence on the biological responses of the test animals to this preparation.
The Solubility of Iodine in Aqueous Solutions of Non-Ionic Surface-Active Agents
Authors: Hugo W B , Newton J M
Published: April 2011

The solubility of iodine in aqueous solutions of Cetomacrogol 1000 B.P.C., polyethylene glycol 1540 and cetyl and lauryl ethers of polyoxyethylene glycol has been determined. In the region of the critical micelle concentration of cetomacrogol the solubility is below that in water. Well above the CMC, the solubility increases linearly with the concentration of cetomacrogol. Over the temperature range 20–50° the solubility of iodine in aqueous cetomacrogol solution increases with rise of temperature. When a solution is heated and cooled the amount of iodine in the cooled solution is greater than can be obtained by equilibration at that temperature alone. Not all the iodine added to the surface-active agent systems is available for titration with sodium thiosulphate; the unavailable iodine can be accounted for as hydrogen iodide. For 200 g./litre solutions of polyoxyethylene glycol cetyl and lauryl ethers, the available iodine in solution decreases with the number of ethylene oxide units of the ether, but the molecular ratio of iodine to ether increases with the number of ethylene oxide units. The evidence indicates that formation of a complex between iodine and the surface-active agents is in some way involved in the mechanism of the solubilisation process.
The Hydrolysis of Propyl Benzoate in Aqueous Solutions of Cetomacrogol
Authors: Mitchell A G
Published: April 2011

The alkaline hydrolysis of n-propyl benzoate in aqueous cetomacrogol solutions has been investigated. The rate of hydrolysis of solubilised ester in the presence of 100 per cent excess of sodium hydroxide is a first order process in which the rate decreases with increase in cetomacrogol concentration. This indicates that incorporation of ester within the micelles protects it against hydrolysis. The rate of reaction depends on the degree of saturation of the dispersion and not on the actual concentrations of ester or cetomacrogol except in so far as these control the degree of saturation. The degree of saturation is expressed as a “Saturation Ratio” which is the ratio of the ester concentration to its solubility.
Eserine and autonomic nervous control of guinea-pig vas deferens
Authors: Bella D Della , Benelli G , Gandini A
Published: April 2011

In the presence of eserine, the isolated preparation of guinea-pig vas deferens responds to electrical stimulation of the hypogastric nerve with enhanced contractions, which are no longer antagonised by adrenergic blocking agents but are strongly inhibited by atropine. Similarly, in preparations from reserpine-pretreated animals which have become unresponsive to the hypogastric stimulation, eserine elicits full-size responses which are almost completely abolished by atropine and not affected by adrenergic blocking drugs. Direct stimulation with acetylcholine contracts the vas deferens both of normal and reserpinised animals: the responses are antagonised by atropine and enhanced by eserine. It is concluded that there are grounds for inferring that eserine acts not by enhancing an adrenergic mechanism, but by uncovering a parasympathetic cholinergic component in the autonomic nervous control of the preparation.
Effect of various drugs on carrageenin-induced oedema in the rat hind paw
Authors: Niemegeers C J E , Verbruggen F J , Janssen P A J
Published: April 2011

Local oedema in the rat hind paw is induced by subplantar injection of a 1% suspension of carrageenin. An assay procedure for the analysis of inhibitory effects of drugs on this inflammatory process is described. The results obtained with a single oral dose of 14 antirheumatic drugs (3 steroids and 11 non-steroids) and of 49 substances without established clinical antirheumatic value are reported. Only 8 compounds were found to be completely devoid of anti-carrageenin activity. Others were active at dose levels producing striking behavioural, autonomic or toxic effects. All clinically established antirheumatic substances were active in the carrageenin test at non-toxic doses producing no obvious behavioural or autonomic effects and data on dose-response relationship of these compounds are presented. It is concluded that the assay in its present form is an acceptable preliminary screening test for antirheumatic activity.
Effect of phenol on the oxygen uptake of Bacillus subtilis spores
Authors: Loosemore Muriel , Russell A D
Published: April 2011

The effect of phenol on the oxygen uptake of Bacillus subtilis spores in glucose is described. All concentrations of phenol tested inhibited respiration, but a comparison with earlier work showed no correlation between this effect and death of the spores.
Toxicity and tissue distribution studies on the hydrochloride, bismuth iodide complex and a resinate of emetine
Authors: Child K J , Davis B , Dodds M G , Tomich E G
Published: April 2011

The hydrochloride, the bismuth iodide complex and a resinate of emetine have been compared on mice, cats and dogs for toxicity, on cats for emetic activity and on rats for distribution of emetine in the tissues. Emetine hydrochloride, injected sub-cutaneously, was as toxic as emetine hydrochloride or emetine bismuth iodide administered orally, but only one-sixth as emetic. Given orally emetine resinate was considerably less toxic and emetic than the other preparations. The patterns of emetine distribution in the tissues of rats were similar for all the preparations, but the tissue concentrations were much lower with emetine resinate. In infected rats the resinate was as amoebicidal as the hydrochloride or the bismuth iodide complex. It is suggested that emetine resinate might be better than emetine bismuth iodide for the treatment of intestinal amoebiasis.
A note on the electrically transmurally stimulated isolated trachea of the guinea-pig
Authors: Foster R W
Published: April 2011

The isolated trachea of the guinea-pig was stimulated electrically transmurally to give a biphasic response. The initial contraction was abolished by atropine and was rapidly succeeded by relaxation which was blocked by low concentrations of dichloro-isoprenaline. The relaxation was also blocked by procaine, guanethidine, or by previous treatment of the animal with reserpine, but not with hexamethonium. It was concluded that the effects of transmural stimulation were mediated by post-ganglionic adrenergic nerves innervating beta receptors.
The synthesis of some potential antibacterial agents
Authors: Chase B H , Weller W T
Published: April 2011

The preparation of 37 potential antibacterial agents is described. Most of them possess the structure R—X—R’ where R and R’ are substituted phenyl groups and X is a short bridging group; 25 different examples of X have been studied. Minimum inhibitory concentrations against Staphylococcus aureus and against Escherichia coli are recorded.
The identification and determination of lysergic acid diethylamide in narcotic seizures
Authors: Genest K , Farmilo C G
Published: April 2011

Methods are described by which lysergic acid diethylamide (LSD) can be identified and determined in the presence of heroin, other narcotics and controlled drugs. Thin layer chromatography and an Ehrlich’s-reagent spray is applied to the LSD-containing material. For confirmation, thin layer chromatography after ultra-violet irradiation and acid hydrolysis should be carried out where ergot alkaloids are present. Spectrophotofluorometric analysis of LSD can be used in the presence of heroin, other narcotics and controlled drugs with a standard error of ±2%. If ergot alkaloids are present, thin layer separation, elution and subsequent fluorometric analysis are recommended.
Translocation of alkaloids in Datura species
Authors: Evans W C , Griffin W J
Published: April 2011

The ditigloyl esters of the hydroxytropanes, normally found in the roots of Datura spp. occur also in the transpiration stream of D, innoxia and D. cornigera although they do not accumulate in the aerial parts. An alkaloid previously isolated from the leaves or roots of a number of species, and now obtained from the transpiration stream is probably an optical isomer of norhyoscine. Hyoscine is the principal alkaloid of the sap of both the species investigated and noratropine and hyoscyamine are also present.
Note on the in vitro assay of corticotrophin
Authors: Cann M C , Devlin W F , Stephenson N R
Published: April 2011

Factors affecting the precision of the in vitro assay of corticotrophin using quartered adrenals of rats have been examined. Satisfactory results were obtained only by using tissue from healthy adult male Wistar rats which had been kept quiet and at a constant temperature for several days before the assay. Greater precision was obtained from rats first anaesthetised with pentobarbitone and then decapitated. The assay is not considered to be an adequate procedure for checking commercial injections of corticotrophin.
Anticholinesterase activity and charge delocalisation in “aliphatic” and “aromatic” quaternary ammonium compounds
Authors: Thomas J , Staniforth D
Published: April 2011

The anticholinesterase activities of a homologous series of trimethyl(phenylalkyl)-ammonium bromides have been determined and compared with anti-acetylcholinesterase activities previously reported. The pattern of results obtained with the two enzymes differs widely. The surface activities of the compounds at a constant molar concentration was determined in order to investigate the influence of the “distribution effect” on the anticholinesterase activities of the compounds. The anticholinesterase activities of a series of polycyclic aromatic quaternary compounds have also been determined and compared with their previously reported anti-acetylcholinesterase activities. With these compounds, the pattern of results obtained with the two enzymes was similar.
The influence of hydrochloric acid on the chromatographic behaviour of sympathomimetic catecholamines
Authors: Roberts D J
Published: April 2011

The behaviour of three catecholamines on paper chromatograms is shown to be markedly influenced by hydrochloric acid. Double spot formation exhibited by noradrenaline acid tartrate, for example, results from the use of hydrochloric acid in the developing solvent, but the formation of the second spot is prevented when the amine is applied to the paper from solution in dilute hydrochloric acid. Retention of amine at the application area and additional multiple spot phenomena are exhibited by all of the three amines investigated when chromatographed from concentrated hydrochloric acid. The significance of these and related observations is discussed in relation to the use of hydrochloric acid during the separation of catecholamines from biological tissues and fluids.
The effect of some ganglionic stimulants and blocking drugs on acetylcholine release from the mammalian neuromuscular junction
Authors: Beani L , Bianchi Clementina , Bieber G , Ledda F
Published: April 2011

The effect of nicotine, dimethylphenylpiperazinium (DMPP), hexamethonium and pempidine on release of acetylcholine from the guinea-pig phrenic nerve diaphragm preparation has been investigated. Neither nicotine nor DMPP, 2 × 10−5, modified acetylcholine release from the hemidiaphragms at rest or indirectly stimulated at 50/sec: therefore their neuromuscular blocking action has only a postjunctional origin. Hexamethonium, 4 × 10−4, significantly reduced the output of transmitter from preparations stimulated at 50/sec at 38°. It did not affect the release of acetylcholine from hemidiaphragms at rest or the acetylcholine content of the muscle. The presynaptic effect of hexamethonium is probably related to its linkage with “receptors” present on the surface of the nerve endings. Pempidine, 1 × 10−4, diminished the release of acetylcholine from the preparations at rest or stimulated either at 50 or at 6/sec. The effect was related to the frequency and to the temperature. Moreover, the drug reduced the acetylcholine content of the muscle. This effect may be the result of non-specific metabolic inhibition or of an impairment of choline transport system.
Oxidation of benzaldehyde in some single phase betaine-benzaldehyde-water systems
Authors: Swarbrick J , Carless J E
Published: April 2011

The oxidation rates of increasing concentrations of benzaldehyde in ternary systems of the L1 type have been measured in aqueous solutions of four betaine homologues. On applying corrections for extra-micellar material, the rate becomes independent of the betaine concentration and is related to the micellar ratio of benzaldehyde to betaine when this ratio exceeds 1. The rate of oxidation in an LC system has been determined and compared with that in L1 systems. The site and mechanism of the oxidation reaction in these systems is postulated.
Synthesis of aliphatic amino-acid hydrazides as potential tuberculostatic agents
Authors: Edwards D , Hamer D , Stewart W H
Published: April 2011

Some dialkylamino-aliphatic acid hydrazides and bis(hydrazinocarbonyl) compounds have been prepared and tested for antituberculosis activity. None of these compounds was found to possess tuberculostatic activity of the same order as that of isoniazid.
Neuromuscular blocking agents: alkyl and heterocyclic analogues of simple linear trisonium compounds
Authors: Carey Fiona MacLeod , Furst C I , Lewis J J , Stenlake J B
Published: April 2011

A further series of linear hexamethylene-NNN-trisonium compounds has been synthesised and tested for neuromuscular blocking activity. In the alkyl-substituted derivatives, at least one Et is required for significant potency in mammals. Apart from the Et2Bun and EtBu2n compounds, larger alkyl substituents lower potency. High potency in mammals requires at least two Et groups on the terminal nitrogens, if the third group is not Me. Only weak activity was shown by the morpholino-deriatives but the fowl was highly sensitive towards the piperidino- and tetrahydro-papaverino-compounds. The results are discussed.
An investigation of die wall friction during the compaction of powders
Authors: Lewis C J , Train David
Published: April 2011

Crystalline aspirin, hexamine, sucrose, and sodium chloride, and simple granulations of hexamine and of sucrose, have been compressed and the die reaction determined using a “moving-die” technique. The shear strength of the ejected compacts has been measured under zero load conditions, and when compressed to theoretical density, using a punch penetration test. Calculated values of die reaction based on friction theory have been compared with experimental measurements. Correlation between the two is best for aspirin and hexamine crystals when the compact approaches theoretical density and shear strength values for compacts of zero porosity are used in the calculations; for sodium chloride, correlation is best when shear strength values under zero load conditions are used.
Inhibition of rat brain glutamate decarboxylase activity by salicylate in vitro
Authors: Gould B J , Smith M J H
Published: April 2011

Salicylate inhibited rat brain glutamate decarboxylase activity in vitro. The mechanism of the inhibition appeared to involve irreversible combination of the drug with the enzyme protein. Salicylate also decreased the incorporation of radioactivity from l-glutamic acid-14C(U) into γ-aminobutyrate in preparations of rat brain, an effect consistent with an inhibition of glutamate decarboxylase activity by the drug.
Modification of the hypoglycaemic response to tolbutamide and insulin by mebanazine—an inhibitor of monoamine oxidase
Authors: Barrett A M
Published: April 2011

Following reports of clinical changes in the carbohydrate metabolism of diabetic patients receiving mebanazine, possible interactions between mebanazine, adrenaline, tolbutamide and insulin have been studied in rats. Mebanazine had no activity on blood sugar levels and was found to have no effect on the metabolic actions of injected adrenaline. In acute experiments, mebanazine appeared to reduce the net hypoglycaemic action of tolbutamide but had no effect on the response to insulin. In chronic experiments, mebanazine pre-treatment led to a significant potentiation of the hypoglycaemic responses both to tolbutamide and insulin. The possible mechanisms of action and the clinical implications are discussed.