bluuebunny/crossref_metadata_2025 huggingface dataset:
The Effects in Rabbits of Thyroidectomy and Treatment with Triiodothyronine on the Sensitivity to Noradrenaline and the Content of Noradrenaline in Aorta and Spleen
Authors: MacMillan W H , Rand M J
Published: April 2011

The sensitivity of spiral strips of aorta and strips of isolated spleen to sympathomimetic amines and nicotine has been studied in the thyroidectomised rabbit and in rabbits treated with triiodothyronine. Aortic strips from hyperthyroid rabbits were less sensitive to noradrenaline and less able to contract than those from normal rabbits; they also usually failed to respond initially to nicotine or tyramine although the nicotine response could be restored by exposure of the tissues to noradrenaline. Strips from hypothyroid rabbits were slightly less sensitive to low doses of noradrenaline than the normal although their maximal responses to high doses was greater. The dose-response curves for noradrenaline of spleen capsules from hyperthyroid and hypothryoid rabbits were more shallow than the normal. While spleen capsules from both experimental groups responded to nicotine with tachyphylaxis, they failed to respond to tyramine. Exposure of the capsules to noradrenaline temporarily restored the nicotine response. The noradrenaline content of aorta and spleen from hyperthyroid and hypothyroid rabbits was determined and in each case was found to be reduced to about 50 per cent of normal. These observations indicate that not all sympathetically innervated tissues of the hyperthyroid rabbit develop an increased sensitivity to sympathomimetic amines. Changes in tissue noradrenaline levels during periods of altered thyroid activity do not explain the altered sensitivity of the aorta and spleen to noradrenaline.
The Urinary Excretion of Trittated Butylated Hydroxyanisole and Butylated Hydroxytoluene in the Rat
Authors: Golder W S , Ryan A J , Wright S E
Published: April 2011

The total radioactivity of rat urine after the administration of tritiated butylated hydroxyanisole and butylated hydroxytoluene has been measured. The results indicate that approximately 90 per cent of the dose of bha is excreted within four days. With bht, the total radioactivity excreted in the same period is equivalent to only 35 per cent of the dose, but some of the radioactivity of the labelled molecule is lost during metabolism and only an approximate estimation of the total urinary excretion is possible.
The Effect of Adrenergic Blocking Agents and of Chlorpromazine on Blood Pressure Increase by Vasopressin and Angiotensin
Authors: Supek Z , Uroić B , Gjuriš V , Marijan N
Published: April 2011

The influence of the adrenergic blocking agents hydergine, dibenamine and tolazoline and of chlorpromazine on the mean arterial pressure response to vasopressin, angiotensin and barium chloride in anaesthetised dogs was investigated. Adrenergic blocking agents potentiate significantly the pressure response to vasopressin while leaving the responses to angiotensin and barium chloride unaltered. Chloropromazine potentiates the responses to both vasopressin and angiotensin. This potentiation is not due to blood pressure lowering produced by adrenergic blockade or by chlorpromazine.
Alkanolamides Sterically Related to Ergometrine
Authors: Chilton J , Stenlake J B
Published: April 2011

The ethanolamides of 3-dimethylaminopropionic acid, 1-methyl-1,2,5,6-tetrahydronicotinic acid (arecaidine) and 1-methylhexahydronicotinic acid, and propanolamides of 3-dimethylaminopropionic acid and arecaidine have been synthesised. None of these compounds had demonstrable oxytocic activity on the isolated oestrous rat uterus in concentrations up to 1 mg./ml. Arecaidine propanolamide inhibited acetylcholine-induced contractions in concentrations of 0.075 to 0.3 mg./ml. The 2-styryl derivatives of 3-dimethylaminopropionic and 4-dimethylaminobutyric acids were found to be unstable.
Hypoglycaemic Agents. Part II
Authors: Hayman D F , Petrow V , Stephenson O , Thomas A J
Published: April 2011

Various derivatives of 1-benzenesulphonyl-3-butyl(or cyclohexyl)ureas substituted in the aryl nucleus are described.
Flocculation and Conductivity of Phosphatide Sols
Authors: Thomas I L
Published: April 2011

Results obtained in flocculation and conductivity studies with sols of lecithin and lysolecithin and solutions of calcium and potassium chlorides are reported. Calcium chloride interacts with lecithin, the extent of interaction depending upon the method of preparation of the lecithin sol. Potassium chloride does not interact with lecithin. These results may explain why potassium ions can be transported across a cell membrane whilst calcium ions cannot.
The Relationship Between Electrical Resistance and Dispersed Phase Concentration in Oil in Water Emulsions
Authors: Harrison I H , James K C
Published: April 2011

The electrical resistance of a series of oil-in-water emulsions has been measured, and used to test the validity of four equations relating resistance with the concentration of dispersed phase. A modification of one of the equations was found to give the best relationship.
The Antiveratrinic Action of Some Local Anaesthetics
Authors: Sharma V N , Arora R B
Published: April 2011

The activity of fifteen local anaesthetics against the “veratrine response” induced in the frog's sartorius muscle by 0.1 μg./ml. of veratridine was investigated. The suppression of potassium efflux by these agents, and the role played by this ion in the action of veratridine has also been examined.
Pharmacological Screening of Some West Indian Medicinal Plants
Authors: Feng P C , Haynes L J , Magnus K E , Plimmer J R , Sherratt H S A
Published: April 2011

A systematic pharmacological examination has been made of 55 Jamaican plants, most of which have a local reputation as medicinals. A number of interesting, but no outstanding, activities were observed. The results are tabulated.
Simple Hypotensive and Hypertensive Principles from Some West Indian Medicinal Plants
Authors: Durand E , Ellington E V , Feng P C , Haynes L J , Magnus K E , Philip N
Published: April 2011

Examination of those plant extracts which were previously found (Feng and others, 1962) to have transient depressor activity has led to the isolation of γ-aminobutyric acid, from the leaves of Artocarpus incisa L. and of Piper amalago L. and to the demonstration by paper chromatography of its presence in several extracts. Extracts showing pressor activity were also examined and tyramine has been isolated from Phoradendron wattii Kr. and Urb. and dopamine has been shown by paper chromatography to be present in Piper amalago L. and Stachytarpheta jamaicensis Vahl.
The Synthesis of Ortho-Substituted 2-Diethylaminoethyl Benzoates as Potential Local Anaesthetics
Authors: Thomas J , Canty J
Published: April 2011

A series of mono-ortho- and di-ortho- substituted benzoic esters of 2-diethylaminoethanol has been synthesised. Improved methods for the preparation of 2,6-difluorobenzoic acid and 2,6-dimethylbenzoic acid are reported. The preparation of esters of di-ortho- substituted benzoic acids is discussed and an efficient method of esterification of these acids is described.
The Chemical Determination of Liothyronine and Thyroxine in Enzymic Hydrolysates of Pork Thyroid
Authors: Devlin W F , Stephenson N R
Published: April 2011

Maximum amounts of liothyronine and thyroxine were released from pork thyroid by the proteolytic action of erepsin and trypsin after incubation for 96 hr. at 39°. The iodinated thyronines were extracted from the hydrolysate with butanol, separated chromatographically, eluted from the paper and measured quantitatively by a chemical method in which the reduction of ceric ion by arsenious acid is catalysed by the iodine containing compounds. The iodine found in liothyronine and thyroxine accounted for 18 to 25 per cent of the total organic iodine in pork thyroid. It is postulated that pork thyroglobulin contains approximately 1 molar residue of liothyronine and 2 molar residues of thyroxine.
A Note on the Analysis of Oil of Peppermint by an Aluminium Oxide-Silicic Acid Double Column
Authors: Karawya M S , Wahba S K
Published: April 2011

The separation and determination of the constituents of oil of peppermint have been effected using two columns in succession, one consisting of aluminium oxide and the other of silicic acid.
The Phosphorylation of Anti-Adrenergic Quaternary Ammonium Salts Related to Choline
Authors: Copp F C , Jones T S G , McCoubrey A
Published: April 2011

Quaternary ammonium salts related to choline with anti-adrenergic properties have been phosphorylated. The resulting betaines were used to investigate a possible means for improving the oral absorption of quaternary ammonium salts. One of these was converted to the α-glycerophosphate for similar study.
Comparative Study of the Calciphylactic Challenging Potency of Various Iron Compounds
Authors: Strebel Ralph , Vašků Jaromir , Selye Hans
Published: April 2011

Systematic experiments in rats sensitised for calciphylaxis by pre-treatment with dihydrotachysterol were made using fourteen different iron compounds as challengers. It was noted that the selective localisation of soft-tissue calcinosis in various organs depends largely upon the carrier to which the iron atom is attached; hence, under otherwise identical conditions, essentially distinct calciphylactic syndromes can be produced in rats given the same amounts of iron attached to different carriers.
The Effect of the Administration of Water or Isotonic Nacl Solution on the Urinary Excretion of 5-Hydroxyindoleacetic Acid in the Rat
Authors: Bertaccini G , Erspamer V
Published: April 2011

Administration of tap water by stomach tube or of isotonic NaCl solution orally or subcutaneously produces a conspicuous increase in the urinary excretion of 5-hydroxyindoleacetic acid (5-hiaa) in the rat. The same increase can be observed after administration of water plus posterior-pituitary antidiuretic hormone (adh). Tap water is less effective than physiological saline; the latter, in its turn, is more effective by the subcutaneous route than by mouth. Increase of 5-hiaa may be, for short periods, as high as 3 times normal. The minimum oral dose of tap water causing a significant increase in urinary 5-hiaa is 2 ml./100 g., that of physiological saline 1 ml./100 g. Repeated doses of both tap water and physiological saline produce a more intense and long-lasting increase of 5-hiaa output than single doses. Generally, excess 5-hiaa coincides with excess urine elimination, but there is no obligatory correlation of the intensity of the two phenomena. Recovery, as urinary 5-hiaa, of exogenous 5-hiaa, 5-hydroxytryptamine (5-ht) and 5-hydroxytryptophan (5-htp) is the same in control, non-hydrated rats and in rats given single or repeated doses of tap water, tap water plus adh, or isotonic saline solution. The mechanism by which water or saline administration produces increased urinary excretion of 5-hiaa is discussed.
Curare-Like Drugs and Vagal Synapses: Comparative Study in vitro on the Isolated Vagus-Stomach Preparation of the Rat
Authors: Bella D Della , Rognoni F , Teotino U M
Published: April 2011

The anti-acetylcholine properties of curare-like drugs have been investigated on the motor responses of the electrically stimulated isolated vagus-stomach preparation of the rat. The synaptic site of the inhibitory action shown to varying degrees by the compounds tested has been located by comparing the modifications of the gastric responses to stimulation of preganglionic vagal fibres with the unmodified responses of the rat stomach strip preparation to acetylcholine.
The Retention of Aqueous Suspensions on Leaf Surfaces
Authors: Challen S B
Published: April 2011

A method has been devised, using lycopodium, for studying the contribution of leaf surface characteristics to the wetting of leaves and the retention of particles applied as suspensions. Plants have been classified according to wettability, in relation to particle distribution and surface roughness. The recession of liquid on leaves of Rumex obtusifolius was studied in detail and the contributing factors analysed.
Biochemical Properties of Bretylium
Authors: McCoubrey A
Published: April 2011

The effect of bretylium (10−3 m) on the respiration of brain slices and certain enzyme systems has been investigated. This concentration of drug is similar to that present in cat sympathetic ganglia after doses of bretylium sufficient to impair adrenergic nerve function. It was a weak inhibitor of monoamine oxidase, but had no effect on the other enzymes investigated. Prolonged treatment with bretylium (10 mg./kg.) did not affect the catecholamine levels of cat adrenals and sympathetic ganglia; larger doses depleted the amine from the ganglia. The noradrenaline content of rabbit spleen tended to rise after chronic dosage with the drug and this treatment appeared to render the amine refractory to the depleting action of reserpine.
A Note on the use of Cellulose Phosphate Cation-Exchange Paper for the Separation of Catecholamines, and Some Other Biogenic Amines
Authors: Roberts Michael
Published: April 2011

Cellulose phosphate cation-exchange paper has been investigated for its ability to separate biogenic amines. Descending chromatography with an ammonium acetate: isopropanol solvent mixture gave good separation of a number of these amines, including the principal catecholamines. The technique has the advantage of eliminating neutral and acidic compounds which may interfere in conventional partition methods. It has been applied to tissue extracts containing catecholamines.
A New Complexometric Method for the Determination of Some Sulphonamides
Authors: Abdine H , Sayed W S Abdel
Published: April 2011

A complexometric method for the determination of some sulphonamides has been evaluated. The sulphonamides are precipitated as cupric salt, filtered and the excess copper is titrated with edta using pan as indicator.
The Nature of Resistance of A Penicillin to Hydrolysis by Penicillinase
Authors: Citri N , Garber N
Published: April 2011

5-Methyl-3-phenyl-4-isoxazolyl penicillin is a competitive inhibitor of penicillinase. Interaction with this compound causes marked conformational changes in the enzyme. The changes are reflected in increased susceptibility to iodination, urea and heat. Present observations are related to previously recorded evidence, and the conclusion is reached that the side-chain of a penicillin may confer resistance by distorting the catalytic orientation of penicillinase.
The Effect of Lowered Temperature on the Neuromuscular Blocking Action of Suxamethonium on the Rat Diaphragm
Authors: Whittaker R
Published: April 2011

The neuromuscular blocking action of suxamethonium on the rat isolated phrenic nerve diaphragm preparation was observed at 20 and at 37°. The effect of lowered temperature is to intensify the neuromuscular block produced by suxamethonium and to render the depolarisation characteristics of the blockade more distinct. Competitive inhibition is not apparent at 20° in contrast to the competitive features of the block which have been reported to be present at 37°.
New Apparatus: A Simple Mechanical Computer for Relating the Contractile Responses of Tissues
Authors: Paterson G
Published: April 2011

The principle of similar triangles has been applied to make a simple mechanical computer for relating the contractile responses of tissues.
Dioxatrine, a potent and specific rumenal ulcer-preventing agent in rats
Authors: Niemegeers C J E , Janssen P A J
Published: April 2011

When rats are starved with free access to a 20% glucose solution, extensive rumenal ulcers are found in almost all animals at the end of the third week. The formation of these ulcers may be inhibited by dissolving adequate amounts of two anti-acetylcholine agents in the glucose solution. A minimum of about 8 mg/kg of atropine sulphate daily is required for significant activity. Submaximal mydriatic effects are observed after oral administration of this dose. Dioxatrine, a tertiary amine of novel structure, inhibited ulcer formation at dose levels devoid of significant mydriatic activity. Dioxatrine prevents experimental ulcers in rats in one twentieth the dose of atropine.
Some pharmacological aspects of a new water-soluble tetracycline
Authors: Tubaro E , Barletta M , Banci F
Published: April 2011

The pharmacological properties of a new derivative of tetracycline have been described. This water-soluble compound has a low toxicity, is stable, and lacks the local side-effects common to other derivatives of tetracycline.
Chronic toxicity of brilliant blue FCF, blue VRS, and green S in rats
Authors: Mannell W A , Grice H C
Published: April 2011

Groups of twenty rats were given weekly subcutaneous injections of one of the food colours Brilliant Blue FCF, Blue VRS, and Green S. The dose, 20 mg in isotonic saline, was given for 45 weeks after which the rats were observed for an additional 26 weeks. There was ulceration and abscess formation at the site of injection in rats given Blue VRS. The other two colours produced no noticeable local or systemic effects. No subcutaneous fibrosarcomas were seen in any of the rats. Two rats given Blue VRS developed rhabdomyosarcomas in the area of the injection site. This finding is being investigated.
Physical and biological changes in an artificial fat emulsion during storage
Authors: Boberg J , Håkansson I
Published: April 2011

A soybean oil emulsion for parenteral nutrition has been stored for about 2 years at 4, 20 and 40°. During storage, the pH fell and the FFA concentration increased. The Michaelis-Menten constant (Km) and the maximum velocity of the lipoprotein-lipase reaction (Vmax) also increased. Gross particles were formed in the fat emulsion, and its toxicity increased with time. All these changes were most pronounced during storage at 40°.
Some aspects of the mode of action of chlorhexidine
Authors: Hugo W B , Longworth A R
Published: April 2011

Chlorhexidine is rapidly adsorbed by bacterial cells and this adsorption is accompanied by other cytological changes which include changes in the permeability of the cells and in their optical properties. The amount of drug adsorption causing maximum leakage of cell constituents and changes in extinction was found to be equivalent for Escherichia coli and for Staphylococcus aureus. Higher doses of chlorhexidine causing a higher level of drug adsorption caused correspondingly less leakage and change in extinction although such higher doses were more rapidly bactericidal.
Oxidation of benzaldehyde in some multiphase betaine-benzaldehyde-water systems
Authors: Swarbrick J , Carless J E
Published: April 2011

The results of oxidation studies in ternary multiphase betaine-benzaldehyde-water systems show that the maximum rate of oxidation depends primarily on the benzaldehyde content and composition of the phase with the shortest induction period in the system under examination. The effects of chain length and concentration of the S-amphiphile (betaine) are important only in so far as they influence the phase equilibria of the ternary systems.
Effect of an anti-acetylcholine drug, methscopolamine bromide, on ulcer formation and gastric mucus
Authors: Robert André , Nezamis James E
Published: April 2011

A 30-hr period of restraint in rats was followed by the appearance of ulcers in the gastric corpus coincidental with a marked reduction of gastric juice volume, acid and also of hexosamine which was used as an estimation of mucus content. Methscopolamine (Pamine), an anti-acetylcholine drug, prevented ulcer formation, reduced further volume and acid output but produced a 3–4 fold increase in hexosamine concentration. Tissue (corpus and antrum) hexosamine was moderately reduced by restraint. In the corpus, this was counteracted by methscopolamine but antrum hexosamine was not influenced by this drug. The anti-ulcer property of methscopolamine may be due not only to its effect on acid secretion but also to the rise in gastric mucus concentration that it produced.
Spectrophotometric determination of isoniazid in excess p-aminosalicylate
Authors: Dutt M C , Chua T H
Published: April 2011

The presence of a large excess of p-aminosalicylic acid prevents the direct application of Vierordt’s spectrophotometric method to the determination of isoniazid in tablets. The method can, however, be applied after the bulk of the p-aminosalicylic acid has been removed with ether. The extinction of the aqueous phase containing all the isoniazid and some of the p-aminosalicylic acid is then determined at two wavelengths and the concentration of isoniazid calculated therefrom.
Genotropic agents: Steroid basic ethers
Authors: Evans D D , Evans D E , Lewis G S , Palmer P J , Weyell D J
Published: April 2011

The synthesis and biological activity of a series of basic ethers of the steroid oestrogens is described. The compounds have genotropic (Black, 1961) activity coupled with low oestrogenicity.
The relation between heat activation and colony formation for the spores of Bacillus stearothermophilus
Authors: Cook A M , Brown M R W
Published: April 2011

Spores suspended in water were heated at 73·5, 100, 115 and 121° and colony counts made. These showed an initial increase followed by an exponential decline. Spores in phosphate buffer showed a reduced activation. Comparison of total (microscopic) and colony counts showed that only about 5% of unheated spores developed into colonies. This increased to about 50% after optimum heat activation.
Effect of chlorhexidine diacetate on “protoplasts” and spheroplasts of Escherichia coli, protoplasts of Bacillus megaterium and the Gram staining reaction of Staphylococcus aureus
Authors: Hugo W B , Longworth A R
Published: April 2011

Chlorhexidine prevents the transformation of Bacillus megaterium cells to protoplasts by lysozyme, of E. coli cells to spheroplasts by penicillin and causes lysis of “protoplasts” and spheroplasts of E. coli stabilised in hypertonic sucrose solution. Transformation of Staphylococcus aureus cells to the Gram-negative condition occurred in contact with 10 to 800 μg/ml of chlorhexidine and 10, 50 and 100 μg/ml of cetyltrimethylammonium bromide but higher concentrations of the latter prevented this change. Results indicate that chlorhexidine damages the permeability barrier of bacterial cells.
Antifungal activity of some imidazole derivatives
Authors: Ellis G P , Epstein C , Fitzmaurice C , Golberg L , Lord G H
Published: April 2011

A series of 4(5)-arylimidazoles and their N-alkyl and other derivatives has been synthesised. Some of these compounds possessed good in vitro antifungal action, especially against strains of Trichophyton and less activity against Microsporum, Aspergillus and Candida strains; their activity against all mycological pathogens was reduced in the presence of serum. The three most active compounds are 1-alkyl-4-(3,4-dichlorophenyl)imidazoles in which the alkyl group is an n-propyl, n-butyl or isobutyl group. 4(5)-(2,3,4-Trichlorophenyl)imidazole is also almost as potent as an antifungal compound. Structure-antifungal activity relations for these compounds are discussed.
Catechu (Gambier): its microscopical characters
Authors: Leong Mun Sum , Jackson Betty P
Published: April 2011

24 different commercial samples of catechu have been examined microscopically for the presence of vegetable fragments, starch and crystalline material. The components of the vegetable débris have been identified as being derived from the leaves and young shoots of Uncaria gambier Roxb. used in the preparation of the extract. The main microscopical characters of value in the identification of catechu are enumerated.
Influence of adrenaline on the diabetogenic effect of alloxan in the rat
Authors: Abd-El-Wahed H , Ghaleb H A , Hegazy M R
Published: April 2011

The effect of alloxan and adrenaline on blood glucose was investigated in 84 rats. The diabetogenic action of alloxan, 200 mg/kg, was prevented by mixing it for 10 min with adrenaline, 50 μg/kg, before injection. No histological changes in the islets were observed after the injection of this mixture. Similar doses of adrenaline and alloxan, injected intramuscularly at the same time but separately produced a diabetogenic action greater than that produced by alloxan alone.
A note on the stability of actinomycin D
Authors: Crevar George E , Slotnick Irving J
Published: April 2011

Visible absorption spectra and an agar-diffusion microbiological assay with Staphylococcus aureus were used to examine the effects of temperature, time, and pH on the stability of actinomycin D in distilled water, Clark and Lubs buffer solutions, and plasma. The most stable storage pH range for actinomycin D in buffer solution is 5 to 7. Actinomycin D in distilled water and stored 5° C (refrigeration) preserved its stability for at least 150 days. Except in buffer at pH 5, the antibiotic is appreciably degraded by autoclaving.
Pharmacological properties of some imidazole derivatives occurring in nature
Authors: Bertaccini G , Vitali T
Published: April 2011

Some naturally occurring histamine derivatives such as monomethylhistamine [4-(2-methylaminoethyl)imidazole], dimethylhistamine [4-(2-dimethylaminoethyl)-imidazole], spinaceamine (4,5,6,7-tetrahydroimidazo[5,4-c]pyridine) and 6-methyl-spinaceamine, and the quaternary ammonium base of histamine [4-(2-trimethyl-aminoethyl)imidazole] hitherto unknown in nature, were submitted to a pharmacological examination. The actions of monomethylhistamine resembled closely those of histamine. Dimethylhistamine was 2 to 20 times less active than histamine and showed some weak “nicotinic” effects. Trimethylhistamine had about 1% of the activity of histamine but showed a potent “nicotinic” activity on the preparations examined. Spinaceamine and 6-methylspinaceamine were virtually inactive. The importance of the N‘-methylhistamines which behave similarly to the methyl derivatives of 5-hydroxytryptamine is discussed.
Estimation of C-glycosides and O-glycosides in cascara (Rhamnus purshiana DC., bark) and cascara extract
Authors: Fairbairn J W , Simic S
Published: April 2011

An assay process is described which enables the cascarosides, the aloins and the O-glycosides of cascara to be estimated separately. The cascarosides are separated from the aloins by partition between water and ethyl acetate; each fraction is then oxidised and hydrolysed by ferric chloride treatment to the free anthraquinones which are determined colorimetrically as aloe-emodin. The O-glycosides are determined colorimetrically as emodin after acid hydrolysis. Results show that commercial extracts contain only about half the theoretical amount of C-glycosides and about quarter of the O-glycosides and there is a significant breakdown of primary glycosides. These results indicate that decomposition occurs during preparation of the official extract. One commercially available extract, which passed current official standards, was shown by the method to be very deficient in activity. In view of the small proportion of O-glycosides in commercial extracts a shortened assay process, for cascarosides and aloins only, is described.
Effect of imipramine and some analogues on the uptake of 5-hydroxytryptamine by human blood platelets in vitro
Authors: Yates Celia M , Todrick A , Tait A C
Published: April 2011

The inhibitory action of imipramine and some analogues on the uptake of 5-hydroxytryptamine by human blood platelets in vitro was investigated. In concentrations comparable with those reached in plasma during therapy, imipramine and the isosteric compound, amitriptyline, were more effective than their metabolites. Chlorpromazine was less effective than the latter and orphenadrine ineffective at the concentrations tested.
Pharmacological actions and toxicity of dimethyl sulphoxide and other compounds which protect smooth muscle during freezing and thawing
Authors: Farrant J
Published: April 2011

Dimethyl sulphoxide and other non-electrolytes have been shown to protect partially, the smooth muscle of the guinea-pig uterus from damage during freezing to and thawing from –79°. The mechanism of this protection is probably physico-chemical in nature, for none of the compounds had any specific pharmacological action on smooth muscle. In the high concentrations needed for protection the compounds themselves caused some non-specific osmotic damage to the smooth muscle. All of the compounds examined had a low toxicity in mice.
Alkaloids of Fagraea fragrans Roxb
Authors: Wan Alfred S C , Chow Y L
Published: April 2011

The major alkaloid of the leaves and fruits of Fagraea fragrans Roxb. has been isolated and shown to be 4-(2-hydroxyethyl)-5-vinyl nicotinic acid lactone identical with gentiamine.
Colorimetric method for the estimation of norethynodrel in tablets containing mestranol
Authors: Chissell J F
Published: April 2011

The colour method proposed for the estimation of norethynodrel in tablets with mestranol utilises a reaction similar to the well known Zimmerman reaction, the reagents employed being m-dinitrobenzene and benzyltrimethylammonium hydroxide solution and a solvent mixture consisting of ethyl acetate and ethanol. Maximum extinction was at a wavelength of 510 mμ and Beer’s law is obeyed for a concentration range 5 to 20μg norethynodrel per ml final solution.
Measurement of body temperature in conscious small laboratory animals by means of an oesophageal thermocouple
Authors: Brittain R T , Spencer P S J
Published: April 2011

A device is described for making rapid repeated measurements of body temperature in conscious small laboratory animals. A thermocouple, sealed inside an 18 gauge hypodermic needle is inserted into the oesophagus and the temperature read directly on a calibrated meter.
Estimation of barbiturates by quantitative thin-layer chromatography
Authors: Morrison J C , Chatten L G
Published: April 2011

A method for separating and analysing quantitatively, mixtures of barbiturates by thin-layer chromatography is described. The barbiturates are eluted from the silica gel and coupled with mercury which is then estimated by dithizone. The method can be used to assay commercial pharmaceutical preparations.
Synthesis of pyridine-2-sulphonhydrazide 1-oxide and α-(2-pyridylthio)acethydrazide and its 1-oxide
Authors: Comrie A M , Mir I
Published: April 2011

The title compounds and some of their alkylidene and acyl derivatives have been prepared. A preliminary examination of representative compounds revealed negligible antibacterial activity against selected Gram-positive and Gram-negative organisms.
Some geometrical considerations concerning the design of tablets
Authors: Cleave J P
Published: April 2011

A theoretical examination of designs best suited to give a uniform rate of release of materials from solution tablets is presented.
A direct and an indirect action of 5-hydroxytryptamine on the distal part of the isolated colon of the rat
Authors: Ulrich Karen
Published: April 2011

The motor response of 5-hydroxytryptamine (5-ht) on the distal part of the isolated rat colon was investigated by constructing dose: response curves to 5-ht, acetylcholine and nicotine; these were repeated in the presence of different antagonists and an anticholinesterase. Hyoscine abolished the responses to acetylcholine, almost completely blocked the effect of nicotine, but reduced the contractions to 5-ht only to about half of the original level. The anticholinesterase NN’-diisopropylphosphorodiamidic fluoride (mipafox) potentiated the responses to acetylcholine, 5-ht or nicotine. Procaine and cocaine inhibited to the same extent the large doses of 5-ht, but had no effect on the small doses. Both drugs reduced the contractions with nicotine. Three ganglion-blocking agents were used. Hexamethonium had no effect on acetylcholine or 5-ht, but antagonised nicotine. Mecamylamine had no effect on acetylcholine; it blocked the responses to nicotine and reduced the large doses of 5-ht. The action of dimethylphenylpiperazinium on the three agonists was similar to that of mecamylamine. 2-Bromolysergic acid diethylamide had no effect on the responses to acetylcholine, but reduced equally the contractions due to 5-ht and nicotine. It was concluded that 5-ht acted indirectly by stimulating the intramural parasympathetic ganglia and directly by an action on the muscle fibres. The direct action was pronounced with small doses, the indirect action with higher doses of 5-ht.
Preparation and antibacterial activity of isatogens and related compounds
Authors: Hooper M , Patterson D A , Wibberley D G
Published: April 2011

A number of 2-substituted isatogens are shown to possess moderate in vitro antibacterial properties. The syntheses of closely related compounds in the pyrrolo-[2,3-c]pyridine and pyrrolo[3,2-b]pyridine series are described. Antibacterial activities of these compounds, of the structurally similar indolones, N-hydroxy-indoles, indoxyls and indoles are recorded, together with those of certain styryl compounds required as intermediates.
Some tryptamine derivatives: 1-aryloxy-3-[(2-indol-3‘-ylethyl)amino]propan-2-ols
Authors: Jackman G B , Petrow V , Stephenson O
Published: April 2011

The preparation of some 1-aryloxy-3-[(2-indol-3′-ylethyl)amino]propan-2-ols is described. Their biological activity was insignificant.
A method for determining the solution rate of fine particles
Authors: Edmundson I C , Lees K A
Published: April 2011

A method is presented for determining the solution rate of fine particles, crystalline hydrocortisone acetate being used as the model substance. The method’s innovation is that it takes account of the changing particle size distribution during the solution process, using a Coulter counter to observe this. The solution rate may be expressed as diameter loss per unit time (dt = do – k2t). The solution rate of hydrocortisone acetate under the conditions of the experiment was found to be linear and to correspond to a diameter loss of 1.68 μ/hr, equivalent to 108 μg/cm2 of surface/hr. Corrections for the Noyes-Whitney effect were made.
Different types of sympathomimetic α-receptors
Authors: Van Rossum J M
Published: April 2011

Sympathomimetic effects have been studied on the isolated vas deferens of the rat, in the isolated jejunum of the rabbit and on the cardiovascular system of the cat. (–)-Noradrenaline (1-R configuration), (+)-noradrenaline (1-S configuration) and dopamine as well as a number of homologues were used as agonists. The adrenergic blocking drugs piperoxan, phentolamine, yohimbine, aceperone and the tranquillising drugs chlorpromazine, (–)-mepromazine, haloperidol, droperidol and spiramide as well as bulbocapnine were used as antagonists. The results obtained with both agonists and antagonists provide evidence that the structural requirements for drugs to react with and to activate α-receptors in the vas deferens and the rabbit intestine are different; epinine and dopamine have an identical mechanism of action.
Applicability of the Ferguson principle to systems of mixed preservatives
Authors: Evans W P
Published: April 2011

Using solubility and distribution data for methyl and propyl p-hydroxybenzoates, the degree of saturation of the aqueous phase of an oil-in-water emulsion has been calculated for various oil: water ratios. In emulsions of low oil content the propyl ester gives the higher degree of saturation of the aqueous phase, while in emulsions of high oil content the methyl ester gives the higher degree of saturation. Irrespective of the oil: water ratio, a mixture of the esters cannot give a higher degree of saturation or a higher thermodynamic activity of the aqueous phase, than either ester alone. The finding of many investigators that mixtures of the esters have higher biological activities than a single ester must therefore depend, not only on the degree of saturation, or thermodynamic activity of the aqueous phase, but also on some other unknown factors.
Comparison of sleeping time, immobility time and arousal time in mice
Authors: Hughes F W , Forney R B , Richards A B
Published: April 2011

The sodium salts of the five barbiturate hypnotics hexoba rbitone, pentobarbitone amylobarbitone, secobarbitone and phenobarbitone, were studied in mice for their effect on duration of sleeping time, immobility time and arousal time. The latter measurement is described herein for the first time and is a measure of the duration of sleep with a moderate shocking stimulus to differentiate sedation and hypnosis in the mouse. The comparative potency of the drugs by these measurements is evaluated.
A comparison of anthelmintic and antibacterial activity of some phloroglucinol derivatives
Authors: Bowden K , Ross W J
Published: April 2011

Some simple phloroglucinol derivatives previously reported to have anthelmintic properties have been tested for antibacterial action against Staphylococcus aureus and Streptococcus pyogenes. A comparison is made of the activities of these compounds against Staph. aureus and Hymenolepis nana.
Viscosity and stability relations of the system ascorbic acid: water: polysorbate 20
Authors: Nixon J R , Chawla B P S
Published: April 2011

The viscosity of dispersions of ascorbic acid in solutions of polysorbate 20 has been determined and found to be Newtonian at all concentrations studied. The course of the oxidation in polysorbate 20 appeared to be by the normal chain reaction, but the rate at which it occurred was modified by a number of factors. Incorporation within the micelle appeared to be responsible for an increase in oxidation rate, but the high viscosity of concentrated polysorbate 20 solutions, which would affect the diffusion of oxygen to the reaction site caused a much larger reduction in oxidation rate.
A new and sensitive bioassay for catecholamines
Authors: De La Lande I S , Harvey Judith A
Published: April 2011

The isolated central artery of the rabbit ear is highly sensitive to catecholamines when perfused with Krebs solution containing 5-hydroxytryptamine. The preparation responds to 1 ng of noradrenaline and is extremely long lasting. It does not discriminate between noradrenaline and adrenaline.
The nature of the adrenergic receptors of the trachea of the guinea-pig
Authors: FOSTER R W
Published: April 2011

The adrenergic receptors of the guinea-pig isolated trachea have been characterised as β-receptors by established criteria. No evidence was obtained that any α-receptors are present. (-)-Isoprenaline was 17 times more potent than (-)-adrenaline which was 10 times more potent than (-)-noradrenaline. High concentrations of piperoxan, thymoxamine and dihydrogenated ergot alkaloids did not antagonise the catecholamines, while phentolamine and phenoxybenzamine potentiated them, isoprenaline almost as much as noradrenaline. Propranolol, pronethalol and the 3, 4-dichloro-analogues of (+)-noradrenaline, adrenaline and isoprenaline each specifically antagonised the catecholamines, isoprenaline moreso than noradrenaline. The characteristics of this blockade by pronethalol and propranolol fulfilled established criteria for competitive antagonism; propranolol (pA2 against noradrenaline 6·56 + 0·21) was 18·6 (11·4 to 30·5) times more potent than pronethalol, (pA2 against noradrenaline 5·29 + 0·07).
The detection and identification of synthetic steroids in horse urine
Authors: MOSS M S , RYLANCE H J
Published: April 2011

A scheme for the detection of synthetic steroids which could be used in the “doping” of race-horses is described. The method involves extraction from urine into ethyl acetate: ether (1:1) followed by initial two-dimensional thin-layer chromatography using (1) ethyl acetate (2) methylene chloride: dioxan: water (100:50:50). Elution of the ultraviolet absorbing spots for extinction measurements is followed by further one way thin-layer chromatography as free alcohols in amyl acetate: acetone (1:1). Further chromatography of the steroid alcohols in chloroform: ether: water (80:20:0·5) on formamide-impregnated plates and chromatography of the acetates in ether helps to identify the unknown steroid. Additional identification is made by colour reactions with (1) a tetrazolium reagent (2) vanillin: perchloric acid.
Biotransformations in vitro undergone by phenothiazine derivatives in a liver preparation
Authors: ROBINSON ANN E
Published: April 2011

Characterisation of the products of biotransformations resulting when a wide range of medicinally used phenothiazine derivatives were incubated with a “microsomal and soluble” fraction of livers from albino Wistar rats, is described. The compounds were chlorpromazine, demethylchlorpromazine, dedimethylchlorpromazine, triflupromazine, promazine, acepromazine, propiomazine, diethazine, promethazine, isopromethazine, ethopropazine, trimeprazine, methotrimeprazine, ethylmemazine, proquamezine, cyamemazine, trifluoperazine, prochlorperazine, thioproperazine, fluphenazine, pecazine, and also the sulphoxides of the first three compounds and of promazine. The predominant reactions were those of dealkylation and of hydroxylation of the aromatic ring. Sulphoxidation did not occur to a significant extent with any of the compounds examined.
Release of tissue histamine by the babesicidal agents quinuronium and amicarbalide
Authors: EYRE P
Published: April 2011

Quinuronium sulphate liberated appreciable quantities of histamine from tissues of mice, rats and sheep. The signs of quinuronium poisoning in mice and rats were more severe than for compound 48/80. The animals acquired tolerance to the latter drug. Thus the toxicity of quinuronium probably depended on factors other than histamine release. Amicarbalide released amounts of histamine comparable with those liberated by quinuronium only in rat tissues.
Liver function and pyrexia caused by a pyrogen from Escherichia coli, lysergic acid diethylamide and dinitrophenol
Authors: VENULET JAN , DESPERAK-NACIαZEK ANNA
Published: April 2011

Rabbits with liver damaged by carbon tetrachloride do not respond with hyperthermia to a lipopolysaccharide pyrogen from Escherichia coli or dinitrophenol, but lysergic acid diethylamide develops its usual effect. Rabbits with obstructive liver damage react with hyperthermia to all three pyrogenic factors. The results support the concept of a peripheral action of pyrogen. It is suggested that the liver plays a rôle in the process of transforming the bacterial pyrogen into the endogenous pyrogen.
A transistorised impulse generator for recording the heart rate from intact and isolated preparations
Authors: CLARKE D E , HISCOE A , HULLEY L N , JACKSON K , LEACH G D H
Published: April 2011

A method for presenting the heart rate from intact and isolated preparations as a kymographic record is described. A transistorised impulse generator with either an integral or independent power supply is used to activate a Thorp impulse counter. The ability of the instrument to follow a wide range of heart rate changes and to measure rates in the usually encountered laboratory species is demonstrated.
The effect of isoprenaline on the contraction of smooth muscle produced by histamine, acetylcholine or other agents
Authors: FARMER J B , LEHRER D N
Published: April 2011

Isoprenaline given intravenously is a more potent antagonist of bronchospasm produced by histamine than of that produced by acetylcholine in the anaesthetised guinea-pig. This greater activity of isoprenaline against histamine was also observed on isolated tracheal muscle and ileum of the guinea-pig. It was also found in isolated guinea-pig ileum that stimulation of the periarterial sympathetic nerves produced a greater inhibition of contractions produced by histamine or 5-hydroxy-tryptamine than of those produced by acetylcholine or bradykinin. The inhibitory actions of isoprenaline were absent in tissues without β-receptors and tissues in which the β-receptors were blocked by pronethalol.
Neuromuscular blocking agents: branched-chain tetra-onium compounds
Authors: EDWARDS D , LEWIS J J , MARREN GLADYS
Published: April 2011

The compounds tri(6-dimethylaminohexyl)amine, tri(6-diethylaminohexyl)amine and tri(6-dipropylaminohexyl)amine have been synthesised and eight tetra-onium derivatives prepared from these bases have been tested for neuromuscular blocking activity on the cat, hen, frog, rat and mouse. Two of the compounds possessed ganglion blocking activity and this was much weaker than in hexamethonium. All the compounds had tubocurarine-like properties, the most active being 7-ethyl-7-(6-triethyl-hexylammonium)-7-azoniatridecamethylenebis(triethylammonium) tetra-iodide. The results of the pharmacological tests give little support for a one-point theory of receptor attachment.
Ionisation constants and partition coefficients of some analgesically active 2-benzylbenzimidazole derivatives and related compounds
Authors: CASY A F , WRIGHT J
Published: April 2011

The ionisation constants (in aqueous ethanol) and the partition coefficients (in a water-cyclohexane system) of some analgesically active 2-benzylbenzimidazole derivatives and related compounds are reported. The results are discussed in terms of structure-activity relationships.
The nephrotoxicity of analgesics
Authors: Prescott L F
Published: April 2011

IN recent years there has been increasing suspicion that prolonged or excessive use of analgesics may result in progressive renal damage very similar to that produced by chronic pyelonephritis. Phenacetin (acetophenetidin) has been widely incriminated as the offending drug, mainly because it was common to all the analgesic mixtures mentioned in the early reports. Histologically and functionally the renal lesions are predominantly tubular, with interstitial fibrosis, tubular degeneration and atrophy and a high incidence of papillary necrosis and pyelonephritis (Rubenstein, Abrahams, Stables & Levin, 1964).
Partial molal volumes of some non-ionic detergents in monomeric and micellar form
Authors: Florence A T
Published: April 2011

Partial molal volumes of five synthetic non-ionic detergents have been measured above and below their critical micellar concentrations. The increases in volume on micellisation are discussed in terms of changes in hydration and hydrophobic bonding. The change in partial molal volume at the critical micellar concentration decreased with temperature. At 20° increases of 5, 9 and 17 ml mole−1 were obtained for the n-butyl, n-hexyl and n-octyl hexaoxyethylene glycol ethers respectively. For comparison with the alkyl ethers, the partial molal volume of hexaoxyethylene glycol was determined at four temperatures. The utility of density measurements for the determination of the critical micelle concentration of these non-ionic detergents depended on the temperature of the system; at higher temperatures the change in slope of density-concentration plots at the critical micelle concentration decreases and sometimes is not detectable.
A periarterial nerve-circular muscle preparation from the caecum of the guinea-pig
Authors: Akubue P I
Published: April 2011

A periarterial nerve-circular muscle preparation from the caecum of the guinea-pig has been described. Stimulation of the periarterial nerve produced relaxation of the circular muscle strip. These responses were blocked by adrenergic neurone blocking agents but not by ganglion blocking drugs. Phenoxybenzamine or piperoxan greatly reduced the relaxation but propranolol abolished it. No relaxation was observed on preparations from animals pre-treated with reserpine. It was observed that after the blockade of the responses to periarterial nerve by adrenergic neurone blocking drugs, stimulation of the periarterial nerves in the presence of physostigmine induced contractions which were blocked by local anaesthetics or hyoscine but not consistently by ganglion blocking drugs.
Aloe-emodin glycosides of senna leaf
Authors: Fairbairn J W , Shrestha A B
Published: April 2011

A new glucoside has been isolated from senna leaf (Cassia senna L.) and shown to be identical with the aloe-emodin-8-mono-β-D-glucoside recently isolated from Rheum palmatum. This new quinone glucoside is insoluble in water and is present in only small quantities and therefore unlikely to contribute much to the activity of the drug. Confirmation of the presence of a second, highly water soluble glycoside based on a reduced form of aloe-emodin is given; this glycoside may well be responsible for the reported “synergistic effect” of the non-rhein glycosides of senna leaf.