bluuebunny/crossref_metadata_2025_split huggingface dataset:
A potent β-adrenoreceptor blocking drug: 4-(2-hydroxy-3-isopropylaminopropoxy)indole
Authors: Moore Glynne E , O’Donnell Stella R 
Published: April 2011

Abstract
4-(2-Hydroxy-3-isopropylaminopropoxy)indole (LB46) is a competitive β-adrenoreceptor blocking drug with a potency of between 4 and 7 times that of propranolol on the guinea-pig isolated trachea and atria (chronotropic effects). LB46 itself produces tracheal relaxation which may result from an indirect sympathomimetic action. The influence of uptake into adrenergic nerves on pA2 and pA10 values for LB46 and propranolol, when using noradrenaline as agonist drug, has been assessed from results obtained on trachea in the presence and absence of cocaine (10−5m). In the absence of cocaine the slopes of the regression of log (dose ratio —1) against negative log molar concentration of antagonist were less than the theoretical value of —1·0. In the presence of cocaine the slopes of these regressions approached —1·0. Thus values of (pA2-pA10) also deviated from the theoretical value in the absence of cocaine but approached it if cocaine was present in the bath fluid.
The activities of α- and β-adrenoceptive blocking agents in reducing intestinal relaxation due to sympathetic stimulation in the pithed rat
Authors: Parkes M W , Gerrard Christine A 
Published: April 2011

Abstract
A pithed rat preparation, stimulated electrically via the pithing rod left in position, was employed to examine the effects of drugs, administered intravenously, on relaxation of a loop of ileum. Relaxation due to injected isoprenaline could be largely blocked by propranolol but that due to nervous stimulation or injected noradrenaline was blocked to only a lesser extent by either propranolol or phenoxybenzamine alone. The combination of phenoxy-benzamine and propranolol was more effective against relaxation from nervous stimulation than either drug alone but was still not as effective against this as against noradrenaline, or as propranolol alone against isoprenaline. It is concluded that intestinal relaxation after nervous stimulation involves both α- and β-adrenergic activity, in variable proportions. Adrenoceptive antagonists are not as effective in blocking these receptors as they are for those concerned in relaxation after injected catecholamines.
The displacement of l-tryptophan and dipeptides from bovine albumin in vitro and from human plasma in vivo by antirheumatic drugs
Authors: Mcarthur J N , Dawkins P D , Smith M J H 
Published: April 2011

Abstract
l-Tryptophan occurs in a protein-bound and an unbound form in serum from normal subjects. The amino-acid is displaced from its binding sites in vitro by salicylate, phenylbutazone, indomethacin, prednisolone, chloroquine and gold salts and is virtually absent in serum obtained from patients with rheumatoid arthritis receiving therapy with antirheumatic drugs. Some dipeptides bind to bovine albumin in vitro and are displaced by salicylate. All the drugs displace l-phenylalanyl-l-phenylalanine from its binding to normal human serum in vitro.
Salicylate-induced inhibition of collagen and mucopolysaccharide biosynthesis by a chick embryo cell-free system
Authors: NAKAGAWA HIDEO , BENTLEY J PETER 
Published: April 2011

Abstract
The ability of a chick embryo cell-free system to synthesize collagen, mucopolysaccharide and non-collagen protein in the presence of sodium salicylate was studied. Added creatine phosphate together with endogenous creatine kinase was the ATP generating system. The incorporation of labelled proline or labelled glucose into collagen or mucopolysaccharide respectively depended on ATP level in the cell-free system used. Salicylate inhibited collagen and mucopolysaccharide synthesis to a greater extent than non-collagen protein synthesis. The ability of the cell-free system to hydroxylate labelled protocollagen was inhibited 50% by storage at −18°. Ferrous iron reversed this inhibition. Salicylate prevented the restoration of the enzyme activity by ferrous iron. Incorporation of radioactivity into hyaluronic acid, when labelled UDP-glucuronic acid and UDP-N-acetylglucosamine were supplied, was inhibited 17% by salicylate. Under the same conditions 47% inhibition of incorporation into chondroitin sulphate was seen. This suggests that UDP-N-acetyl-glucosamine-UDP-N-acetylgalactosamine epimerase is inhibited by salicylate.
The influence of test conditions on the disintegration time of gelatin capsules
Authors: JONES B E , COLE W V J 
Published: April 2011

Abstract
The British Pharmacopoeia test for capsule disintegration is basically the same test as that used to measure tablet disintegration and as such it has some shortcomings, particularly in the determination of the end point. The results were significantly affected by the capsule size, the nature of the test solution, the temperature, and whether single capsules were tested instead of groups of five. The effect of temperature on capsule solubility was demonstrated. A modified test was applied to both hard and soft capsule products selected from the British Pharmacopoeia. Recommendations are made for new specifications for an official pharmacopoeial test.
Application of orthogonal functions to spectrophotometric analysis of weakly absorbing compounds in tablets
Authors: ABDINE H , WAHBI A M , KORANY M A 
Published: April 2011

Abstract
Glenn's method of orthogonal functions has been applied to correct for irrelevant absorption during the analysis of tablets of chlorpheniramine maleate, phenyltoloxamine dihydrogen citrate, diphenhydramine hydrochloride and ephedrine hydrochloride. The results suggest that the method can be used for routine analysis.
Constituents of two varieties of Indian dill
Authors: SHAH C S , QADRY J S , CHAUHAN M G 
Published: April 2011

Abstract
Two varieties of Indian dill, Anethum sowa, are available. They differ morphologically and have a different oil composition. They have a low dillapiole content (12–15%) and have a high content of carvone-dihydrocarvone (50–64%).
The relation between the vapour pressure of a drug and its concentration emerging in the air stream from a nasal inhaler
Authors: ARMSTRONG P A M , CARLESS J E , ENEVER R P 
Published: April 2011

Abstract
A method of determining the absolute vapour pressures of volatile drugs and drug-adjuvant mixtures is described. The absolute vapour pressures of methylamphetamine, propylhexedrine and eucalyptol have been determined over a range of temperatures. The concentrations of these drugs emerging from a nasal inhaler system have also been measured under similar experimental conditions. From the inhaler results, it has been possible to derive values for the vapour pressures of the drugs in the system and compare them with absolute vapour pressure values. The derived pressures were lower than the absolute pressures at any given temperature. Nevertheless, there seems to be reasonable agreement among the latent heats of vaporization of the three drugs using either parameter. The factors that may give rise to the low values of derived vapour pressure are discussed. Mixtures of eucalyptol and methylamphetamine examined using the same techniques, show that both with the inhaler system and with mixtures of the pure drugs a similar liquid-vapour equilibrium exists. The vapour pressure-composition diagram constructed from either set of results shows a positive deviation from Raoult's law.
The drug release characteristics of various rectal suppositories as determined by specific ion electrodes
Authors: THOMAS W H , MCCORMACK R 
Published: April 2011

Abstract
Suppositories containing sodium phenobarbitone (200 mg) were manufactured with the following bases; cocoa butter, cocoa butter plus beeswax, Dehydag and polyethylene glycols. The release of sodium ions through a dialysis membrane was conveniently measured with a sodium-specific ion electrode. The method facilitates evaluation and comparison of suppository bases and allows continuous monitoring of the release of active ingredient.
Species-dependent effects of fenfluramine on the central nervous system
Authors: FUNDERBURK WILLIAM H , HASH AVERY M , HAZELWOOD JEAN C , WARD JOHN W 
Published: April 2011

Abstract
The cortical effects of fenfluramine and a metabolite, norfenfluramine, were studied in rabbits and cats. The parent compound produced slow waves in the e.e.g. which were compatible with sedation in cats. Norfenfluramine also produced slow waves and apparent sedation in cats, but neither compound produced marked changes in the cortical waves of rabbits. When cortical waves in both species were slowed with pentobarbitone, fenfluramine increased the frequency of the waves in rabbits but did not alter the frequency in cats. Both fenfluramine and the metabolite blocked cortical after-discharges in both species. There is no apparent explanation for the differences in the action of the two drugs in the two species.
The estimation of the “free” and “bound” acetylcholine content of rat brain
Authors: SLATER P 
Published: April 2011

Abstract
Rat brains, not frozen, were homogenized in saline solution containing physostigmine, and also cupric chloride to inhibit choline acetyl-transferase. When brains were homogenized for periods of up to 3 min, the amount of acetylcholine extracted was proportional to the duration of homogenization. After 3 min, there was no further significant increase in acetylcholine. The acetylcholine extracted in this way was termed “free”; whereas that remaining in the brain tissue and extracted by acid-ethanol solution was termed “bound”. The total amount obtained from each brain was not significantly different from the total amount extracted by a more conventional method from the brains of rats killed by rapid freezing in liquid air. This observation applied also to brains removed from animals during anaesthesia and convulsions.
The site of the inhibitory action of salicylate on protein biosynthesis in vitro
Authors: BURLEIGH MARY , SMITH M J H 
Published: April 2011

Abstract
Salicylate (10 mm) affects neither the transfer of the amino-acid from leucyl-tRNA into protein by rat liver polysomes nor the formation of the leucyl-tRNA. However, lower concentrations of salicylate inhibit the activities of other aminoacyl-tRNA synthetases. The most sensitive enzymes are those which incorporate glutamate, aspartate and histidine. It is suggested that salicylate interferes with the in vitro biosynthesis of protein by preferentially inhibiting the production of certain aminoacyl-tRNA species. The drug, in concentrations of 0·6 mm and above, inhibits the ATP-pyrophosphate exchange reaction promoted by individual amino-acids, including leucine.
Anti-acetylcholinesterase activity of some stereoisomeric aminobornanes
Authors: BECKETT A H , LAN NGIAM TONG , KHOKHAR ABDUL Q 
Published: April 2011

Abstract
Bornyl analogues of choline and acetylcholine with eclipsed cis- and trans-configurations displayed low inhibitory activity towards acetylcholinesterase catalysed hydrolysis of acetylcholine; cis-isomers were slightly better inhibitors than their trans-counterparts. (+)-Bornan-2-one-3-endo-yltrimethylammonium bromide with its oxygen atom and the quaternary ammonium group fixed rigidly in the gauche configuration is much more potent inhibitor than its enantiomorph.
The effect of starch type, concentration and distribution on the penetration and disruption of tablets by water
Authors: FRASER D R , GANDERTON D 
Published: April 2011

Abstract
The effect of starch type, and its concentration and distribution, on the pore structure of tablets of aspirin and magnesium carbonate has been measured using air permeability and liquid penetration techniques. The addition of starch had no significant effect on the pore structure of the dry tablet but caused disruption and alteration of this structure when penetrated by water. When each starch was incorporated into the granules in wet massing the rate of disruption decreased in the order potato, maranta, wheat, corn, waxy corn and rice; but a more complicated pattern was produced when the starch was added to the granules as a pre-dried powder. Maximum breakup efficiency of magnesium carbonate tablets was produced when 10 % potato starch was incorporated internally and the tablet compacted to a porosity of 28 %.
The modifying effects of a cationic surfactant on the rates of base catalysed hydrolysis of esters of different structures
Authors: MEAKIN B J , WINTERBORN I K , DAVIES D J G 
Published: April 2011

Abstract
The effect of a cationic surfactant, cetyltrimethylammonium bromide (CTAB), on the hydrolysis rates of four esters of different structure has been investigated. The esters used were ethyl p-aminobenzoate (EPAB), p-nitrophenyl acetate (PNPA), ethyl p-nitrobenzoate (EPNB) and p-aminophenyl acetate (PAPA). Association between the esters and the CTAB occurs so that above its cmc the surfactant modifies the rates of hydrolysis, increasing those of EPNB and PNPA and decreasing those of EPAB and PAPA. It thus appears that the type of group on the p-position of the aromatic ring plays a major role in determining the kind of effect brought about by the CTAB. Possible reasons to explain the two different effects that CTAB has on ester hydrolysis are put forward.
The analysis of nicotine-1‘-N-oxide in urine, in the presence of nicotine and cotinine, and its application to the study of in vivo nicotine metabolism in man
Authors: BECKETT A H , GORROD J W , JENNER P 
Published: April 2011

Abstract
A rapid quantitative assay for nicotine-1′-N-oxide in urine, in the presence of nicotine and cotinine, is reported. The urinary excretion of nicotine, cotinine and nicotine-1′-N-oxide was determined after nicotine had been administered in cigarette smoke, orally, or intravenously to subjects with either fluctuating, controlled acidic or controlled alkaline urinary pH. The urinary excretion of the N-oxide in 24 h from smokers under normal conditions was about half that of the cotinine excretion; more trans- than cis-diastereoisomer of nicotine-1′-N-oxide was excreted.
The effect of smoking on nicotine metabolism in vivo in man
Authors: BECKETT A H , GORROD J W , JENNER P 
Published: April 2011

Abstract
Nicotine and a basic metabolite, cotinine, were determined in the urine by gas-liquid chromatography after intravenous administration of (—)-nicotine hydrogen (+)-tartrate to groups of male and female smokers and non-smokers in whom the urine was maintained at an acid pH. The urinary recoveries of nicotine and cotinine from male smokers fell in two groups. One showed a lower recovery of both alkaloids than was seen with male non-smokers. The other showed a similar recovery of nicotine but more cotinine than the male non-smokers. Female smokers excreted less nicotine but more cotinine than female non-smokers. More nicotine but less cotinine was excreted by female non-smokers than by male non-smokers. The results show sex dependent metabolism of nicotine occurs in non-smoking humans and that smoking causes alterations in nicotine metabolism.
Buccal absorption as a parameter of analgesic activity of some p-substituted acetanilides
Authors: DEARDEN J C , TOMLINSON ERIC 
Published: April 2011

Abstract
The extent of buccal absorption of 16 p-substituted acetanilides is related parabolically to analgesic activity. The correlation is slightly better than that between log (partition coefficient) and analgesic activity. Thus, for this series of compounds at least, an in vivo partition test provides a slightly better parameter of biological response than does an in vitro test.
Membrane osmometry of solubilized systems
Authors: ATTWOOD D , ELWORTHY P H , KAYNE S B 
Published: April 2011

Abstract
The solubilization of decane, ethyl p-hydroxybenzoate, methyl anisate and p-hydroxybenzoic acid by aqueous micellar solutions of cetomacrogol 1000 has been examined by membrane osmometry and viscosity techniques. The effect of the solubilizates on the number-average micellar molecular weight, Mn, has been related to their site of incorporation in the micelle. Decane and methyl anisate are solubilized in the hydrocarbon core of the micelles and both compounds produce an increase in Mn up to a maximum value of 2·0 times 105, at a solubilizate concentration of approximately 80% of the saturation limit for each compound. This increase is shown to result from an increase in the number of molecules of both solubilizate and of surfactant per micelle. Further addition of solubilizate, to produce a saturation level in excess of 80%, results in a decrease in micellar size in both systems. The solubilization of ethyl p-hydroxybenzoate and p-hydroxybenzoic acid is thought to involve the oxyethylene region of the micelle and both solubilizates cause an increase in Mn owing to the inclusion of solubilizate into the micelle, the number of molecules of surfactant per micelle being unaffected by the solubilization process. Viscosity studies on the decane-ceto-macrogol-water system are interpreted as indicating no change in either micellar symmetry or hydration as a result of solubilization. A spherical model for the micelles is shown to be consistent with the experimental data.
A laser light scattering apparatus
Authors: PUGH W J , SAUNDERS L 
Published: April 2011

Abstract
The use of a low power helium-neon laser for light scattering measurements is described. The Rayleigh and Cabannes theories have been modified for polarized incident light. A new procedure is recommended for data when the solvent correction is relatively high. Using this method a precision of 4·7 % was obtained for the molecular mass of bovine plasma albumin in water, compared with 6·3 % for the more usual method.
Adsorption of phosphatidylcholine at the benzene-water interface
Authors: JOHNSON M C R , SAUNDERS L 
Published: April 2011

Abstract
Interfacial tensions between benzene solutions of egg-phosphatidyl-choline and aqueous bovine plasma albumin have been studied. The presence of the protein in the aqueous phase leads to a more rapid adsorption of the phospholipid at the interface, this being a result of interaction between the phospholipid and protein. The most probable mechanism for the interaction is discussed. The interfacial tensions between aqueous dispersions of egg-phosphatidyl-choline and pure benzene have also been determined. The results clearly indicate the effect of ultrasonic treatment in producing a stable aqueous phospholipid dispersion.
The particle-size of sulphadiazine produced by a solvent-change method
Authors: ELWORTHY P H , WORTHINGTON H E C 
Published: April 2011

Abstract
The factors affecting the particle-size of sulphadiazine produced by a solvent-change method of crystallization have been studied. The most important variables appear to be the degree of turbulence in the pipeline mixer used for the crystallization process, and the concentration of drug in the dimethylformamide injection solution. Mechanisms which can account for these, and other features of this crystallization method, are presented.
Inactivation of resistant Pseudomonas aeruginosa by antibacterial combinations
Authors: RICHARDS R M E 
Published: April 2011

Abstract
P. aeruginosa resistant to preservative concentrations of benzalkonium chloride, phenylmercuric nitrate and chlorocresol in nutrient broth was inactivated by using phenylethanol-antibacterial combinations. EDTA-antibacterial combinations also showed increased activity using benzalkonium and chlorocresol. P. aeruginosa resistant to 0·25% chlorbutol was inactivated using phenylethanol-chlorbutol combinations at concentrations which were ineffective alone. Similarly P. aeruginosa having an increased resistance to chlorhexidine was inactivated by phenylethanol-chlorhexidine combinations at concentrations that were ineffective alone. Phenylethanol showed a greater general usefulness than EDTA at the concentrations tested.
Phenylethanol enhancement of preservatives used in ophthalmic preparations
Authors: RICHARDS R M E , MCBRIDE R J 
Published: April 2011

Abstract
The growth rates of P. aeruginosa in subinhibitory concentrations of antibacterial preservatives alone and in combination with phenylethanol were determined by an extinction method. Phenylethanol enhances the effect of benzalkonium chloride on growing cultures of P. aeruginosa and the results have been confirmed by viable counts. A similar effect is shown by phenylethanol in combination with chlorbutol, chlorhexidine diacetate, chlorocresol, merthiolate, methyl and propyl hydroxybenzoate mixture and phenylmercuric nitrate.
The application of photoelastic techniques to a rotary tabletting machine
Authors: RIDGWAY K , ROSSER P H 
Published: April 2011

Abstract
Powders have been compacted on a rotary tabletting machine, using a Perspex die mounted above the die table, with an extended lower punch and a shortened upper punch. By high speed cine photography in polarized light, the fringes due to the radial stress in the die wall were recorded during compaction. At the same time, the upper and lower punch forces were monitored by instrumented pressure rollers coupled to a recording oscilloscope. The total information thus obtained was sufficient to enable compression cycles to be determined for the first time on a rotary machine.
Effect of nigral lesion on chlorpromazine-induced acceleration of dopamine synthesis from [14C]tyrosine
Authors: NYBÄCK HENRIK , SEDVALL GÖRAN 
Published: April 2011

Abstract
The nigro-neostriatal dopamine pathway of the rat brain was subjected to a unilateral stereotaxic lesion at the level of the hypothalamic-mesencephalic junction. Fifteen days after the operation endogenous dopamine and[14C]dopamine formed in vivo from [14C]tyrosine were reduced to about 15% in the striatum ipsilateral to the lesion. Twenty-four h after the lesion the contents of endogenous and labelled dopamine were about the same in the striata of both sides. Chlorpromazine (15 mg/kg) accelerated several fold the accumulation of [14C]dopamine formed from [14C]tyrosine in the striatum on the intact side. However, in the striatum on the side of the lesion, chlorpromazine did not increase the accumulation of [14C]dopamine. The results indicate that chlorpromazine accelerates dopamine synthesis in the striatum by an indirect mechanism, presumably by activating the nerve impulse flow in the nigro-neostriatal dopamine pathway.
The oestrogenic and anti-oestrogenic properties of ring methyl-substituted stilboestrols
Authors: CLARK E R , McCRACKEN ANNA M 
Published: April 2011

Abstract
3,3′,5,5′-Tetramethylstilboestrol (I) and its α,α′-dimethyl- (II) and α,α′-diethyl- homologues (III) have been tested for oestrogenic and anti-oestrogenic activity. α,α′-Diethyl-3,3′,5,5′-tetramethylstilboestrol (III), by the uterine weight assay in immature mice, is 2·1 times 10−4 times as potent as an oestrogen as 17β-oestradiol [fiducial limits (0·95) = 1·59 times 10−4 −2·74 times 10−4] but 3,3′,5,5′-tetramethylstilboestrol (I) and α,α′,3,3′,5,5′-hexamethylstilboestrol (II) were oestrogenically inactive at a dose of 0·8 mg. Compound III exhibited auto-inhibition of its own oestrogenic response at doses between 1·8 and 7·2 mg. None of the compounds tested inhibited the uterotrophic response to 17β-oestradiol. Compounds II and III, but not compound I, produced a highly significant inhibition of the vaginal cornification response to 17β-oestradiol when the test compounds (5 μg) and 17β-oestradiol were administered intra-vaginally in a single solution. It is suggested that the compounds II and III compete with 17β-oestradiol for the oestrogen receptor and that methyl groups positioned ortho to the phenolic hydroxyl group sterically interfere with the binding of the compounds to the oestrogen receptor, or with the initiation of the oestrogenic response, or both.