bluuebunny/crossref_metadata_2025_split huggingface dataset:
Gas-liquid chromatographic estimation in blood of ICI 58 834
Authors: Case D E 
Published: April 2011

Abstract
The blood levels attained at therapeutic oral doses of ICI 58 834 hydrochloride, a novel psychotropic agent, are adequately assayed by gas-liquid chromatography. The free base is extracted into benzene and converted to its heptafluorobutyrate derivative. The derivative is chromatographed on a column of 1% XE60 on Gas-Chrom Q and detected by electron capture. Recovery from blood is 80–90% and the minimum detectable level is about 20 ng compound ml−1 whole blood.
An infrared study of the interaction between Aerosil-200 and polydimethylsiloxane (dimethicone-1000)
Authors: Buist G J , Burton J S , Elvidge J A 
Published: April 2011

Abstract
The individual hydrogen-bonds formed between Aerosil-200 and dibutyl ether are stronger than those formed between the Aerosil and dimethicone-1000 (PMS). Nevertheless, because there is multiple hydrogen-bonding to the PMS and because the molecules of this fit the Aerosil surface well, the total interaction is very strong.
The effects of phospholipase C on excitation-contraction coupling mechanisms in smooth muscle
Authors: Lodge S , Leach G D H 
Published: April 2011

Abstract
The technique of incubation with phospholipase C has been used as a means of investigating the role of phospholipids in the excitation-contraction coupling mechanisms of smooth muscle. The effects of this incubation procedure were observed upon the interactions of calcium with the contractile responses of the guinea-pig ileum longitudinal muscle preparation under a number of conditions. The reduction in the acetylcholine responses of both normal and potassium depolarized tissues after incubation was partially restored by a tenfold increase in the calcium concentration of the bathing medium. A faster rate of decline of contractile responses upon immersion in calcium-free solutions and a slower rate of restoration upon the reintroduction of calcium were seen in both normal and depolarized tissues. The relation between the external calcium concentration and the size of the contractile responses to a given stimulus was also changed. The size of the response to added calcium obtained in a potassium depolarized preparation was also reduced after phospholipase C incubation. These results and their implications are discussed.
The bronchoconstrictor action of the tetradecapeptide bombesin in the guinea-pig
Authors: Impicciatore M , Bertaccini G 
Published: April 2011

Abstract
The tetradecapeptide bombesin was found to exert a potent spasmogenic action on the bronchiolar muscle of the anaesthetized guinea-pig. The threshold bronchoconstrictor dose ranged between 50 and 200 ng kg−1. Other spasmogenic substances tested in the same experimental conditions, except physalaemin, were much less effective. Since antagonists of acetylcholine, histamine or 5-hydroxytryptamine did not inhibit the bronchoconstriction it is suggested that bombesin acts either by direct stimulation of the smooth muscle or by the prior release of other, as yet unidentified, spasmogenic substances.
Anti-inflammatory activity in human plasma
Authors: Ford-Hutchinson A W , Insley M Y , Elliott P N C , Sturgess E A , Smith M J H 
Published: April 2011

Abstract
Pooled human plasma contains a fraction, separable by ultrafiltration and column chromatography, which possesses anti-inflammatory activity in the carrageenan oedema test in the rat, may be partially purified by solvent extraction, has an apparent molecular weight below 1000, and is resistant to acid and proteolytic digestion.
A substance showing experimental anti-inflammatory activity has been isolated from human serum (McArthur, Smith & Freeman, 1972). The present paper describes a much simpler preparation of this material from pooled human plasma, its partial purification by extraction with acetone and ethanol, its ultrafiltration through several membranes, and its resistance to acidic, proteolytic and thermal degradation. A preliminary account of part of this work has been published (Elliott, Ford-Hutchinson & others, 1973).
Stereochemical and structural assignment to benzomorphans by mass spectrometry
Authors: Vaughan D P , Beckett A H 
Published: April 2011

Abstract
The fragmentation of some alkyl-substituted-6,7-benzomorphans upon electron impact (70eV) is characteristic. The relative intensities of some ions varies in a predictable manner depending on the configuration of the C-9 hydrogen atom. Configuration and structure of 5,9-disubstituted-6,7-benzomorphans can be assigned by mass spectrometry even when only one isomer of a structure capable of existing in diastereoisomeric forms is available.
The use of radioisotopically labelled methyl esters in the determination of the 15-epimer content of prostaglandins
Authors: Jones M F 
Published: April 2011

Abstract
The quantitative determination of the 15-epimer content of prostaglandins by formation of their isotopically-labelled methyl esters is described. Either [3H]dimethyl sulphate or [14C]diazomethane are used as esterification reagents. The reaction products are separated by thin layer chromatography and the epimer ratio determined by scintillation counting of the labelled ester zones. The accuracy of the technique is illustrated by the determination of 15-epimer in ICI 74 205, a close analogue of PGF2α. Evidence for the uncatalysed reaction of diazomethane with the alcoholic hydroxyl groups of prostaglandin molecules, which could be significant in other prostaglandin analysis techniques (e.g. g.l.c.) which depend on quantitative esterification with this reagent, is also presented.
Studies on the nature of the increased monoamine oxidase activity in the rat heart after adrenalectomy
Authors: Callingham B A , Laverty R 
Published: April 2011

Abstract
The increased activity, induced by adrenalectomy, of the enzyme monoamine oxidase (MAO) in the rat heart was found to resemble closely that present in the hearts of control animals. No significant differences were observed in the nature of the response to heat denaturation, changes in pH or to inhibition by pargyline or clorgyline. The relative activities using the substrates tyramine, 5-hydroxytryptamine, dopamine or benzylamine were the same. No evidence was found to suggest the presence of a heat-stable or dialysable inhibitor of enzyme activity. In young rats there was an increase in the relative enzyme activity using benzylamine as substrate, compared with the activity using tyramine, in the first few days after adrenalectomy. No effect of adrenalectomy could be detected upon the MAO activity in the rat brain or liver. It is concluded that the increase in rat heart MAO following adrenalectomy cannot be due to the synthesis of an enzyme with different catalytic properties, nor to the transformation of the existing enzyme into one of increased catalytic ability but with different properties.
Chemical composition and potential activity of Argentine marihuana
Authors: Chiesa E P , Rondina R V D , Coussio J D 
Published: April 2011

Abstract
The occurrence and amount of Δ1-tetrahydrocannabinol, cannabidiol and cannabinol in Argentine marihuana have been investigated, and its potential activity assessed. The analytical method was applied to thirteen different samples obtained from the Argentine Police or from domestic cultivations of Cannabis sativa L. The Δ1-tetrahydrocannabinol content including decarboxylated precursors ranged from 0.1 to 8.3 g per 100 g of the dried drug according to the source.
Kinetics of three structurally related bicyclic antidepressant compounds—a comparison in the dog
Authors: Overø K Fredricson 
Published: April 2011

Abstract
Kinetic experiments have been made with three structurally related compounds selected from a series of bicyclic antidepressant compounds. Plasma concentrations were assayed after doses of 5 mg kg−1 given as an intravenous infusion over 2 h to three dogs. The data were evaluated according to a two compartment open model, and kinetic parameters reflecting distribution and elimination characteristics of the drugs were calculated. An attempt was made to evaluate possible relations between chemical structure and these parameters. The lowest drug levels and the most rapid elimination were obtained with a compound utilizing sulphoxidation as an additional pathway of metabolism. The compounds lacking this possibility had considerably slower elimination kinetics, the less lipophilic being the slowest one. Little individual variation was seen. A relation between increased lipophilicity and increased localization in the peripheral compartment was indicated. However, the importance of other factors, such as binding phenomena within tissues, was also indicated.
The binding of paracetamol to plasma proteins of man and pig
Authors: Gazzard B G , Ford-Hutchinson A W , Smith M J H , Williams R 
Published: April 2011

Abstract
The binding of N-acetyl-4-aminophenol (paracetamol) to human and porcine plasma at both toxic and therapeutic concentrations was investigated by ultrafiltration and equilibrium dialysis over the range 50–300 μg ml−1. Plasma protein binding occurred at paracetamol concentrations greater than 60 μg ml−1. The extent of protein binding at a plasma concentration of 280 μg ml−1 of the drug is between 15 and 21% for both pig and man. There is no appreciable binding to erythrocytes in either species over the whole concentration range studied.
Dissolution and bioavailability of digoxin tablets
Authors: Fraser E J , Leach R H , Poston J W , Bold A M , Culank L S , Lipede A B 
Published: April 2011

Abstract
A dissolution test is described for tablets of digoxin B.P. Dissolution profiles are reported for 11 brands of digoxin tablets available in Gt. Britain in 1972. Good correlations exist between both the area under the serum concentration/time curve from 0–6 h and (1) the amount of digoxin dissolved in 1 h, (2) the reciprocal of the time for 50% dissolution.
Determination of the thermodynamics of hydroxyl and carboxyl groups in solutions of drug molecules
Authors: Davis S S 
Published: April 2011

Abstract
The contributions of hydroxyl and carboxyl groups to solute activity and partition coefficients have been investigated using literature data. Both polar functions give rise to a reduced activity coefficient for aromatic solutes in water and differences exist between ring and asubstitution. Partition coefficients are similarly affected but the magnitude of the group contribution to the free energy of transfer is dependent on the nature of the solute and the organic partition solvent. The contribution for the groups in the terminal position in aliphatic compounds can be obtained by an extrapolation procedure where the group value is a composite of the polar function and a term that takes into account the inequality of aliphatic CH2 and CH3 groupings (H. .OH, H. .COOH). For a range of solvents there is good correlation between hydroxyl and carboxyl group values. In addition an attempt has been made to correlate group values for CH2, CH3, H. .OH, H. .COOH, with physico-chemical parameters that are characteristic of the partition system. The best correlations are obtained between group values and the solubility of water in the organic partition solvent. The H. .OH and H. .COOH group values can also be correlated with infrared spectroscopy data and self-association constants respectively.
A note on the chemical change of pentazocine in aqueous acidic media
Authors: Vaughan D P , Beckett A H 
Published: April 2011

Abstract
Pentazocine decomposes in the acidic conditions used to hydrolyse glucuronides. The structure of the decomposition product was identified as 2′-hydroxy-2-(3-methyl-3-hydroxy-butyl)-5,9-dimethyl-6,7-benzomorphan. Pentazocine is stable when incubated at 37°, pH 5.0, and can be stored in biological fluids without drug loss.
Factors affecting the antidiuretic actions of the 18-monoacetate of (+)-aldosterone and of a substance secreted by heart muscle, in rats
Authors: Lockett Mary F 
Published: April 2011

Abstract
The method for the assay of a steroid-like substance secreted by the heart (HS) in terms of the biological activity of the 18-monoacetate of (+)-aldosterone (18MA) has been improved. Rats were equipped with ascending carotid, descending external jugular and bladder polyethylene cannulae and the urethra was ligated, under pentobarbitone anaesthesia, 24–36 h before use. Assays were made in restrained animals during sustained water diuresis induced by an intravenous infusion of glucose, 5%, and NaCl, 0&#x006d;̇9%; 2: 1 at 9 mlh−1. Antidiuretic responses (measured as the area under the curve) to ascending carotid injections of 18MA and of HS, made at 0&#x006d;̇01 ml s−1, maximum 15 s, were obtained from single dilutions of HS and 18MA: urine flow per min was recorded from drop (0&#x006d;̇025 ml) counters. Denervation of the carotid sinus above the carotid cannula did not influence the antidiureses. Data obtained were analysed by normal statistical procedures. Ascending carotid injections of 18MA and HS did not influence mean systemic arterial pressures, the clearances of creatinine and of PAH or the urinary outputs of Na+ and K+. The antidiuresis produced was compatible with the release of ADH by HS and by 18MA. Marked seasonal variations in threshold sensitivity to 18MA and in the slopes of the log dose-effect curves for the antidiuretic actions of 18MA are described. Variations both in the threshold sensitivity and in the log dose-effect curves for the anti-diuresis caused by 18MA occur between rats of different strains.
A note on the effect of amantadine on body temperature in mice
Authors: Davies J A , Redfern P H 
Published: April 2011

Abstract
Amantadine hydrochloride caused a dose-dependent fall in rectal temperature in mice. This response was antagonized by haloperidol, which itself produced some hypothermia, and by pretreatment with α-methyl-p-tyrosine. The mode of action of amantadine and the possible involvement of dopamine in the control of body temperature is discussed.
The determination of fluorochlorocarbons in air and body fluids
Authors: Rauws A G , Olling M , Wibowo A E 
Published: April 2011

Abstract
A gas chromatographic method for the separation and determination of fluorochlorocarbons (FCC's) is described. Porapak Q is used as the solid phase. The column temperature is 150°. The compounds are detected by means of a tritium foil electron capture detector. The retention times under the conditions used are 1, 2, 4 and 7&#x006d;̇5 min for the FCC's 11, 114, 12 and 113 respectively. Concentrations in air are determined directly, the concentrations in body fluids are determined by means of head space analysis. The detection limits for the various FCC's vary between 0&#x006d;̇5 and 35 pg. The method is applied in determining FCC concentrations in air and in rat blood in vivo.
Some properties of an oil-soluble phosphated fatty alcohol ethoxylate
Authors: Groves M J , Mustafa R M A , Carless J E 
Published: April 2011

Abstract
Although phosphated hydrocarbon ethoxylates are claimed to have properties associated with the presence of both non-ionic and anionic groups in their molecules, a recent investigation of a phosphated nonylphenol ethoxylate demonstrated that the phosphate group had only a slight influence on the properties of this compound. The properties of an oil-soluble phosphated fatty alcohol ethoxylate of commercial origin has now been investigated. This material was substantially homogeneous, corresponding to a structure C9H19-(OCH2CH2)3-O-PO(OH)2—mol wt = 356
Although with considerable solubility in non-polar solvents, the compound has a slight solubility in water which is increased with increased pH, suggesting that the polar phosphate group has an influence on the properties of the compound. Measurement of the surface tension of aqueous solutions over a temperature range of 20–50° showed that there was an inflection point in the relation between cmc and temperature, behaviour typical of an anionic surfactant. As the pH is increased, the interfacial cross-sectional area of the molecule is progressively reduced at the air-water interface, but increased at the hexane-water interface. These results are discussed in terms of the orientation of the molecule at the interface, and the influence of a charged polar head group.
The interaction of Escherichia coli and magnesium trisilicate in aqueous suspension
Authors: Beveridge E G , Todd Kathleen 
Published: April 2011

Abstract
E. coli interacted strongly with magnesium trisilicate particles in buffer solution with aggregation of the particles and ready removal of bacteria from suspension, an equilibrium being attained between adhering and unattached cells. The relation between log10 (uptake bacteria g−1 magnesium trisilicate) and log10 (equilibrium concentration bacteria cm−3) suggested some analogy to the Langmuir type adsorption of solutes. Since both bacteria and particles possessed moderate negative electrical charges of similar magnitude, their interaction is thought to be due to long range additive Van der Waals forces rather than by electrostatic attraction.
Effects of adrenalectomy and of hypophysectomy on the development of sound-withdrawal hypertension
Authors: Marwood J F , Ilett K F , Lockett Mary F 
Published: April 2011

Abstract
Female rats, initially 160–180 g, of a single inbred Wistar strain develop an hypertension reaching peak value at 4 weeks and stabilizing at a slightly lower level by the 6th week after transfer to a sound-proof semi-anechoic room (SPR). Blood corticosterone and deoxycorticosterone levels do not change significantly: urinary catecholamine excretion gradually decreases, and the rates of the urinary excretion of water and of Na+ in the first hour of water diuresis are depressed throughout the first week in the SPR. Adrenalectomy with salt maintenance, and hypophysectomy, prevent the development of this hypertension. Treatment with methyl prednisolone restores the ability of the adrenalectomized, but not of the hypophysectomized, rats to develop sound-withdrawal hypertension.
Metabolism and excretion of diethylpropion in man under acidic urine conditions
Authors: Testa B , Beckett A H 
Published: April 2011

Abstract
After oral administration, diethylpropion is rapidly and extensively metabolized in man by N-de-ethylation and stereoselective carbonyl reduction. The unchanged drug excreted in acidic urine represents about 2% of the dose, while the total metabolites determined account for some 85%. The excretion curves indicate that the probable contribution of the parent compound to the observed activity is small. The major metabolites, together representing about 70% of the dose, are N-ethylaminopropiophenone, (+)-N-diethylnorpseudoephedrine, (+)-N-ethylnorpseudoephedrine, (-)-norephedrine and (-)-norpseudoephedrine. The other stereoisomers of the three amino-alcohols, and aminopropiophenone, are present in minor amounts.
Competitive binding of two drugs for a single binding site on albumin: a circular dichroic study
Authors: Perrin J H , Nelson D A 
Published: April 2011

Abstract
Sulphaethidole has been previously shown to have two classes of binding site on bovine serum albumin (BSA). Only the primary binding site is capable of inducing optical activity in the drug. Drugs that bind to the same primary binding site as sulphaethidole, but do not become optically active themselves on binding, reduce the size of the circular dichroism signal in competitive binding studies with sulphaethidole. The binding constant for such antagonists can be calculated. It appears that a range of acidic drugs share the same primary binding site on bovine serum albumin; basic drugs do not compete for this site.
Adsorption of benzoic acid on sulphadimidine: suppressive effect of some hydrophilic polymers
Authors: Khalil Saleh A H , Nasipuri R N 
Published: April 2011

Abstract
The uptake of benzoic acid on sulphadimidine particles has been investigated. Depending on the concentration of sulphadimidine in the system, benzoic acid was adsorbed to the extent of 94%. Data from the adsorption experiments were shown to fit a Langmuir plot for systems containing up to 0.2 g 100 ml−1 sulphadimidine. The suppressive effect of three hydrophilic polymers on adsorption was studied; the results followed the sequence: Polyvinylpyrrolidone (PVP) &gt; methylcellulose &gt; sodium carboxymethylcellulose. Dialysis experiments revealed that, within the range of concentrations used, neither PVP nor methylcellulose was significantly bound to benzoic acid.
The extraction and estimation of the cannabinoids in Cannabis sativa L. and its products
Authors: Fairbairn J W , Liebmann J A 
Published: April 2011

Abstract
A convenient method for the complete extraction of the cannabinoids from fresh plant material, herbal cannabis, cannabis resin and reefers, has been devised. Chloroform was a more suitable solvent than light petroleum or ethanol and simple shaking of powdered material with the solvent was effective. Fresh material should be air-dried and powdered before extraction. The main cannabinoids in the extract are determined by g.l.c. using androst-4-ene-3,17-dione as internal standard. The coefficient of variation for repeated determinations of THC on a single extract was 1.4%; for all operations, including sampling and extraction, it was 2.7%. Duplicate analyses of 24 samples of herbal cannabis and of 20 reefers, all of varying potency, showed that the errors fell within the expected limits for THC, CBD and CBN. The method is simple and rapid; duplicate determinations can be completed in about 2 1/2 h.
Steryl esters of Digitalis purpurea L. herb
Authors: Evans F J 
Published: April 2011

Abstract
The non-polar fraction sterols of Digitalis purpurea flowering plants were separated into a steryl ester and free sterol fraction. The ester fraction consisted of cycloeucalenol, obtusifoliol, 24-methylenelophenol, 24-ethylenelophenol, cholesterol, campesterol, stigmasterol, sitosterol, isofucosterol and 24-methylenecholesterol. These compounds were esterified with an αβ-unsaturated C10 fatty acid, whereas the glycerides from the same plant consisted of a complex of acids predominated by C18 and C16 types. The free sterols consisted of cycloartenol, 24-methylenecycloartenol, cholesterol, campesterol, stigmasterol, sitosterol, fucosterol and 24-methylenecholesterol. The relative proportions of each of these steroids in the two fractions were recorded.
The oxidation of 6-hydroxydopamine
Authors: Powell W S , Heacock R A 
Published: April 2011

Abstract
The oxidation of 6-hydroxydopamine (I) with molecular oxygen or potassium ferricyanide in aqueous solution has been shown to lead mainly to the formation of the uncyclized quinone 2-(β-aminoethyl)-5-hydroxy-p-benzoquinone (VII). However this quinone cyclized slowly, presumably to norepinochrome (i.e. indoline-5,6-quinone, XII), since 5,6-dihydroxyindole (II), known to be readily formed by rearrangement of norepinochrome (XII), can be isolated from these solutions. 5,6-Dihydroxyindolines (cf. XIII) can also be isolated (as their acetyl derivatives) from the products obtained by the addition of reducing agents to solutions containing 6-hydroxydopamine oxidation products. No evidence was found to suggest that the possible alternative cyclization of the quinone VII to the p-quinonoid aminochrome 6-hydroxyindoline-4,7-quinone (III) occurred to any significant extent.