bluuebunny/crossref_metadata_2025_split huggingface dataset:
Sex and species differences in the biliary excretion of tartrazine and lissamine fast yellow in the rat, guinea-pig and rabbit. The influence of sex hormones on tartrazine excretion in the rat
Authors: BERTAGNI P , HIROM P C , MILLBURN P , OSIYEMI F O , SMITH R L , TURBERT H B , WILLIAMS R T 
Published: April 2011

Abstract
A sex difference in the biliary excretion of tartrazine, which occurs in the rat, has been found not to occur in the guinea-pig and rabbit. Male and female rats excrete 13 and 29% respectively of an intravenous dose of tartrazine (50 μmol/kg) in the bile in 3 h. The corresponding figures for male and female guinea-pigs and rabbits were 33 and 39%, and 5 and 6%, respectively. The sex difference in the rat was unrelated to any differences in renal function, for when the renal pedicles were ligated 22 and 63% of a dose was excreted in the bile of males and females respectively. Treatment of male and female rats with oestradiol and testosterone respectively influenced this sex difference in hepatic function but males were not affected by treatment with progesterone. Thus the extent of biliary excretion of tartrazine in males was increased by oestradiol pretreatment from 14 to 33% of the dose whereas testosterone pretreatment of females decreased excretion from 31 to 16% of the dose. The related dye lissamine fast yellow does not exhibit marked sex or species differences, 75–90% of a dose being excreted in the bile of males and females of all three species. Both dyes are excreted unchanged in the bile and urine of the three species.
The metabolic fate of quinine in rabbits
Authors: WATABE TADASHI , KIYONAGA KAZUE 
Published: April 2011

Abstract
Six metabolites of quinine were detected in the urine of rabbits given its monohydrochloride orally. Of the metabolites detected, three major ones were quantitatively separated and characterized as 2′-hydroxyquinine, 2′,3-dihydroxyquinine, and 2′,6′-dihydroxycinchonidine. No unchanged alkaloid was detected in the urine. The present results indicate that the most important reaction in the metabolism of the alkaloid in the rabbit is the formation of 2′-carbostyril derivatives.
Influence of the electron-donating properties on the psychotropic activity of phenothiazine derivatives
Authors: MERCIER M J , DUMONT P A 
Published: April 2011

Abstract
The electron-donating properties of substituted phenothiazine derivatives and related cyclic compounds have been determined by measuring the maximum of the lowest-energy absorption band of the corresponding charge transfer complexes with tetracyanoethylene and other electron acceptors. Phenothiazine displays a high electron-donating power. The presence and the nature of the side-chain in the 10-position do not significantly influence this property, which is much modified according to the substituent on the 2-position of the ring. The electron donor ability of phenothiazine progressively falls as the Hammet s̀ para constant of this substituent rises. The decrease parallels increase of psychotropic activity. The observations are consistent with the view that an essential part in the mechanism of psychotropic activity of the phenothiazine drugs is played by a positive radical ion.
Effect of micelle formation and the nature of the oil-phase on the distribution of a non-ionic surfactant in three- and four-component emulsions
Authors: MARLAND J S , MULLEY B A 
Published: April 2011

Abstract
As part of an investigation into the mechanisms responsible for the formation and stability of emulsions, the partition of the homogeneous non-ionic surfactant C8H17 [O·CH2·CH2]6OH or C8E6 (E = ethoxy) in the main two-liquid (2L) regions of the three-component systems C8E6–water–dodecane, C8E6–octanol–water and the four-component system C8E6 octanol–water–dodecane has been determined. Cmc and aggregation numbers have been obtained for the surfactant in the different phase regions. The relation of these results to emulsification in the systems is discussed.
Determination of the thermodynamics of the methyl group in solutions of drug molecules
Authors: Davis S S 
Published: April 2011

Abstract
The contribution of the CH3 group to the solution thermodynamics of drug molecules is dependent on whether it is attached to a ring system or is in the terminal position in an aliphatic chain. In the former case group contributions for CH3 are very similar to those found for the CH2 group. For instance, in partition, the CH3 group contribution (log Fch3) is in the range 0.65 to 0.28 (ΔG = 2.303 RT log Fch3) and is dependent on the polarity of the organic solvent. The contribution for the terminal aliphatic CH3 is not equivalent to the mid chain CH2 and a CH3 correction factor or 1.14 to 1.34 kcalmol−1 (4.77 to 5.61 kJmol−1), has been calculated from alkane solubility data and partition studies. The additivity of group contributions and the correct choice of reference state are also discussed.
Effect of additives on the kinetics of interconversion of sulphamethoxydiazine crystal forms
Authors: Ebian A R , Moustafa M A , Khalil Said A , Motawi M M 
Published: April 2011

Abstract
The effect of various additives on the rate of transformation of the more energetic sulphamethoxydiazine Form II to the water-stable Form III in aqueous suspension has been studied. Representative structurally related compounds, viscosity imparting agents, surfactants and colouring agents have been used to inhibit the transformation. Significant transformation retarding effects were observed in most cases. The effects vary, however, from slight retardation to almost complete inhibition of the transformation for periods of over a year (e.g. using 1 % w/v of polyvinylpyrrolidone). The effect of seeding suspensions of Form II with nuclei of Form III in the presence and absence of additives has also been examined. Accelerated stability testing is shown to be inadequate for the prediction of stability of Form II in aqueous suspension in the presence of acacia or polyvinylpyrrolidone. The use of the results in the formulation of dosage forms containing sulphamethoxydiazine is suggested.
Interference of alkanes in the gas chromatographic analysis of cannabis products
Authors: de Zeeuw R A , Wijsbeek J , Malingré Th M 
Published: April 2011

Abstract
Leaves of young marihuana plants (Cannabis sativa L.) were found by gas liquid chromatography to contain appreciable amounts of two long-chain alkanes, n-heptacosane and n-nonacosane. These alkanes, along with other straight chain alkanes ranging from C19 to C32 could also be detected as minor components in a variety of other marihuana and hashish samples. Depending on the polarity of the g.l.c. column used, the alkanes may have retention times similar to those of the major cannabinoids and thus interfere with qualitative and quantitative analyses of the latter. The findings indicate that g.l.c. alone cannot be used as an accurate and reliable technique for cannabinoid analysis, unless the alkanes are previously removed. However, the alkane composition may be of additional advantage in determining the origin of seized cannabis samples.
Evidence for a difference in mechanism of action between fenfluramine- and amphetamine-induced anorexia
Authors: Jespersen Sune , Scheel-Krüger J 
Published: April 2011

Abstract
The influence of drugs, active on 5-hydroxytryptamine (5-HT) mechanisms, has been examined on the anorexigenic activity of fenfluramine and (+)-amphetamine in rats trained to consume their daily food ration during 6 h. Chlorimipramine, which inhibits the re-uptake mechanisms in central 5-HT neurons, and the 5-HT blocking drugs methergoline and methysergide were used. Fenfluramine, 7.5 mg kg−1, and amphetamine, 2.5 mg kg−1, given 1/2 h before feeding reduced the food intake during the following 2 h to approximately 40% compared with control days. Pretreatment with methergoline in the optimal dose (1 mg kg−1) produced only a weak but significant antagonism to amphetamine anorexia, whereas the fenfluramine anorexia was strongly antagonized by methergoline in all doses tested (0.3, 1 and 3 mg kg−1). Methysergide (0.1, 0.3, 1 and 3 mg kg−1) showed no significant antagonism against amphetamine or fenfluramine anorexia. Chlorimipramine produced a strong antagonistic effect to the fenfluramine anorexia, but showed no antagonism against amphetamine. In contrast the highest dose of chlorimipramine (20 mg kg−1) potentiated amphetamine anorexia. The present results together with other evidence discussed support the conclusion that 5-HT mechanisms are involved in fenfluramine anorexia, whereas amphetamine anorexia seems mainly correlated with catecholamine dependent mechanisms.
Drug-induced changes of striatal cholinergic and dopaminergic functions in rats with spreading depression
Authors: Keller H H , Bartholini G , Pletscher A 
Published: April 2011

Abstract
In rats with reversible, functional inactivation of one striatum by spreading depression (SD), dopaminergic stimulation of the intact striatum by Ro 4–4602 plus L-dopa, pargyline plus Ro 4–1284 as well as apomorphine or methamphetamine caused body torsion and rotational movements towards the side of SD. Neuroleptic drugs lead to contralateral body torsion. The apomorphine-induced functional changes were antagonized by the acetylcholine-like drugs arecoline and oxotremorine, but not by nicotine. Atropine, but not methylatropine, blocked the action of arecoline. It is concluded that in the regulation of muscle tone and locomotor activity, a cholinergic system (probably with muscarinic cholinoceptive sites) and a dopaminergic system in the striatum, antagonistic to each other, are involved.
Some actions of 4,17a-dimethyl-4,17a-diaza-D-homo-5α-androstane dimethiodide (HS-342), a new neuromuscular blocking drug
Authors: Marshall I G , Paul Dharami , Singh Harkishan 
Published: April 2011

Abstract
The effects of the newly-synthesized bisquaternary steroid 4,17a-dimethyl-4,17a-diaza-D-homo-5α-androstane dimethiodide (HS-342) have been investigated on the rat isolated phrenic nerve-hemidiaphragm, chick biventer cervicis and intact cat tibialis anterior muscle preparations, on the guinea-pig isolated ileum and on the rat isolated vas deferens preparations. The anticholinesterase activity of HS-342 was also measured. In the skeletal muscle preparations HS-342 exhibited properties of a post-junctionally active neuromuscular blocking agent of the non-depolarizing class. In the anaesthetized cat HS-342 exhibited approximately equal activity to that of tubocurarine, but its duration of action was about one-third of that of tubocurarine. HS-342 exhibited low anticholinesterase activity, low muscarinic blocking activity and apparently had no effect on the adrenergic neuroeffector junction studied.
Pharmacology of diferuloyl methane (curcumin), a non-steroidal anti-inflammatory agent
Authors: Srimal R C , Dhawan B N 
Published: April 2011

Abstract
Some pharmacological actions of curcumin (diferuloyl methane) have been examined in rats, mice and cats. The compound possesses significant anti-inflammatory activity in acute as well as in chronic models of inflammation. It is as potent as phenylbutazone in the carrageenan oedema test but only half as potent in chronic tests. Curcumin possesses a much lower ulcerogenic index than phenylbutazone. It prevents the inflammation induced increase in SGOT and SGPT levels. It lacks analgesic and antipyretic activity. It has no other significant pharmacological effects. The oral LD50 in mice is more than 2&#x006d;̇0 g kg−1.
Micromethod for the determination of bupivacaine in maternal and foetal blood during obstetric analgesia
Authors: Berlin Anita , Persson Bengt-Arne , Belfrage Patrick 
Published: April 2011

Abstract
A method for the determination of bupivacaine in maternal and foetal blood during obstetric analgesia is described. The drug and the internal standard, 1-pentyl-2-(2,6-xylylcarbamoyl)-piperidine, are initially extracted into methylene chloride. Perchloric acid is added to retain bupivacaine and the standard as Perchlorates in the organic phase accomplishing a selective separation from less hydrophobic amines. Bupivacaine and the standard are then re-extracted into sulphuric acid, followed by a purification with methylene chloride. The aqueous extract is finally made alkaline and the compounds extracted into 10 μl methylene chloride. This extract is analysed by gas chromatography using a 3% OV-17 column. The standard deviation of the method at therapeutic concentrations is about 10% and the lowest level which can be determined with reasonable accuracy is 15 ng ml−1.
Release of dipicolinic acid and calcium and activation of Bacillus stearothermophilus spores as a function of time, temperature and pH
Authors: Brown M R W , Melling J 
Published: April 2011

Abstract
The kinetics of release of dipicolinic acid and calcium from Bacillus stearothermophilus spores and the rate of increase of colony count have been shown to be determined by conditions of time, temperature and pH. The apparent activation energies for release of dipicolinic acid, calcium and colony count increase were similar. The results support the hypothesis that breaking of dormancy involves a rupture of dipicolinic acid bonds and that the nature of these bonds rather than the dipicolinic acid content determines dormancy and resistance.
The ganglion blocking and vagolytic actions of three short-acting neuromuscular blocking drugs in the cat
Authors: Marshall I G 
Published: April 2011

Abstract
Three recently-introduced short-acting neuromuscular blocking drugs with non-depolarizing mechanisms of action, stercuronium, dacuronium and AH8165 (1,1′-azobis [3-methyl-2-phenyl-1H-imidazo (1, 2a) pyridinium] dibromide) have been tested in the anaesthetized cat on the responses of the nictitating membrane to stimulation of the cervical nerve, and of the heart to vagal stimulation. The effects of the three drugs at the superior cervical ganglion and at the cardiac neuroeffector junction have been compared with their neuromuscular blocking effects. At doses lower than those required to block neuromuscular transmission all three compounds possessed a selective atropine-like action at the cardiac vagus neuroeffector junction in that they inhibited the bradycardia produced by vagal stimulation and by acetyl-β-methylcholine, whilst the depressor action of acetyl-β-methylcholine was unaffected. The ratios of the doses of the drugs to block the responses of the preganglionically-stimulated nictitating membrane and of the tibialis anterior muscle were 16&#x006d;̇7 for stercuronium, 8&#x006d;̇5 for dacuronium and 3&#x006d;̇8 for AH8165. The greater ganglion-blocking activity of AH8165 was reflected in the depressor action of the compound, whereas the weak ganglion-blocking actions of stercuronium and dacuronium were insufficient to mask the tachycardia and pressor effect caused by their blocking action on the cardiac vagus neuroeffector junction.
The recovery of bacteria from white soft paraffin
Authors: Allwood M C , Hambleton R 
Published: April 2011

Abstract
Methods have been investigated for isolating and enumerating, by a membrane filtration technique, E. coli inoculated into white soft paraffin. Of three solvents used to prepare the ointment base for filtration, the best recovery (54%) was obtained with light liquid paraffin. Superior recovery levels (ca 75%) were obtained by homogenizing the ointment base with a Tween 80/peptone water mixture. Recovery levels were greatly affected by the weight of ointment base taken but the Tween 80/peptone water system permitted the estimation of the contamination in up to 0&#x006d;̇25 g of white soft paraffin.
Total and free-plasma tryptophan concentrations in rheumatoid disease
Authors: Aylward Mansel , Maddock Jeffrey 
Published: April 2011

Abstract
It has been proposed (McArthur, Dawkins & others, 1971) that human connective tissue diseases may arise from modifications in the binding characteristics of the plasma proteins. McArthur, Smith & Freeman (1972) presented evidence that human serum contains a substance that possesses anti-inflammatory activity and is bound to circulating proteins. Furthermore, it has been suggested that, in patients with active rheumatoid arthritis, the anti-inflammatory substance is bound to an abnormal extent to the plasma proteins and that the clinically useful antirheumatic drugs act by re-establishing the bound: free ratio to that in the normal subject (Smith & Dawkins, 1971). There is evidence that the behaviour of L-tryptophan mimics that of the hypothetical substance which protects susceptible tissues against chronic inflammatory insults. All the clinically useful antirheumatic agents were found to displace L-tryptophan from human plasma in vitro (McArthur, Dawkins & Smith, 1971) but not so other drugs which bind to plasma proteins to an equivalent extent but have no demonstrable antirheumatic effects (Smith, Dawkins & McArthur, 1971). In patients with rheumatoid arthritis receiving drug therapy the percentage of L-tryptophan bound to plasma proteins is significantly reduced but increases when drug administration is stopped (McArthur, Dawkins & others, 1971).
A note on the solubilization of preservative mixtures by cetomacrogol
Authors: Crooks M J , Brown K F 
Published: April 2011

Abstract
Preliminary data are reported for the solubilization of several pairs of preservatives by the non-ionic surfactant cetomacrogol. In all cases the addition of a second preservative altered the equilibrium solubility of the first to an extent which depended on the particular co-solute and the concentration added.
Use of substituent constants in structure-activity relations and the importance of the choice of standard state
Authors: Davis Stanley S 
Published: April 2011

Abstract
The value of the hydrophobic group substituent constant (π), calculated from logarithms of partition coefficients, is normally independent of the choice of the standard state used for the partition studies. However, in some cases e.g. when a partition coefficient for the intact molecule is taken as being equivalent to a π value, the choice of standard state is of utmost importance. It is suggested that π values may be additive on the mole fraction (thermodynamic partition coefficient) scale and not the molar scale as has been previously assumed. Consequently, some published π values may be in error.
The excitation of neurons by noradrenaline
Authors: Bevan P , Bradshaw C M , Roberts M H T , Szabadi E 
Published: April 2011

Abstract
Responses of single cortical neurons to microelectrophoretically applied noradrenaline at pH 3.1 and 5.0 and to hydrogen ions were compared in the halothane-anaesthetized cat. Of 16 neurons sensitive to noradrenaline, 13 were excited and 3 were depressed by noradrenaline at both pH values, whereas hydrogen ions released from an HCl solution did not affect the firing rate. Dose-response studies showed that noradrenaline at pH 3.1 was more potent than at pH 5.0. It is concluded that excitatory responses to noradrenaline are not artifacts and that the adjustment of the pH of noradrenaline solutions with NaOH should be avoided.
Gas chromatographic determination of ethosuximide and phensuximide in plasma and urine of man
Authors: van der Kleijn Eppo , Collste Per , Norlander Björn , Agurell Stig , Sjöqvist Folke 
Published: April 2011

Abstract
Ethosuximide and phensuximide in plasma and urine can be assayed to a concentration of 2–5 μg ml−1 by a rapid and specific gas chromatographic assay. The method can be used to monitor plasma concentrations in patients with petit mal treated with these drugs alone or in combination with other antiepileptic drugs. The steady-state plasma concentrations of ethosuximide in children given 10–45 mg kg−1 day−1 varied between 10 and 150 μg ml−1 indicating marked interindividual differences in pharmacokinetics.
The identification, properties and analysis of N-hydroxyamphetamine—a metabolite of amphetamine
Authors: Beckett A H , Al-Sarraj S 
Published: April 2011

Abstract
N-Hydroxyamphetamine (Ib) can be extracted from aqueous solutions at neutral pH, but is readily decomposed into syn- and anti-phenylacetone oximes (II) at alkaline pH values. Gas chromatography of Ib is possible, provided the compound does not come into contact with heated metal surfaces. In aqueous media the hydroxylamine can be determined (1) by extraction from the medium with ether and analysis of the ethereal solution by g.l.c.; (2) by separation of the compound on a thin-layer then oxidation of the hydroxylamine spot with ammoniacal silver nitrate to give phenylacetone oximes which may then be determined by g.l.c.; (3) by reduction with lithium aluminium hydride to amphetamine (Ia) followed by g.l.c.; (4) conversion to phenylacetone oximes by shaking at pH 12 in air, extraction of the oximes, followed by g.l.c.; (5) Alternatively, N-hydroxyamphetamine can be determined directly in aqueous solution by polarography provided the measurement is made immediately after the supporting electrolyte, sulphite/NaOH, has been added.
The central and peripheral activities of anti-acetylcholine drugs. Some concepts of practical relevance
Authors: Inch T D , Green D M , Thompson Pamela B J 
Published: April 2011

Abstract
Five procedures have been used to compare the pharmacological effects and time-activity profiles of anti-acetylcholine drugs in the central and peripheral nervous system (ens, pns). In particular, the potencies of optically pure enantiomers of anti-acetylcholine drugs which contain an asymmetric centre have been determined. The following four observations are made which are of relevance to all studies of anti-acetylcholine drugs. (1) Times to onset of activity of anti-acetylcholine drugs in three in vivo tests and the duration of action in one in vivo test are shown to increase as affinity constants, determined in vitro, increase. (2) Below a dose of ca 0.03 μmol kg−1no anti-acetylcholine drug produces maximum mydriatic effects and all anti-acetylcholine drugs which have log affinity constant values &gt;9.49 produce maximal effects at approximately this dose. (3) The receptor with which anti-acetylcholine drugs interact is essentially the same in the eye, salivary gland and ens of the mouse, the guinea-pig ileum, and in the cat ens. (4) For any anti-acetylcholine drug the time to onset of effects in the ens is similar to the time of onset of effects in the pns and appears to depend on the affinity constant rather than on the partition properties of the drug. The practical and theoretical significance of these and other observations are discussed.