bluuebunny/crossref_metadata_2025_split huggingface dataset:
Metabolism and excretion of promazine by the horse
Authors: Weir J J , Sanford J 
Published: April 2011

Abstract
The urinary excretion of promazine and its metabolites has been examined in five horses, by ultraviolet spectrometry and thin-layer chromatography. In each horse, excretion continued for at least 96 h although the amount excreted was low, being about 11% of the dose. No correlation of excretion and pH or urinary volume was observed. Glucuronic acid conjugates predominated, their ratio to unconjugated metabolites being about 5:1. Promazine was found only in small amounts and traces of unconjugated sulphide metabolites were found in only one horse. At least nine metabolites of promazine were detected, the major one being the glucuronide of 3-hydroxypromazine.
The pharmacology of 5-(2-t-butylamino-1-hydroxyethyl) salicylamide (AH 3474), a β-adrenoreceptor blocking agent
Authors: Blackburn C H , Byrne L J , Cullum V A , Farmer J B , Levy G P 
Published: April 2011

Abstract
AH 3474 is a specific β-adrenoreceptor antagonist, devoid of stimulant activity. When given by mouth to conscious guinea-pigs and dogs, AH3474 and propranolol are equiactive in antagonizing isoprenaline-induced tachycardia. In anaesthetized animals AH 3474 was 2–4 times less active than propranolol when given intravenously. A similar potency ratio was found in volunteer studies in which the drug was taken orally. On isolated tissues AH 3474 was much less active than propranolol. AH 3474 had 1/10th the activity of propranolol in blocking the inhibitory action of isoprenaline on the rat uterus and was at least 100 times less active in antagonizing the tachycardia induced by adrenaline on the guinea-pig atria. In vitro, equilibrium conditions for AH 3474 were obtained in 15 min, whereas 45 min were required for propranolol. AH 3474 antagonized the cardiac arrhythmias induced by ouabain in the anaesthetized dog. The amount required far exceeded the β-adrenoreceptor blocking dose. AH 3474 possessed no “quinidine-like” actions on cardiac muscle of dog or guinea-pig. The local anaesthetic activity of AH 3474 was 400 times less than that of propranolol.
Comparison of intracisternally and intraperitoneally injected harmaline on body temperature and tremor in the rat
Authors: Bruinvels J 
Published: April 2011

Abstract
Low doses of harmaline (1–10 mg/kg) injected intraperitoneally into rats caused hypothermia, while higher doses (10–30 mg/kg) induced tremor in addition to hypothermia. Harmaline injected intracisternally decreased body temperature without inducing tremor. To induce a maximal fall in body temperature following intraperitoneal injection of harmaline, 1000 times more harmaline was needed than after intracisternal administration. Harmaline by this route induced hypothermia much faster than by intraperitoneal injection. It is concluded that harmaline-induced hypothermia is at least partly localized in the central nervous system and is not associated with the tremor.
The effect of two synthetic steroids on the ultrastructure of the liver of Rattus norvegicus L.
Authors: Hines W J W 
Published: April 2011

Abstract
Flumedroxone acetate and an analogue [17-acetoxy-3β(β-carboxypropionyloxy)-6-trifluoromethylpregn-5-ene-20-one] each produce a liver weight increase and a change in hepatic cell ultrastructure, following chronic administration in mice and rats. In all liver cells there is much proliferation of the smooth endoplasmic reticulum, which arises from the ergastoplasm, or rough membranes. An effect on esterase enzyme specificity and the evidence for the induction of an esterase isoenzyme after treatment with these steroids, is referred to. The distribution of the new smooth endoplasmic reticulum is of interest as it varies with each analogue.
A note on the colorimetric determination of butyrophenones with 3,5-dinitrobenzoic acid
Authors: Haemers A , Van Den Bossche W 
Published: April 2011

Abstract
Butyrophenones react with 3,5-dinitrobenzoic acid in an alkaline medium with the formation of a red coloured complex. This reaction can be used for the quantitative determination of these drugs in pharmaceutical preparations. The influence of the ethanol concentration, the alkalinity and the reagent concentration was investigated separately. The results show that the proposed method is suitable for the assay of solutions and tablets. It requires less time than existing methods.
The in vitro and in vivo metabolism of optically active methylcyclohexanols and methylcyclohexanones
Authors: Elliott T H , Jacob E , Tao Rosaline C C 
Published: April 2011

Abstract
The in vitro reduction and oxidation of the isomeric methylcyclohexanones and methylcyclohexanols by horse liver alcohol dehydrogenase, in the presence of NADH2 or NAD has been studied. The enzymic reactions closely resemble the corresponding in vivo metabolic conversions and support the view that the oxido-reductase in the animal body is similar to liver alcohol dehydrogenase. The findings are discussed in terms of the conformations of the alcohols and ketones and a correlation of the observed rates, Km values, and the steric specificity supports the view that the in vivo inversion of the thermodynamically less stable alcohols (±)-cis-2-, (±)-trans-3-, and cis-4-methylcyclohexanol could occur through a ketone intermediate.
The effects of 1-[di(2-chloroethyl)aminomethyl]benzimidazole and related compounds on the growth of experimental tumours
Authors: Reddy V V Subba , Sirsi M , Revankar G R , Siddappa S 
Published: April 2011

Abstract
The inhibitory activity of some benzimidazole Mannich-base nitrogen mustards on the growth of experimental tumours, viz. mouse fibrosarcoma in mice and Yoshida ascites sarcoma in rats has been examined. Amongst the compounds tested 5,6-dichloro-1-[di(2-chloroethyl)aminomethyl]benzimidazole and 1-[di(2-chloroethyl)-aminomethyl]-2-phenylbenzimidazole showed inhibitory effect on mouse fibrosarcoma; while 4-bromo-1-[di(2-chloroethyl)aminomethyl]benzimidazole, 4-chloro-1-[di(2-chloroethyl)aminomethyl]-benzimidazole and 1-[di(2-chloroethyl)aminomethyl]-5-methoxybenzimidazole were active against Yoshida ascites sarcoma.
The evaluation of inflammation induced by material implanted subcutaneously in the rat
Authors: Hicks R 
Published: April 2011

Abstract
Inflammation induced by cotton pellets, implanted subcutaneously in the rat, has been compared with that resulting from implantation of pellets impregnated with irritant substances. Time sequences of fluid exudation and granulation tissue formation have been evaluated by differential weighing. Increased irritancy of the pellets resulted in increased exudate volume, and heavier granulation deposition. Contact between granulation tissue and irritant pellets was delayed until the volume of exudate had subsided. Penetration of the pellet was also delayed. Systemic anti-inflammatory effects from granulomata surrounding implanted pellets were related to either the size of the implantation lesion or the degree of irritancy of the implanted material. Evaluation of granulation tissue formation is suggested as a test for irritancy of surgical fabrics.
The effect of ultrasonic energy on the extraction of anthraquinones from senna pericarps
Authors: Woodford R , Morrison J C 
Published: April 2011

Abstract
Ultrasonic irradiation increased the extraction rate of rhein glycosides, free anthraquinones and total water-soluble solids from whole senna pericarps, irrespective of the temperature conditions employed. An increase in ultrasonic power from 35 to 100 W increased the yield of extractable constituents over a 15 min period, the ratio of rhein glycosides to total water-soluble solids being higher in extracts prepared using ultrasound than in preparations obtained by simple maceration, but that ratio decreased slightly with an increase in ultrasonic power. Ultrasonic irradiation produced occasional visible damage to epidermal cell walls and the significance of this in the extraction of senna pericarps is discussed.
The diffusion of sennoside A through a cellulose membrane
Authors: Woodford R , Morrison J C 
Published: April 2011

Abstract
The diffusion rate of sennoside A through a cellulose membrane into water increased irrespective of the temperature conditions under which diffusion took place, when the membrane was irradiated with ultrasound. The results are consistent with the hypothesis of boundary layer disruption at the phase interface and their significance in the effect of ultrasonic energy on the aqueous extraction of senna pericarps is discussed.
Calibration and application of high torques to a reaction air turbine viscometer
Authors: Barry B W , Saunders G M 
Published: April 2011

Abstract
A reaction air turbine viscometer has been calibrated with the air bearing placed both horizontally and vertically. It has been shown that changing the position of the bearing varied the result by less than 2%. The air bearing pulley employed in the calibration is described; this may also be used to apply high torques during a rheological analysis.
Quantitative analysis of 4‘-chloro-2-ethylaminopropiophenone, 4’-chloro-2-amino-propiophenone and the corresponding aminoalcohols in a mixture of the four compounds
Authors: Beckett A H , Hossie R D 
Published: April 2011

Abstract
A method specific for the quantitative analysis of 4′-chloro-2-ethyl-aminopropiophenone, and 4′-chloro-2-aminopropiophenone in the presence of their corresponding aminoalcohols in urine is described. The instability of the aminoketones makes extraction from alkaline solutions impractical. Hence they are quantitatively reduced to their corresponding alcohols and analysed using gas-liquid chromatography.
The relation between circulating and tissue concentrations of salicylate in the mouse in vivo
Authors: McArthur J N , Dawkins P D , Smith M J H 
Published: April 2011

Abstract
The blood and water contents of mouse liver, brain, kidney, heart, spleen and skeletal muscle were measured and used to correct observed values for the salicylate concentrations in these tissues after the intraperitoneal injection of the drug. The binding of salicylate in vitro to mouse whole blood, liver, kidney and brain was studied. It was concluded that blood, liver and kidney but not the other tissues, bind the drug in vivo.
The effect of acute adrenalectomy on the blood pressure responses to noradrenaline and to preganglionic nerve stimulation
Authors: Drew G M , Leach G D H 
Published: April 2011

Abstract
The quantitative contribution of the adrenal medulla to the pressor response resulting from stimulation of the entire preganglionic sympathetic spinal outflow of the rat, has been estimated. Adrenalectomy reduced the pressor responses not only to preganglionic nerve stimulation but also to injected noradrenaline. This reduction in cardiovascular sensitivity occurred within about 10 min of adrenalectomy and continued throughout the course of each experiment. Intramuscular injection of cortisone (20 mg/kg) restored cardiovascular sensitivity to injected noradrenaline thus allowing analysis of the adrenal medullary component of the overall response to spinal nerve stimulation.
The isolated perfused heart preparation: two suggested improvements
Authors: Beckett P R 
Published: April 2011

Abstract
A new method of recording the contractions of the isolated perfused heart is described. By “transverse” recording, a signal of simple waveform is obtained from the right ventricle at constant diastolic tension. Changes in heart rate and force of contraction of the rat isolated perfused heart caused by (-)-noradrenaline were measured. Of the three methods of assessing the response: (1) the increment as a percentage of the control record, (2) the increment in absolute units and (3) the increment as a percentage of the maximum, the latter has most pharmacological meaning.
The synthesis and anti-acetylcholinesterase activities of (+)-physostigmine and (+)-physovenine
Authors: Dale F J , Robinson B 
Published: April 2011

Abstract
(+)-Physostigmine and (+)-physovenine have been synthesized. The anti-acetylcholinesterase activities of these two bases, which have been investigated in vitro using erythrocyte acetylcholinesterase, have been found to be much lower than the corresponding activities of the alkaloids (-)-physostigmine and (-)-physovenine. Possible reasons for these activity differences are discussed.
The stabilization-lysis action of anti-inflammatory steroids on lysosomes
Authors: Lewis D A , Symons A M , Ancill R J 
Published: April 2011

Abstract
The effect of anti-inflammatory steroids on lysosomal enzyme release has been investigated. Most of the steroids stabilized lysosomes at pharmacological concentrations (10−4–10−6M) but lysed them at higher concentrations. Etiocholanolone, a steroid pyrogenic in man, had no stabilizing effect. The concentration of steroid would therefore seem critical in determining its subcellular action. Experiments with albumin suggest that anti-inflammatory steroids (at 5 × 10−4M) have little effect in aiding its thermal denaturation whereas other steroids greatly increase denaturation. Increasing concentrations of cortisol and prednisolone however caused greater denaturation of albumin. Although the correlation between albumin solutions and lysosomal membrane proteins is tenuous it is suggested that the lytic effect of anti-inflammatory steroids could be due to protein denaturation. Their stabilizing effect, however, probably involves steroidlipid interactions.
The actions of some non-steroidal drugs on lysosomes
Authors: Lewis D A 
Published: April 2011

Abstract
Several non-steroidal acidic anti-inflammatory drugs had a lytic action on lysosomes at high concentrations but no apparant action at lower concentrations. The drugs also inhibited acid phosphatase activity but only at high concentrations. High concentrations of drugs accelerated the thermal denaturation of albumin solutions but partially protected the albumin against denaturation at lower concentrations. The possibility that the denaturing action of drugs on proteins at high concentrations is related to lysosomal damage and that this damage may be associated with ulceration in vivo is discussed. Salicylate was found to inhibit the stabilizing action of cortisol on lysosomes.
Formulation and pharmacological studies of a controlled release pentagastrin injection
Authors: Wai K N , Gerring E E L , Broad R D 
Published: April 2011

Abstract
Four formulations were designed to release pentagastrin at different rates after subcutaneous injection. These formulations were tested in vitro for rate of diffusion across a dialysis membrane into pH 7·3 phosphate buffer, and in vivo in rats for rate of excretion in the bile and on dogs for pharmacological responses. Good agreement was observed between the in vitro data, elimination rate and dose response data for the rate of release and duration of action of the four formulations. The results agreed with the theory that by controlling the rate of release of a short acting drug, one could sustain the pharmacological response to the drug and increase the total response by better utilization of an administered dose.
Preparation of active, drug-metabolizing, microsomal enzymes under optimal conditions and by iso-electric precipitation
Authors: Mitchard M 
Published: April 2011

Abstract
The influences of homogenization technique and of relative centrifugal force on the enzyme activity of hepatic microsomes have been investigated to establish optimal conditions for preparation. In general, a glass or Ultra Turrax homogenizer provided a satisfactory homogenate having maximal enzyme activity when nuclear and mitochondrial material were removed by centrifugation at &gt;6500 g for 20 min. Esterase, UDP-transglucuronylase, reductase and oxidase activities of microsomes prepared from liver breis under optimal conditions from guinea-pig, rabbit and rat have been compared. The enzyme activities in microsomes prepared by isoelectric precipitation at pH 5·0 were similar to those prepared by differential centrifugation except for a 50–75% reduction in glucuronyl transferase activity observed in rabbit and guinea-pig.
The relation between the uptake of cetyltri-methylammonium bromide by Escherichia coli and its effects on cell/growth and viability
Authors: Salt W G , Wiseman David 
Published: April 2011

Abstract
The effects of CTAB uptake on cells of E. coli have been examined in terms of growth inhibition and decrease in cell viability. Different thresholds of CTAB uptake exist below which no effect on cell growth or viability could be detected and there was a distinct separation of the two effects. It is suggested that both reflect all or none responses by individual cells. A mechanism for the mode of antibacterial action of CTAB against E. coli is postulated.
A test for the assessment of the duration of the action of neostigmine and of the relative potencies of various anticholinesterases using the pupil of the mouse
Authors: Schneider R 
Published: April 2011

Abstract
The miotic effect of anticholinesterases was used to monitor the duration of their activity and to compare the relative potency of different members of this group. Female albino mice were used and the diameter of their pupils measured with the help of a monocular microscope at a magnification of × 60. After a suitable control period, readings were taken at 30 min intervals. This test was found to be superior to previous tests described for the same purpose.
Infrared identification of some hallucinogenic derivatives of tryptamine and amphetamine
Authors: Mesley R J , Evans W H 
Published: April 2011

Abstract
The use of infrared spectroscopy for the identification of psychotomimetic derivatives of amphetamine and tryptamine is discussed. Numerous characteristic absorptions are assigned on the basis of spectra recorded from 123 bases and salts. These permit the recognition of compounds of these types even when no reference materials or spectra are available. Distinction between the spectra of optically active and racemic forms of some amphetamine derivatives is also possible.
Some observations on the use of fatty alcohols and fatty acids to increase the consistency of oil-in-water emulsions
Authors: Talman F A J , Rowan Miss E M 
Published: April 2011

Abstract
A range of fatty alcohols and fatty acids of different chain lengths and chemical configuration has been examined to determine which of these may be usefully employed to increase the consistency of liquid paraffin-in-water emulsions stabilized by condensed complex films. Of the alcohols, a straight chain of 16 carbon atoms (cetyl alcohol) or a physical mixture of straight chains of 16 and 18 carbon atoms (cetostearyl alcohol) gave maximum bodying action. To a lesser extent a straight chain of 14 carbon atoms (myristyl alcohol) and in some cases a straight chain of 12 carbon atoms (lauryl alcohol) also increased the consistency of emulsions. Other homologues (C8, C10 and C18), unsaturated or branched chain alcohols and fatty acids were, in general, found to be of little value for this purpose.
A comparison of the effects of 6-hydroxy-dopamine immunosympathectomy and reserpine on the cardiovascular reactivity in the rat
Authors: Finch L , Leach G D H 
Published: April 2011

Abstract
In the conscious rat, 6-hydroxydopamine, or reserpine (5 mg/kg) pretreatment produced a marked fall in the mean systolic blood pressure whilst immunosympathectomized rats had resting blood pressures just below that of control animals. In pithed preparations, 6-hydroxydopamine treatment or immunosympathectomy potentiated the pressor responses to injected noradrenaline; reserpine pretreatment did not potentiate the noradrenaline response to the same degree. Tyramine responses were abolished after 6-hydroxydopamine or reserpine pretreatment but were unaffected by immunosympathectomy. Stimulation of the sympathetic outflow by the Gillespie & Muir (1967) preparation was abolished after 6-hydroxydopamine and reserpine pretreatment, and reduced after immunosympathectomy. It is concluded that 6-hydroxydopamine produces a destruction of the sympathetic nerve endings, abolishing the physiological uptake process and, therefore, producing supersensitivity to injected noradrenaline. Immunosympathectomy, although showing a marked reduction in sympathetic nerve supply leaves a functional uptake process. Reserpine (5 mg/kg), given 6 h previously, depletes endogenous catecholamines without significantly altering the sensitivity to injected noradrenaline, the uptake process remaining functional.
Potentiation of oxotremorine lethality by antihistamines
Authors: Gerald Michael C , Maickel Roger P 
Published: April 2011

Abstract
Antihistamines, representing the major chemical classes, administered intraperitoneally to mice in non-toxic doses potentiated the lethal effects of an LD10 dose (3·5 mg/kg) of oxotremorine in a dose related manner. Atropine and methylatropine were highly effective in blocking oxotremorine lethality alone and when it was potentiated by antihistamines. The antagonism by methylatropine suggests a peripheral site of toxicity. Antihistamines might enhance lethality by interfering with the inactivation of oxotremorine by liver microsomal drugs enzymes in a manner similar to SKF 525A.
Colorimetric determination of amphetamine salts in dosage forms
Authors: Fontani Febo , Morandini Franco 
Published: April 2011

Abstract
A colorimetric method for the determination of primary amines has been applied to the assay of amphetamine salts in dosage forms. Aqueous solutions of amphetamine salts heated in acidic medium with 2,5-dimethoxytetrahydrofuran and subsequently reacted with p-(dimethylamino)benzaldehyde, give a red colour. This reaction is useful for photometric determinations at 557 nm. Secondary and tertiary amines do not interfere.
The determination of sodium aminosalicylate in cachets of sodium aminosalicylate and isoniazid by ultraviolet absorption
Authors: Clough D 
Published: April 2011

Abstract
Sodium aminosalicylate can be determined in the presence of isoniazid by its ultraviolet absorption at 299 nm. The method is at least as accurate as the B.P.C. 1968 bromination method for cachets of sodium aminosalicylate and isoniazid. Analysis of a powder mix containing sodium aminosalicylate (2 g) and isoniazid (50 mg) gave a mean value of 2.02 ± 0.01 (s.d.) for ten determinations using the proposed method. The B.P.C. method gave a mean value of 2.03 ± 0.33 (s.d.). The proposed method has the advantage that the determination is independent of the isoniazid content and is more rapid than the official method. It can be easily adapted for automatic analysis.
Acid gastric secretory responses to histamine, crude porcine gastrin and pentagastrin in rats
Authors: Amure B O , Omole A A 
Published: April 2011

Abstract
The log dose-response curves for graded doses of the secretagogues porcine gastrin (a partially purified sample; the crude and its gastrin II equivalent), histamine, and a gastrin pentapeptide (pentagastrin) on the perfused stomachs of urethanized rats are parallel. On weight basis, pentagastrin is 60 times and histamine four times more active than the crude porcine gastrin preparation. The partially purified porcine gastrin sample is six times more potent than histamine but half as potent as pentagastrin. On molar basis gastrin (as the pure porcine gastrin II) has 3000 times the activity of histamine dihydrochloride and 5000 times that of the histamine base. Gastrin is 50 times more potent than pentagastrin. Gastrin and pentagastrin are more potent and have less undesirable side-effects than histamine.