bluuebunny/crossref_metadata_2025_split huggingface dataset:
The effect of SC-15396, atropine and mepyramine on gastrin-, bethanechol- and histamine-stimulated gastric acid secretion in rats and guinea-pigs
Authors: Albinus Margitta , Sewing K-Fr 
Published: April 2011

Abstract
The effect of SC-15396 (“antigastrin”; 2-phenyl-2-(2-pyridyl)thioacetamide), atropine and mepyramine on gastrin-, bethanechol- and histamine-stimulated gastric acid secretion was studied in rats and guinea-pigs. For all three stimulants parallel dose response curves were obtained except in guinea-pigs where bethanechol even in very high doses displays a poor activity in stimulating gastric acid secretion. The maximal secretory response was found to be 12·7 ± 5·0 μ-equiv HCl/10 min in rats and 53·2 ± 27£9 μ-equiv HCl/10 min in guinea-pigs. All stimulating effects on gastric acid secretion were reduced by SC-15396; atropine abolished the secretory responses to bethanechol. Mepyramine was ineffective. In accordance with these findings the mechanism of action of gastrin and a receptor model on the oxyntic cell are discussed.
The actions of atropine, tropenziline and N-butyl hyoscine bromide on the isolated distal colon of the guinea-pig: a comparison of their activities and mechanisms of action
Authors: Lecchini S , Del Tacca M , Soldani G , Frigo G M , Crema A 
Published: April 2011

Abstract
In the guinea-pig isolated distal colon, the order of anticholinergic activity is as follows: atropine &gt; tropenziline bromide &gt; N-butyl hyoscine bromide. The reduction in the responses to pelvic and transmural stimulation produced by tropenziline and N-butyl hyoscine bromide is due partly to their ganglion blocking activity. This effect also explains the reduction they cause in acetylcholine output on pelvic nerve and transmural stimulation. Since atropine also reduces acetylcholine release on pelvic nerve stimulation, it is suggested that muscarinic receptors of the parasympathetic ganglia are involved in transmission of pelvic nerve impulses.
Gas chromatographic identification of thioridazine in plasma, and a method for routine assay of the drug
Authors: Curry S H , Mould G P 
Published: April 2011

Abstract
Thioridazine had a retention time of approximately 4 min on a 3% OV-17 gas chromatographic column at 260°. Using flame or argon ionization detectors samples as low as 0μ01 μg could be detected. The drug could be extracted into n-heptane containing 1·5% isoamyl alcohol or 20% toluene. Recovery of drug added to plasma was 100%. Unchanged thioridazine was identified in the plasma of two experimental samples, on the basis of chromatographic and solvent distribution data.
Identification of a urinary metabolite of perazine as a piperazine-2,5-dione derivative
Authors: Krauss Dietlinde , Otting Walter , Breyer Ursula 
Published: April 2011

Abstract
A non-basic perazine metabolite has been isolated from the urine of schizophrenic patients ingesting perazine. Identification of this compound as 10-[3‘-(2“,5”-dioxo-4“-methyl-piperazinyl)-propyl]-phenothiazine sulphoxide was achieved using ultraviolet, infrared, nuclear magnetic resonance and mass spectroscopy.
The effects of etorphine and of morphine on respiration, blood carbon dioxide tension, and carbon dioxide sensitivity in the conscious rabbit
Authors: Pleuvry Barbara J , Rees J M H 
Published: April 2011

Abstract
The effects of intravenous doses of morphine and etorphine on respiration, blood pCO2 and sensitivity to carbon dioxide were investigated in the conscious rabbit. Both morphine and etorphine depressed respiratory rate and elevated pCO2. Etorphine was about 5000 times more potent than morphine as a depressant of respiratory rate. With etorphine, depression of respiratory rate was always accompanied by a large increase in tidal volume. In the normal rabbit, inhalation of mixtures of carbon dioxide up to 15% (in oxygen) produced a concentration-dependent increase in tidal volume accompanied by no increase in respiratory rate. After injection of morphine followed by inhalation of carbon dioxide there was a dose-dependent depression of carbon dioxide sensitivity which was concurrent with the depression of respiratory rate; 8 mg/kg completely abolished the respiratory stimulant effects of concentrations of carbon dioxide up to 12%. Whilst high doses of etorphine depressed carbon dioxide sensitivity, a dose of 0·5 μg/kg (which depressed respiratory rate by about 30%) did not depress carbon dioxide sensitivity. Doses of 1 μg/kg of etorphine administered to pregnant animals produced an increase in respiratory rate and a depression of tidal volume. The significance of the differences between the respiratory pharmacology of etorphine and that of morphine is discussed.
The determination of cellulase activity by viscometry
Authors: Joos P , Sierens W , Ruyssen R 
Published: April 2011

Abstract
The enzymatic activity of cellulase has been estimated by the decrease of viscosity of a hydroxyethylcellulose solution as a function of incubation time. This decrease is a function of the applied shear stress. It is proposed that the viscosity be measured in an ordinary Ostwald viscometer under conditions where the viscosity is Newtonian, that is, the decrease of viscosity by enzymatic activity is independent on the shear stress.
Dissolution rates of sparingly soluble tablets
Authors: Hersey J A , Barzilay R B 
Published: April 2011

Abstract
The automated dialysis method offers an opportunity for the accurate evaluation of the dissolution rates of sparingly soluble dosage forms. By the analysis of kinetic models, the dissolution rates for disintegrating and non-disintegrating dosage forms may be calculated. The theory is used to examine the effect of additives and compression force on the dissolution rates of sulphathiazole tablets. At the fairly low compression forces used (640–1430 kg) the dissolution rate gradually increases due to penetration of the tablet by the dissolution medium. Polyethylene oxide causes an initial rapid increase in dissolution rate, but the formation of a mucilaginous film results in a constant rate. Using starch, dissolution rate increases rapidly as a result of tablet disintegration. This disintegration is shown to make available less than half the surface area of the original powder. The dissolution rate constant for sulphathiazole under the experimental conditions is 2–75 × 10−4 cm min−1.
Stabilization of oil-in-water emulsions by non-ionic detergents: properties of synthetic detergents at anisole- and chlorobenzene-water surfaces
Authors: Elworthy P H , Florence A T 
Published: April 2011

Abstract
As part of an investigation into the mechanisms of stabilization of emulsions, the interfacial activity of three synthetic non-ionic detergents, CH2·[CH2]15·[O·CH2·CH2·]xOH, with x = 3, 6 and 9, at the anisole-water and chlorobenzene-water interface has been determined by measurement of interfacial tension. Surface pressure (π)-area (A) relations have been derived. The films are more expanded than at the air-water interface and an equation of the form (π- πR)A = xkT fits the results. It is suggested tentatively that πR, which is in most cases positive, and which increases with polyoxyethylene chain length, arises from the interaction between the ethylene oxide chains as they approach closely. The apparent critical micelle concentrations determined from the interfacial tension-concentration curves are higher than the true critical micelle concentrations obtained at the air-water interface.
Adrenergic receptors in the guinea-pig trachea
Authors: Everitt B J , Cairncross K D 
Published: April 2011

Abstract
The effects of adrenaline, noradrenaline and isoprenaline have been investigated on the guinea-pig isolated trachea in the presence of propranolol hydrochloride 10−5 and 10−6 g/ml. Adrenaline and noradrenaline were both shown to produce contractions of the tissue. The relative order of potency of the catecholamines (adrenaline &gt; noradrenaline &gt; isoprenaline), together with the antagonism exhibited by phenoxybenzamine, suggests that the contractions were due to α-adrenergic receptor involvement.
Relative activity of prostaglandins E1, A1, E2 and A2 on lipolysis, platelet aggregation, smooth muscle and the cardiovascular system
Authors: Weeks J R , Chandra Sekhar N , Ducharme D W 
Published: April 2011

Abstract
The relative activities of four prostaglandins (PGE1, PGA1, PGE2 and PGA2) were determined in several biological tests. They were compared as intestinal muscle stimulants on rabbit duodenum and guinea-pig ileum, as inhibitors of adrenaline-induced lipolysis in rat isolated epididymal fat, inhibitors of platelet aggregation in rabbit plasma, as vasodepressor agents in anaesthetized rats and dogs, and on both blood pressure and cardiac output in unanaesthetized dogs. Formation of PGAs by dehydration and introduction of one additional double bond virtually abolished activity in all of these systems except the cardiovascular system. PGE2 was more active than PGE1 on isolated rabbit duodenum and as an antilipolytic agent, but less active in the other systems. Only PGE1 had high potency as an inhibitor of platelet aggregation.
Relation of brain sensitivity and hepatic metabolism of hexobarbitone to dose-response relations in infant and young rats
Authors: Kalser Sarah C , Forbes Eleanore , Kunig Rosemarie 
Published: April 2011

Abstract
The dose-response relation to hexobarbitone of infant (5 day) and young (44 day) male rats was examined, and the relative contribution of hepatic metabolism (measured in vitro) and changes in brain sensitivity to the overall response were evaluated. The infant rat shows a parallel shift to the left in its dose-response curve with the relative potency of hexobarbitone almost 5 times greater than for the 44 day old animal. The slope of the curves show marked changes at the first lethal dose level of drug. This and other evidence suggest that death may not be merely an extension of the mechanism causing hypnosis. Infant rats exhibited a shorter increment in sleep time for increasing doses of hexobarbitone than is predictable from their low rate of in vitro metabolism. Although this is also true for the young rats, the two values are in much closer agreement than for the infant animals. Brain concentrations of hexobarbitone, measured upon regaining of the righting reflex, were lower in the infant than in the young rat. This suggests the central nervous system of the infant rat has an increased sensitivity to the drug.
Kinetics of the hydrolysis of phosphatidylcholine and lysophosphatidylcholine
Authors: Marriott P H 
Published: April 2011

Abstract
An experimental technique capable of estimating as little as 10 nano-equivalents of long-chain carboxylic acids (fatty acids) has been used to study the decomposition of phospholipids. The rate of release of acids varied with the monovalent cation which was associated with the hydroxyl ion in the hydroxide used. Because the concentration of hydroxide was much greater than the concentration of phospholipid, the rate of hydrolysis was first order with respect to the phospholipid. The pseudo-first order reaction velocity constant varied as the first power of the concentration of lithium hydroxide, but as the second power of the concentration of potassium, sodium, tetramethylammonium, or tetraethylammonium, hydroxides. It is postulated that (i) lecithin and lysolecithin, in strong alkaline solution, bind lithium ions much more strongly than potassium, sodium, tetramethylammonium, or tetraethylammonium ions, and (ii) it is only this cation-phospholipid complex which is broken down by hydroxyl ions.
Esters of choline and β-trimethylammoniopropionic acid: geometrical isomerism and anti-acetylcholinesterase activity
Authors: Kay J B , Robinson J B 
Published: April 2011

Abstract
The preparation of the choline esters of cis- and trans-4-t-butylcyclohexanecarboxylic acid is reported. The similar inhibitory potency displayed by these isomers towards the acetylcholinesterase catalysed hydrolysis of acetylcholine is explained on the basis of the binding of a thermodynamically unstable conformation of the cis-isomer to the active site. Similar studies employing the β-trimethylammoniopropionate esters of cis- and trans-4-t-butylcyclohexanol suggest that the “reverse esters” do not bind to the active site in an identical manner to the acylcholines.
Anticholinergic effects and passage through the intestinal wall of N-butylhyoscine bromide
Authors: Pomeroy A R , Rand M J 
Published: April 2011

Abstract
The effects of N-butylhyoscine bromide (Buscopan) were examined on responses of guinea-pig isolated intestine to transmural stimulation and to peristalsis induced by raising the intraluminal pressure. The drug acted rapidly and in low concentration to abolish peristaltic activity and responses to transmural stimulation when applied to the serosal surface of the ileum, but from 100 to 1000 times the concentration was required when it was applied to the mucosal surface. The effects were more persistent after mucosal than after serosal application. N-Butylhyoscine bromide was bound to mucus and mucosal material, the ratio of free to bound drug being 2:1. The drug passed through portions of the intestinal wall containing Peyer’s patches more rapidly than through portions containing no macroscopically visible lymphoid tissue. The rate of passage through Peyer’s patches, but not through other portions, increased with increasing hydrostatic pressure. These findings help to explain why enterally administered N-butylhyoscine bromide exerts anti-cholinergic effects on the gut without producing systemic actions.
Competitive antagonism of isoprenaline-induced cardiac necroses by β-adrenoreceptor blocking agents
Authors: Dorigotti L , Gaetani M , Glässer A H , Turolla E 
Published: April 2011

Abstract
Histological methods show that low doses of (±)-isoprenaline may produce cardiac necroses in the rat. The percentage of animals with focal necroses was related to the dose within the range 0·005 to 0·5 mg/kg administered subcutaneously. Therefore the heart-damaging effect of isoprenaline as well as the antagonistic effect of β-adrenoreceptor blocking agents could be evaluated quantitatively. Pre-treatment of animals with dichloroisoprenaline, pronethalol and propranolol produced a parallel displacement to the right of the dose-response line for isoprenaline. However, when lesions were already in progress, these agents were without protecting effect.
Simulation of the apparent effects of mebanazine on growth hormone by pair-feeding of control animals
Authors: Barrett A M 
Published: April 2011

Abstract
The degree and duration of insulin hypoglycaemia was potentiated by chronic oral medication with mebanazine in rats. Hypophysectomy alone increased sensitivity to insulin but did not abolish the potentiating effect of mebanazine. Chronic mebanazine treatment (15 mg/kg/day) for 6 weeks markedly reduced weight gain, food and water consumption and pituitary growth hormone content, but the results were not significantly different from those in unmedicated pair-fed controls. Similarly, immature rats treated with mebanazine had a significant reduction in the width of the tibial epiphysial cartilage but this was not different from that in pair-fed animals. After 18 h of fasting, acute administration of mebanazine had little effect on food consumption in the 2 h period following dosing but a significant effect over 24 h. In fed rats mebanazine in a single oral dose significantly reduced eating in the following 6 h. Treatment with mebanazine at 2·5 mg/kg for 15 days significantly reduced food intake but did not potentiate insulin hypoglycaemia. From the results it would appear that previous suggestions that mebanazine specifically interferes with growth hormone release are incorrect and the findings emphasize the importance of measuring food intake in experiments of long duration.
The control of oil-in-water emulsion consistency using mixed emulsifiers
Authors: Barry B W 
Published: April 2011

Abstract
Mixtures of emulsifiers of the surfactant-fatty alcohol type are widely used to stabilize oil-in-water emulsions and to alter their consistency from fluid to semi-solid. A mechanism, involving the formation of a viscoelastic network in the continuous phase, is proposed to explain this self-bodying action. Evidence has been adduced from published data on a variety of systems. Support for this concept is also provided by the results obtained from a concentric cylinder study of the rheology of liquid paraffin in water emulsions containing a fixed concentration of cetostearyl alcohol and varying amounts of polyoxyethylene sorbitan monooleate, cetomacrogol 1000, sodium dodecyl sulphate or cetrimide.
Interaction between phenylpropanolamine and monoamine oxidase inhibitors
Authors: D’Mello A 
Published: April 2011

Abstract
The role of monoamine oxidase in the potentiation of the pressor effect of phenylpropanolamine (norephedrine) by monoamine oxidase inhibitors has been investigated. In vitro, phenylpropanolamine was not a substrate of monoamine oxidase from guinea-pig liver. In spinal cats the pressor effects of both phenylpropanolamine and tyramine were potentiated by a monoamine oxidase inhibitor, nialamide, and by the microsomal enzyme inhibitor SKF 525-A, which is not a monoamine oxidase inhibitor. These results suggest that the enhanced pressor effect of phenylpropanolamine in the presence of monoamine oxidase inhibitors is caused by inhibition of other enzymes.
Adrenergic neuron blocking properties of (±)-propranolol and (+)-propranolol
Authors: Barrett A M , Nunn Barbara 
Published: April 2011

Abstract
The action of (±)-propranolol and (+)-propranolol on the electrical stimulation of adrenergic nerves to smooth muscle has been studied in the isolated ear artery from rabbits and the isolated vas deferens preparation from rats. Both drugs exhibited an adrenergic neuron blocking action at a pre-junctional site at concentrations ranging from 4·6 to 14 μg/ml. At lower concentrations the effects were variable and more often potentiation of the responses was observed. The responses to added noradrenaline were uniformly potentiated. The effect was related to local anaesthetic activity and not considered to be a specific adrenergic neuron blocking effect as occurs with guanethidine or bretylium.
The interaction of ethanol and amphetamine metabolism
Authors: Creaven P J , Barbee Theresa , Roach Mary K 
Published: April 2011

Abstract
Ethanol, 1, 3, and 5 g/kg, depresses the hydroxylation of amphetamine by the rat in vivo. At 5 g/kg, ethanol does not affect the hydroxylation of acetanilide or biphenyl in vivo. Amphetamine hydroxylation is unaffected by phenobarbitone or benzo[a]pyrene pretreatment but is depressed by pretreatment with 2-diethylaminoethyl-2, 2-diphenyl-valerate (SKF 525-A), 2, 4-dichloro-6-phenylphenoxyethylamine (DPEA), and 2, 4-dichloro-6-phenylphenoxy-NN-diethylethylamine (Lilly 18947).
The biliary metabolism of butylated hydroxytoluene (3, 5-di-t-butyl-4-hydroxy-toluene) and its derivatives in the rat
Authors: Holder G M , Ryan A J , Watson T R , Wiebe L I 
Published: April 2011

Abstract
The biliary metabolism of 3, 5-di-t-butyl-4-hydroxybenzyl alcohol (BHT-CH2OH), 3, 5-di-t-butyl-4-hydroxybenzaldehyde (BHT-CHO) and 3, 5-di-t-butyl-4-hydroxybenzoic acid (BHT-COOH) after parenteral administration has been examined in the rat and compared to that of 3, 5-di-t-butyl-4-hydroxytoluene. Quantitative excretion and chemical examination of bile showed that in the enterohepatic circulation BHT-COOH or its ester glucuronide is the recirculating compound from the four compounds studied. Biliary excretion data are also presented for 1, 2-bis(3, 5-di-t-butyl-4-hydroxyphenyl)ethane.
Microcrystalloptic tests for lysergic acid diethylamide and other hallucinogens
Authors: Genest K , Lowry Lorna J 
Published: April 2011

Abstract
Microcrystallopic tests for LSD, NN-diethyltryptamine, NN-dimethyltryptamine, bufotenine, psilocin, psilocybin and STP are described. The tests are recommended in conjunction with other analytical techniques if applied for the forensic identification of hallucingens.
A note on the identification of sulphonamides by thin-layer chromatography
Authors: clarke E G C , Humphreys D J 
Published: April 2011

Abstract
A method is described for the identification of 25 sulphonamides by thin layer chromatography. Four systems are used, the solvents being (I) chloroform-methanol (4:1), (II) chloroform-carbon tetrachloride-methanol (7:2:1), (III) ethyl acetate-methanol (9:1), (IV) acetone-methanol (4:1), the plates being coated with silica gel G mixed with (I) sodium hydroxide, (II) potassium hydrogen sulphate, (III) water, (IV) sodium hydroxide. The location reagents are (a) copper sulphate, (b) p-dimethylamino-benzaldehyde, (c) N(1-napthyl) ethylenediamine di-HCl, and (d) fluorescein.
Application of the ΔA method to the determination of morphine
Authors: Wahbi A M , Farghaly A M 
Published: April 2011

Abstract
Tablets, suppositories and ear-drops have been assayed using the ΔA method to eliminate interferences. The absorbance at 298 nm is measured for solutions in acid and alkaline media, the difference (Δ A) being taken as a measure of morphine content. The same method has been applied to suppositories after extraction of the drug from the base. Ear-drops containing phenol in addition to morphine were assayed by measuring ΔA at 288 and 298 nm and evaluating the morphine concentration from a pair of simultaneous equations.
Structure-activity relations for anticholinergic dioxolans
Authors: Brimblecombe R W , Inch T D 
Published: April 2011

Abstract
4-Dimethylaminomethyl 1, 3-dioxolan derivatives have been examined for anticholinergic potency. Quaternary derivatives in which C-2 was substituted with two bulky substituents were found to have anticholinergic potencies similar to those of atropine in the peripheral nervous system. A comparison of the enantiomeric cis and trans 2-cyclohexyl-2-phenyl-4-dimethylaminomethyl-1, 3-dioxolan methiodides showed that the observed configurational selectivity depended mainly on the configuration at C-2 and not on the geometrical relation between C-2 and C-4.
The effects of salicylate on the concentrations of amino-acids in mouse tissues
Authors: Dawkins P D , Smith M J H 
Published: April 2011

Abstract
The concentrations of amino-acids in chopped preparations of mouse liver incubated with 0 to 20 mM salicylate were measured. The changes, observed with salicylate concentrations of 10 mM and above, were increased concentrations of aspartate, glutamine, tyrosine and ornithine and decreased concentrations of glutamate and γ-aminobutyrate. The effects of the intraperitoneal injection of salicylate, in doses ranging from 75 to 600 mg/kg body weight, on the amino-acid concentrations in mouse blood, kidney, liver and brain were studied. With a dose of 600 mg/kg, the amino-acid concentrations were decreased in the blood (except glutamate and aspartate which increased) and in the kidney, were increased in the liver (except glutamine, glutamate, glycine and alanine which decreased) and were unchanged in the brain (except alanine, valine and leucine which decreased and γ-aminobutyrate which increased). These changes may result from a combination of an inhibitory effect of salicylate on the renal tubular transport of the amino-acids and intracellular actions of the drug on aminotransferase and other enzyme activities.