bluuebunny/crossref_metadata_2025_split huggingface dataset:
The Anticonvulsant Properties of 2-Methyl-3-p-Bromophenyl-3H-4-Quinazolone Hydrochloride (B.D.H. 1880) and Some Related Compounds
Authors: Bianchi Camillo , David Alan 
Published: April 2011

Abstract
Twenty-five 2-alkyl-3-aryl-3H-4-quinazolone derivatives, eight 2-aryl-3-alkyl-3H-4-quinazolone derivatives and six 2-alkyl-3-aryl- 3H-4-thioquinazolone derivatives were examined for orala nticonvulsant properties against leptazol induced convulsions in mice. 2-Methyl-3- p-bromophenyl-3H-4-quinazolone hydrochloride (B.D.H. 1880) was the most active compound and was therefore examined more fully. It is fourteen times more active than troxidone against leptazol and eight times more active against electroshock induced convulsions. B.D.H. 1880 also has a better therapeutic index than troxidone. It has approximately one-quarter the activity of phenytoin against leptazol and one-twelth the activity against electroshock-induced convulsions. B.D.H. 1880 and primidone have similar anticonvulsant properties against leptazol induced convulsions but B.D.H. 1880 is only one-third as active as primidone against electroshock induced convulsions.
Some 2, 3-Disubstituted 3H-4-Quinazolones and 3H-4-Thioquinazolones
Authors: Jackman G B , Petrow V , Stephenson O 
Published: April 2011

Abstract
Some 2-alkyl-3-aryl-3H-4-quinazolones (I; X = 0) have been prepared and a number of them converted into the thioquinazolones (I; X = S). A new method for the synthesis of 3-alkyl-2-aryl-3H-4-quinazolones (VI) has been developed and has been employed for the synthesis of representative derivatives.
Biological study of the above compounds revealed that some of them, and in particular the 2-alkyl-3-halophenyl-3H-4-quinazolones are potent anticonvulsant agents.
Determination of Xenopus Index and Haemolytic Index in Fruits of Sapindus Mukorossi Gaertn. (Sapindaceae) and Seeds of Entada Scandens Benth. (Mimosaceae)
Authors: Blyberg Marthe 
Published: April 2011

Abstract
Two drugs, known from the Burmese and Indian folk medicines, the fruits of Sapindus mukorossi and the seeds from Entada scandens, were examined for their effect on Xenopus larvae. As a comparative test the haemolytic index of the drugs was also determined.
The investigations showed that parts of both drugs contained substances which were toxic for Xenopus larvae and which haemolysed blood. The fruit wall from Sapindus mukorossi and the seed kernel from Entada scandens had a Xenopus index of approximately 7,000 and 400 respectively. The corresponding haemolytical indexes were approximately 7,000 and 150.
Micellar Size and Surface Activity of Some C18α-Monoglycerides in Benzene
Authors: Robinson N 
Published: April 2011

Abstract
Some C18 α-monoglycerides in benzene have been studied by the light-scattering and surface tension methods. The glycerol esters of stearic, oleic and linoleic acids had micellar weights of less than 7,000; glycerol monoricinoleate had a micellar weight of over 18,000. All the mono-glycerides showed some surface activity in benzene, glycerol monoricinoleate having the greatest, the other unsaturated monoglycerides the least.
A New Colorimetric Method for the Determination of Chloral Hydrate
Authors: Archer A W , Haugas E A 
Published: April 2011

Abstract
A colorimetric method is described for the determination of chloral hydrate, particularly in the presence of its decomposition products. Quinaldine ethiodide reacts with chloral hydrate in alkaline solution to produce a stable, blue cyanine dye. Chloroform, trichloracetic acid and formic acid do not react under the conditions described. The colour produced conforms to the Beer-Lambert law up to 100 μg./10 ml. of reaction mixture.
The Pressor Action of Guanethidine in the Spinal Cat
Authors: Bartlet A L 
Published: April 2011

Abstract
Guanethidine has a marked pressor action in the spinal cat. Doses of 2–4 mg./kg. produce a greater increase in blood pressure than doses of 8–16 mg./kg. Large doses of guanethidine (16 mg./kg.) inhibit the pressor action of small doses (2 mg./kg.). Guanethidine potentiated the pressor action of noradrenaline but inhibited that of tyramine. The degree of inhibition of tyramine increased with the dose of guanethidine, but was inversely related to the pressor action of guanethidine.
Assay of Digitalis in Pigeons by Intraperitoneal Administration
Authors: Kušević Vladimir 
Published: April 2011

Abstract
A new biological method of assay for digitalis is proposed. Preparations are administered intraperitoneally and the LD50 estimated by means of the “up-and-down” procedure. The LD50 of the preparation examined is compared with the LD50 of the standard preparation, and the result expressed in international units. The proposed method gives more evidence on the loss in potency of the drug than does the intravenous method in pigeons (U.S.P. XVI).
The Alkaloids of the Genus Datura, Section Brugmansia: Part I. D. Cornigera Hook
Authors: Evans W C , Than M Pe 
Published: April 2011

Abstract
Hyoscine has been isolated as the main alkaloid from the leaves, flowers, pericarp and seeds of Datura cornigera Hook. Noratropine occurs in the leaves, flowers and pericarp. The following alkaloids have been obtained from the roots, (—)-3α,6β-ditigloyloxytropane, 7-hydroxy-3,6-ditigloyloxytropane, hyoscine, hyoscyamine, atropine, norhyoscyamine, noratropine, 3α,6β-dihydroxytropane and the presence of others indicated. Hyoscyamine is the principal alkaloid of the whole roots but the root-wood, although giving a low yield of total alkaloids, contains a relatively high proportion of noratropine.
The Biological Assay of Oxytocin in the Presence of Ergometrine
Authors: Berde B , Stürmer E 
Published: April 2011

Abstract
The oxytocin content of a solution of oxytocin and ergometrine can be assayed with great accuracy by the chicken blood pressure method provided the rooster preparation is highly sensitive to oxytocin. The hormone can also be assayed with reasonable accuracy by measuring the response of the milk-ejection pressure in the mammary gland of the lactating rabbit. However, the rat uterus in vitro method yields erroneously high results due to the additional uterotonic effect of the ergometrine.
The Neuromuscular Blocking Action of Suxamethonium on the Rat Diaphragm
Authors: Whittaker R 
Published: April 2011

Abstract
Experiments are described using the rat isolated phrenic nerve diaphragm preparation, in which suxamethonium produced a neuromuscular block consisting of an initial phase of fairly sharp onset followed by a prolonged phase, which first remained at a steady level and then slowly decreased in intensity over several hours. Suxamethonium block is antagonised by potassium and intensified by tubocurarine in both phases. It would therefore appear that the depolarising action of suxamethonium is complicated by some measure of competitive inhibition in the isolated nerve-muscle preparation as in the intact animal.
The Effect of Ortho Substitution on the Pharmacology of Benzoylcholine
Authors: Thomas J , Buckley D 
Published: April 2011

Abstract
The effects of mono- and di-ortho substitution of benzoylcholine on actions on the rat phrenic diaphragm and frog rectus abdominis preparations have been examined. Ortho substitution of benzoylcholine does not necessarily lead to a reduction in activity and may increase potency. It appears that mono-ortho-iodo substitution provides most stability combined with pharmacological activity.
Dissociation Constants of Some Compounds Related to Lysergic Acid
Authors: Chilton J , Stenlake J B 
Published: April 2011

Abstract
Dissociation constants have been recorded for ergometrine, ergometrinine and a number of alkanolamides of 3-dimefhylaminopropionic acid, 1-methylhexahydronicotinic acid and arecaidine. The similarity of ΔpK (amide) values for the alkanolamides with that for ergometrine, offers evidence that such values may be taken as an indicator of amino-carboxyl distances.
Antagonism of Guanethidine by Dexamphetamine and Other Related Sympathomimetic Amines
Authors: Day M D , Rand M J 
Published: April 2011

Abstract
Dexamphetamine and certain other indirectly acting sympathomimetic amines prevent or reverse the sympathetic nerve blocking action of guanethidine in anaesthetised cats and dogs. Noradrenaline and dopamine do not antagonise the blocking action of guanethidine. These observations are discussed in relation to the mode of action of guanethidine and to a possible clinical significance of these findings.
Drug-Plasma Binding Measured by Sephadex
Authors: Barlow C F , Firemark H , Roth L J 
Published: April 2011

Abstract
A method is described using the cross-linked dextran gel, Sephadex, for the study of drug binding. Although not quantitative in terms of per cent bound, this method gives an indication of the comparative strength of binding. The usefulness of this method in the separation of compounds with different plasma binding characteristics is suggested.
Ultrasonic Irradiation of Some Phospholipid Sols
Authors: Saunders L , Perrin J , Gammack D 
Published: April 2011

Abstract
Ultrasonic irradiation of turbid sols of egg lecithin and of highly unsaturated synthetic lecithins, breaks down the large particles in the sols into micelles of micellar weight of about 5 × 106. The irradiated sols are clear and do not show any great increase of turbidity over a period of several days; they are capable of solubilising large quantities of cholesterol. The size and shape of micelles in the irradiated sols has been studied by means of viscosity and diffusion measurements and by determination of sedimentation coefficients in the ultra-centrifuge.
The Morphology and Anatomy of the Leaf of Podophyllum Hexandrum Royle
Authors: Ellis S , Fell K R 
Published: April 2011

Abstract
A brief review of the history and medicinal uses of Podophyllum hexandrum Royle (= P. emodi Wall.) is given, together with an illustrated account of the macroscopy and anatomical structure of the leaf. The diagnostic characters of the powdered leaves are recorded and illustrated.
The Absorption of Bretylium and Related Quaternary Ammonium Salts from the Alimentary Tract
Authors: Boura A L A , McCoubrey A 
Published: April 2011

Abstract
N-Methyl-14C-labelled bretylium was injected into the lumen of segments of the gastrointestinal tract of cats prepared so that blood draining from these segments could be collected for analysis. The drug was not absorbed from the stomach. The concentration of drug in the venous blood from the duodenum rose steadily during 1.5–2 hr. but then declined to a value slightly exceeding that in the systemic blood. The greater part of the dose was not absorbed. Bretylium slowly traversed rat duodenum (mucosa to serosa) in vitro and the rate was not affected by factors that can influence carbohydrate metabolism. Transfer proceeded equally well from serosa to mucosa. To investigate means of obtaining better absorption of quaternary ammonium anti-adrenergic drugs a close analogue of bretylium bearing a choline residue was phosphorylated to give a phosphoric ester betaine (III). This was about twice as active by the oral route in cats as the parent drug, in which form it was excreted in the urine.
The Effects of Hydrocortisone on the Changes in Lipid Metabolism Induced in Guinea-Pig Lung Tissue by Anaphylaxis in vivo
Authors: Goadby P , Smith W G 
Published: April 2011

Abstract
Exposure of sensitised guinea-pigs to aerosolised antigen causes alterations in the lipid metabolism of their lung tissue. The responses of control animals exposed to aerosolised distilled water has suggested that these metabolic disturbances are probably a manifestation of a “stress reaction”. Pretreatment of sensitised animals with anti-anaphylactic dosage of sodium hydrocortisone hemisuccinate abolished this reaction.
Influence of the length of the stimulus period and frequency of sympathetic stimulation on the response of the guinea-pig isolated vas deferens to bretylium, guanethidine and amphetamine
Authors: Day M D 
Published: April 2011

Abstract
The height of contraction of guinea-pig isolated vas deferens preparations in response to pre- or postganglionic sympathetic nerve stimulation at various stimulus frequencies was shown to vary with varying length of stimulation period. Short stimulation periods, as used by some workers, produced suboptimal contractions especially at the lower frequencies. It is suggested that variations in the length of the stimulation period could account for some of the contradictory results reported by various workers using this preparation. Thus the effect of low concentrations of dexamphetamine was qualitatively changed as the length of the stimulation period was increased; with short stimulation periods dexamphetamine impaired the responses to sympathetic stimulation but enhanced them if stimulation was continued until contractions had reached the maximum height obtainable. Higher concentrations of dexamphetamine impaired the contractions, the effect being most marked against the higher stimulus frequencies. Using stimulation to maximal effect a qualitative difference in the blocking actions of bretylium and guanethidine was demonstrated. Bretylium reduced the responses to the higher stimulus frequencies to a greater extent than it reduced the responses to the lower frequencies. Guanethidine reduced the responses to all frequencies so that there was a parallel shift of the frequency/response curve to the right. The possible significance of these findings is discussed.
Protein binding and the excretion of some azo dyes in rat bile
Authors: PRIESTLY B G , O'REILLY W J 
Published: April 2011

Abstract
The kinetics of biliary excretion of four dyes, amaranth, geranine, lissamine and dechlorolissamine have been examined in the rat. The protein binding of each dye to blood and liver in vitro was examined, and a correlation found between excretion rate and the relative degree of binding of dye to the liver compared with the blood.
Effect of solubilisation on the antibacterial activity of hexachlorophane
Authors: Anderson R A , Morgan K J 
Published: April 2011

Abstract
The solubilisation of hexachlorophane by various non-ionic agents has been studied at pH 2·5 and 8·0. The interaction of the phenol with these agents in unsaturated systems at pH 8·0 has been determined by a dialysis technique using rubber latex membranes. The bactericidal activity is shown to depend on the concentration of unbound hexachlorophane, but this is not simply related to the degree of saturation of the total system. The results of agar-plate diffusion tests cannot be correlated with either the concentration of unbound hexachlorophane or the total concentration.
Accumulation of α-methyltyramine by the noradrenaline uptake process in the isolated rat heart
Authors: IVERSEN LESLIE L 
Published: April 2011

Abstract
In the perfused isolated rat heart 3H-α-methyltyramine is accumulated as rapidly as noradrenaline. The accumulation of 3H-α-methyltyramine is reduced by the presence of noradrenaline or other drugs known to inhibit the noradrenaline uptake mechanism. 3H-α-Methyltyramine and noradrenaline probably compete for a common uptake mechanism. In these experiments less than 5% of the 3H-α-methyltyramine accumulated by the heart was metabolised to α-methyloctopamine.
The preparation of some derivatives of glycyrrhetic acid and oleanolic acid
Authors: DEAN P D G , HALSALL T G , WHITEHOUSE M W 
Published: April 2011

Abstract
Some new derivatives of glycyrrhetic acid and oleanolic acid were prepared and characterized. Various combinations of the modified and normal functional groups were synthesized as required for a separate study of the uncoupling activities of glycyrrhetic acid and oleanolic acid. The hydroxyl functions of these two acids were modified to β-carboxypropionyl, acetyl and β-methoxycarbonylpropionyl esters. The carboxyl function of glycyrrhetic acid was converted to amide, p-amidobenzoic acid, o-amidobenzoic acid and the glycine conjugate of the acid. 11-Deoxy (glycyrrhetic acid) and 9,11-dehydro-11-deoxo (from both acids) analogues were prepared. 11-Oxo analogues of oleanolic acid were synthesized as well as the methyl esters.
The effect of succinylcholine on the isolated retractor bulbi muscle of the cat
Authors: BACH-Y-RITA PAUL , LEVY JOSEPH V , STEINACKER ANTOINETTE 
Published: April 2011

Abstract
The retractor bulbi muscle of the cat does not contain multi-innervated slow fibres, and succinylcholine (suxamethonium), 1–1000 μg/ml, causes no contracture of the isolated muscle. However, succinylcholine in a concentration of 1 μg/ml causes a contracture of the isolated inferior oblique and rectus muscles of the cat eye.
Modification of morphine analgesia by drugs affecting adrenergic and tryptaminergic mechanisms
Authors: Fennessy M R , Lee J R 
Published: April 2011

Abstract
The effects of drugs that modify adrenergic or tryptaminergic mechanisms were tested on the analgesic action of morphine in mice. Analgesia was assessed by the hot plate method and phenylquinonewrithing method. Reserpine antagonized the analgesic action of morphine in both tests, the maximal effects occurring 6–8 h after the administration of reserpine. p-Chlorophenylalanine antagonized the analgesic action of morphine as assessed by the writhing method but not by the hot plate method. The analgesic action of morphine was not modified in either test by pretreatment with α-methyl-p-tyrosine, propranolol, phentolamine or methysergide. These results suggest that the analgesic action of morphine, as measured in the writhing test, may be mediated by 5-hydroxytryptamine but that other mechanisms may be involved in the hot plate test.
Decreased distribution of oxotremorine to brain after pharmacological blockade of its peripheral acetylcholine-like effects
Authors: KARLÉN BO , TRÄSKMAN LIL , SJÖQVIST FOLKE 
Published: April 2011

Abstract
The distribution of [3H]oxotremorine, after intravenous injection, to brain and tissues of rats and mice has been studied. In rats, oxotremorine (0·3 mg/kg) rapidly reached the brain with a peak concentration of 1200 ng/g at 1 min. Blockade of the peripheral muscarinic effects of oxotremorine with amitriptyline methyl iodide or atropine methyl nitrate (25 mg/kg, s.c.) markedly decreased the brain content of oxotremorine (peak concentration 400 ng/g), probably as a result of its more rapid distribution to peripheral tissues and an increased volume of distribution. The ratio of drug distribution between plasma and brain is unaffected by pretreatment with anticholinoceptive drugs. Also, the total body concentrations of oxotremorine are similar in pretreated rats and controls. A small dose of oxotremorine (10 μg/kg) is distributed similarly in pretreated rats (amitriptyline methyl iodide, 25 mg/kg, s.c.) and in controls. In mice there was a linear relation between dose, up to 180 μg/kg, and brain concentration of oxotremorine. At higher doses, relatively; more drug reached the brain. Oxotremorine induced a marked fall in blood pressure in the unanaesthetized rat that was reduced by amitriptyline methyl iodide and reversed by atropine methyl nitrate. It seems likely that differences in blood flow between pretreated rats and controls are responsible for the differences in the distribution of the drug.
A method for the continuous recording of peripheral vascular conductance
Authors: GARDINER D G , HAMILTON T C , PARKES M W 
Published: April 2011

Abstract
A method is described for the continuous recording of the conductance of a perfused vascular bed, derived from simultaneous measurement of blood flow and perfusion pressure. For the autoperfused hindquarters of the anaesthetized cat, it is shown that for vasoconstrictor or vasodilator drugs, injected either intravenously or into the arterial perfusion circuit, a record of changes in conductance may be of considerable aid in clarifying the responses of the vessels.
The quantitative analysis of polyvinylpyrrolidone by infrared spectrophotometry
Authors: RIDGWAY K , RUBINSTEIN M H 
Published: April 2011

Abstract
The quantitative assay of the binding agent polyvinylpyrrolidone (PVP) in granules of magnesium carbonate has been shown to be possible. The method is to determine the infrared absorption spectrum of a chloroform extract. Quantities of PVP down to 0·1 mg can be successfully assayed to ±1 % in solution as dilute as 0·1 % w/v.
Correlation of the recovery of the granular uptake-storage mechanism and the nerve impulse induced release of [3H]noradrenaline after reserpine
Authors: ALMGREN O , LUNDBORG P 
Published: April 2011

Abstract
Rats were treated intraperitoneally with 10 mg/kg reserpine. After various time intervals 1 μg/kg ± [3H]noradrenaline (3H-NA) was administered intravenously, and the uptake into subcellular fractions of the submaxillary gland was measured or, in some of the rats, the sympathetic chain of the neck was electrically stimulated with 10 impulses/s for 30 min. The release of 3H-NA and the contraction response of the lower eye-lid were measured. A striking parallel was observed between the recovery of the 3H-NA uptake into the amine storage particles and the nerve impulse-induced release of 3H-NA, and also the recovery of the functional response. The somewhat earlier recovery of the 3H-NA uptake into the coarse fraction might reflect the existence of another type of amine storage granule or might represent granules present near the nerve cell membrane. A possible increase in the turnover of the adrenergic transmitter during the period of recovery after reserpine is discussed.
The effects of sympathetic nerve stimulation and guanethidine on parasympathetic neuroeffector transmission; the inhibition of acetylcholine release
Authors: VIZI E S , KNOLL J 
Published: April 2011

Abstract
The effect of noradrenaline released either by sympathetic nerve stimulation or guanethidine added to the organ bath has been studied on acetylcholine release from parasympathetic nerve terminals and compared with the effect of exogenous noradrenaline. Sympathetic nerve stimulation, guanethidine and noradrenaline reduced the release of acetylcholine from resting rabbit intestine by up to 70%. Sympathetic stimulation and guanethidine failed to reduce acetylcholine release in preparations previously depleted of noradrenaline. Noradrenaline added to the bath still remained effective. The fact that noradrenaline released is capable of inhibiting acetylcholine release supports the concept that noradrenaline physiologically controls the release of acetylcholine.
Myocardial necroses produced by intravenous infusion of isoprenaline into rats
Authors: GRYGLEWSKI R J , KULIG A , KOSTKA-TRABKA E 
Published: April 2011

Abstract
Intravenous infusion of isoprenaline in doses of 2,20,200,2000 μg/kg per min over 20 min into heparinized Wistar rats results in myocardial necroses and a rise in SGPT activity, erythrocyte sedimentation rate and leucocytosis. A quantitative method for estimation of intensity and distribution of myocardial necrotic foci is described. The intensity of myocardial lesions is observed linearly related to the infused isoprenaline at 2, 20 and 200 μg/kg per min. Damaged areas are mainly found in subendocardial and apical regions of left ventricle.