bluuebunny/crossref_metadata_2025_split huggingface dataset:
Pharmacological studies with adenine, adenosine and some phosphorylated derivatives on guinea-pig tracheal muscle
Authors: Farmer J B , Farrar D G 
Published: April 2011

Abstract
Adenine, adenosine and three adenine nucleotides all caused relaxation of the guinea-pig trachea. The relaxation to the nucleotides was often preceded by a contraction. The response to adenosine and the nucleotides, but not adenine, was potentiated by dipyridamole. Imidazole inhibited the response to adenine alone. Propranolol had no effect on the response to any of the compounds. It is concluded that the guinea-pig trachea does not possess a nucleotide-specific receptor as has been postulated for some other smooth muscle preparations. An alternative hypothesis postulating an adenosine-specific receptor is presented.
Interactions of bradykinin, prostaglandin E1, 5-hydroxytryptamine, histamine and adenosine-5′-triphosphate on the dye leakage response in rat skin
Authors: Chahl Loris A 
Published: April 2011

Abstract
Dye leakage in rats produced by intracutaneous injections of irritants was quantitated using an azovan blue technique. Concentration-response lines were obtained for irritants alone and in presence of constant concentrations of other irritants. 5-Hydroxytryptamine (5-HT) (10−7m) potentiated histamine, bradykinin and prostaglandin E1 (PGE1), but inhibited adenosine-5′-triphosphate (ATP). Histamine (10−5m) potentiated bradykinin, PGE1 and ATP. Bradykinin (10−6m) potentiated PGE1 only, but PGE1 (10−6m) potentiated bradykinin, 5-HT and histamine. ATP (10−4m) potentiated 5-HT, histamine and PGE1. Release of ATP during stimulation of sensory nerves might explain enhanced neurogenic oedema observed in skin surrounding an area pretreated with compound 48/80.
Polymorphism of disopyramide
Authors: Gunning S R , Freeman M , Stead J A 
Published: April 2011

Abstract
Two crystal forms of disopyramide have been characterized using X-ray diffraction, differential scanning calorimetry and infrared spectroscopy. The kinetics of the solid state transformation of Form I to Form II has been analysed using the Prout-Tompkins theory. An activation energy of 144 kJ mol−1 is calculated for the system. Dissolution and plasma concentrations show no significant differences in bioavailability between the two polymorphs.
Brain areas involved in the catecholamine mediated regulation of electroshock seizure intensity
Authors: Stull Richard E , Jobe Phillip C , Geiger Paul F 
Published: April 2011

Abstract
Selective treatments which alter the catecholamine content of discrete areas of the brain were tested for their effect on electroshock seizure intensity in the rat. The data indicate that depletion of noradrenaline and dopamine in near ventricular areas by the intracerebroventricular administration of the benzoquinolizine, Ro 4–1284, enhances electroshock seizure intensity. The enhancement of seizure produced by systemic Ro 4–1284 was antagonized by the intracerebroventricular injection of noradrenaline or dopamine which do not appear to penetrate more than 1 mm into the brain. Further, pretreatment with systemic iproniazid and l-dopa completely antagonized the increased seizure intensity produced by intracerebroventricular Ro 4–1284 and repleted brain catecholamines in both near and far ventricular areas. Thus, the effects of both noradrenaline and dopamine in attenuating electroshock seizure intensity appear to be exerted principally through periventricular structures.
The properties of tablets containing microcrystalline cellulose
Authors: Sixsmith David 
Published: April 2011

Abstract
Tablets have been prepared from mixtures of microcrystalline cellulose (Avicel) and spray dried lactose. Tests on these showed that a maximum value of dissolution rate occurred as the percentage of the cellulose increased. This maximum was at 4% w/w for mixtures containing Avicel PH 101 and coincided with the point of maximum liquid penetration rate. With grade PH 105 this maximum was at 2% w/w and corresponded to the optimum balance between the opposing factors of disintegration and liquid penetration rate. Addition of up to 2% w/w magnesium stearate to the formulation containing 4% w/w PH 101 grade had little effect on pore structure, but decreased the dissolution rate by retarding water penetration. Similar concentrations of Carbowax 4000 caused no such decrease.
Effect of oxotremorine and sodium pentobarbitone on the pharmacokinetics of intravenous tracer doses of radioactive choline
Authors: Nordberg Agneta 
Published: April 2011

Abstract
The present study explains for the previous findings that oxotremorine increases and sodium pentobarbitone decreases the initial brain uptake of intravenously injected radioactive choline (3H—Ch). The effects are explained by haemodynamic changes since a corresponding increase and decrease in the plasma concentrations of 3H—Ch were found. This is important to know when 3H—Ch is used for estimation of acetylcholine turnover in the brain. The drugs did not affect the distribution of radioactivity (3H) between plasma and erythrocytes.
Possible subdivisions among α-adrenoceptors in various isolated tissues
Authors: Barker Kathryn A , Harper Barbara , Hughes I E 
Published: April 2011

Abstract
The ratio (expressed in log10 units) of the equieffective concentrations of (+)- and (—)-noradrenaline has been measured in a variety of isolated tissues in the presence of cocaine (1 times 10−5m), tropolone (3 times 10−5m) and (±)-propranolol (5 times 10−7 to 5 times 10−5m). The values obtained fall into 3 distinct and statistically different groups. Firstly, a high group comprising (mean ± s.e.) mouse vas deferens (2·78 ± 0·04), rabbit duodenum (2·91 ± 0·07) and ileum (2·86 ± 0·05). Secondly a middle group comprising rabbit vas deferens (2·54 ± 0·04), bladder neck muscle (2·56 ± 0·07) and spleen (2·50 ± 0·02), guinea-pig vas deferens (2·55 ± 0·10) and bladder neck muscle (2·48 ± 0·13) and rat deferens (2·40 ± 0·08) and thirdly, a low group comprising the bladder detrusor muscle from both the rabbit (2·08 ± 0·08) and the guinea-pig (2·07 ± 0·04). Under the same conditions measurement of pA2 values for phentolamine and piperoxan against noradrenaline gave the following values in rat vas deferens (8·22 ± 0·07 and 6·72 ± 0·03 respectively) and mouse vas deferens (8·31 ± 0·05 and 6·53 ± 0·07 respectively). The results are discussed in relation to other findings concerning the nature of the α-adrenoceptor in these tissues. In spite of the absence of any significant difference between the potency of the α-adrenoceptor blocking agents in the two species it is suggested that α-adrenoceptors may not belong to a single homogeneous population but may vary in their characteristics from tissue to tissue.
Effect of butaclamol, a new neuroleptic, on serotoninergic mechanisms
Authors: Pugsley T A , Lippmann W 
Published: April 2011

Abstract
Butaclamol (1·0–0·1 mg kg−1, i.p.) and spiroperidol (1·0–0·5 mg kg−1, i.p.), but not (—)-butaclamol (15 mg kg−1, i.p.), blocked the hyperactivity induced in rats by tranylcypromine-l-tryptophan pretreatment. Neither butaclamol nor spiroperidol altered the accumulation of brain 5-HT following pargyline or the decline of brain 5-HT following inhibition with the tryptophan hydroxylase inhibitor α-propyldopacetamide thus indicating that butaclamol and spiroperidol do not affect either the synthesis or the turnover of brain 5-HT. It is concluded that the antagonism of the tranylcypromine-l-tryptophan-induced hyperactivity by butaclamol and spiroperidol is due to their blockade of dopaminergic receptors rather than an action on neuronal serotoninergic mechanisms.
Hyperpyrexic interaction between debrisoquine and pethidine in rabbits
Authors: Osman O H , Eltayeb I B 
Published: April 2011

Abstract
Pethidine injection into rabbits treated with debrisoquine either acutely or chronically resulted in severe interaction and fatal hyperpyrexia. Pretreatment of rabbits with p-chloro-phenylalanine, chlorpromazine, or cyproheptadine protected them against the interaction, while α-methyl-p-tyrosine was ineffective. In addition the administration of debrisoquine into 5-HTP pretreated rabbits produced a severe interaction and hyperpyrexia. The hepatic N-demethylation of pethidine was significantly inhibited by debrisoquine pretreatment both in vivo and in vitro. The debrisoquine-pethidine interaction could be due to 5-HT potentiation or prevention of uptake. Alternatively it could be due to inhibition of biotransformation of pethidine by debrisoquine. However, neither mechanism by itself alone could be held responsible as the sole explanation of the interaction.
Synthesis and pharmacological properties of a series of antidopaminergic piperidyl benzamides
Authors: Prieto J , Moragues J , Spickett R G , Vega A , Colombo M , Salazar W , Roberts D J 
Published: April 2011

Abstract
The synthesis and pharmacological screening for anti-apomorphine, stomach emptying and local anaesthetic activities of some new piperidylbenzamides is described. One of these, N-(1′-benzyl-4′-piperidyl)-2-methoxy-4-amino-5-chlorobenzamide (clebopride) is more potent than metoclopramide in tests related to blockade of cerebral dopamine receptors.
Structure and rheology of cetomacrogol creams: the influence of alcohol chain length and homologue composition
Authors: Eccleston G M 
Published: April 2011

Abstract
Liquid paraffin-in-water emulsions prepared with cetomacrogol 1000 and alcohols cetostearyl (A), cetyl (B), stearyl (C) and myristyl (D) were examined by microscopical, particle size analytical and rheological (continuous shear, small strain creep and oscillation) techniques at 25° as they aged over 30 days. The particle sizes of the emulsions were similar and did not increase significantly with age. Thus the rheological stabilities were not correlated with particle size distributions, but rather with viscoelastic networks formed in the continuous phases when the non-ionic mixed emulsifiers interacted with water. The rheological properties of emulsions B and D differed from those of emulsion C. Emulsion A, of mixed homologue composition, showed some properties similar to each of the pure alcohol emulsions. Emulsions B and D were semi-solid immediately after preparation whereas emulsion C was so mobile initially that small strain data were not derived. On ageing, the consistencies of B and D changed slightly initially, and then remained essentially constant. In contrast, the consistency of emulsion C increased on ageing, especially over the first few days when there was a change from mobile liquid to semisolid. Emulsion A was a semisolid initially but like emulsion C increased in consistency especially over the first 24 h. Continuous shear data indicated that this emulsion was the most resistant to structure breakdown. Microscopical examinations supported the view that the networks formed in emulsion A were the most extensive and that stearyl alcohol networks in C formed comparatively slowly. Although the cetomacrogol/pure alcohol networks were diffuse and sometimes crystallized, they did not rapidly disintegrate on storage as did the ionic surfactant/pure alcohol networks examined previously.
Pharmaceutical suspensions: relation between zeta potential, sedimentation volume and suspension stability
Authors: Kayes J B 
Published: April 2011

Abstract
The effect of added surface-active agents of various ionic types on the sedimentation volume of drug suspensions of betamethasone, griseofulvin, nalidixic acid and thiabendazole has been investigated, and the results correlated with previously measured zeta potentials. Study of the zeta potential/sedimentation volumes versus concentration plots showed that apparently only coagulated, deflocculated or sterically stabilized systems were formed. In most cases the sterically stabilized systems were produced from mixtures of ionic/non-ionic surfactants. These are examples of controlled coagulation, although non-ionic surfactant alone conferred stability against caking. Secondary minimum flocculation was not apparent but this may have been due to the method of examination of suspensions. The work confirmed that the DLVO theory of colloid stability and its modification to include a steric term can be applied to coarse suspension systems.
The in vitro bioavailability of various drugs formulated as hard gelatin capsules
Authors: Newton J M , Razzo F N 
Published: April 2011

Abstract
A factorially designed experiment has been carried out to study the influence of various additives on the in vitro release of drug from hard gelatin capsules. Analysis of variance confirms previous findings that, although the main factors of diluent type, diluent concentration, the absence and presence of both magnesium stearate and sodium lauryl sulphate, were highly significant, the existence of interactions between the factors prevented exact quantitative prediction of the influence of each factor. There appears however, to be a strong indication that the in vitro drug release of capsule formulations (y), expressed as the % of the drug content of the capsule which dissolves, can be related to the solubility of the drug (cs) by the expression y = 21·2 log cs + 31.2.
Phase equilibria and stability characteristics of chlorpropamide-urea solid dispersions
Authors: Ford James L , Rubinstein Michael H 
Published: April 2011

Abstract
Physical mixtures and melts of various compositions of chlorpropamide and urea have been prepared. The phase diagrams and the effects of ageing of the systems have been measured by differential scanning calorimetry. The eutectic composition was found to contain 89% w/w chlorpropamide. Greater concentrations of chlorpropamide produced solid solutions of urea in chlorpropamide, whereas solid solution formation did not occur at compositions less than 89%. Melts in the range 50–100% chlorpropamide, which included the eutectic, existed as glass solids. The effect of ageing produced generally an increase in the liquidus peak temperature which was considered to be due to a gradual increase in crystal size.
Carrageenan and thrombin trigger prostaglandin synthetase-independent aggregation of rabbit platelets: inhibition by phospholipase A2 inhibitors
Authors: Vargaftig Bernardo B 
Published: April 2011

Abstract
Acetylsalicylic acid, salicylic acid and indomethacin were equally effective in inhibiting aggregation of plasma-free rabbit platelets induced by carrageenan and by thrombin. In contrast, only acetylsalicylic acid and indomethacin suppressed the accompanying formation of prostaglandin-like activities. Blockade of aggregation required the presence of the inhibitors in the platelet preparation, whereas blockade of prostaglandin synthetase remained even when the inhibitors were washed out. Prostaglandin synthetase-derived products appear not to be involved in the development of aggregation by carrageenan or by thrombin. Such aggregation was inhibited by two phospholipase A2 inhibitors, bromophenacyl bromide and mepacrine. It is suggested that carrageenan and thrombin-induced aggregation are mediated by non-prostaglandin, phospholipase A2-derived products.
The decomposition of acidic and neutral cannabinoids in organic solvents
Authors: Smith R N , Vaughan C G 
Published: April 2011

Abstract
High-pressure liquid chromatography was used to study (a) the relative efficiencies of methanol, chloroform, light petroleum (B.P. 40–60°) and methanol-chloroform (9:1) for extracting neutral and acidic cannabinoids from cannabis resin; (b) the decomposition patterns of the resulting solutions under various storage conditions, and (c) the cannabinoid profile of a cross section through a block of cannabis resin. The results show that (a) methanol is the most effective extracting solvent of those tested; (b) acidic cannabinoids in solution decompose in darkness by varying amounts depending on the temperature, solvent, storage time and particular cannabinoid; (c) neutral cannabinoids in solution are relatively stable in darkness; (d) daylight causes appreciable decomposition of both acidic and neutral cannabinoids in solution, and (e) the cannabinoid profile of a resin is complex with lower levels of acidic material in the outer layers.
The distribution of components in the different size fractions of granules prepared from binary mixtures
Authors: Opakunle W O , Spring M S 
Published: April 2011

Abstract
Boric acid, sulphanilamide and citric acid have been mixed separately with lactose and then granulated by massing and screening. The granules have been fractionated by sieving and each fraction has been analysed for lactose content. The effect of premixing time, massing time, binder volume and ratio of components on the distribution of lactose between size fractions of granules prepared from lactose: boric acid mixtures has been investigated. Uneven distribution of lactose has been found for all blends examined. There is a premixing time and massing time that gives the optimum distribution of lactose for any given blend and binder volume. Increased binder volume in some cases improves granule uniformity. The proportion of lactose in the blend has a major effect on the distribution of this component in the granules, as does the particle size of the lactose. Granules prepared from blends of lactose with sulphanilamide and with citric acid were also examined for lactose distribution.
The pharmacology of benoxaprofen (2-[4-chlorophenyl]-α-methyl-5-benzoxazole acetic acid), LRCL 3794, a new compound with anti-inflammatory activity apparently unrelated to inhibition of prostaglandin synthesis
Authors: Cashin C H , Dawson W , Kitchen E Ann 
Published: April 2011

Abstract
Benoxaprofen is a potent and long-acting anti-inflammatory and antipyretic compound. Its anti-inflammatory activity has been demonstrated in carrageenan-induced oedema, in cellulose pellet granuloma and in both developing and established adjuvant arthritis tests in rats. Its antipyretic activity is greater than either aspirin or paracetamol in tests inducing pyrexia with yeast or ‘E’ pyrogen in rats and rabbits. Benoxaprofen has analgesic activity in tests where pain is accompanied by inflammation but not in other experimental models of pain. The weak prostaglandin synthetase inhibiting properties of this compound differentiate it from other acid anti-inflammatory compounds. The low ulcerogenic potential of benoxaprofen seen in animal models may be related to its relative inability to inhibit PG synthetase.
Differentiation of the dopamine mechanisms mediating stereotyped behaviour and hyperactivity in the nucleus accumbens and caudate-putamen
Authors: Costall Brenda , Naylor Robert J , Cannon Joseph G , Lee Theresa 
Published: April 2011

Abstract
A number of dopamine agonists were applied intracerebrally to the nucleus accumbens and caudate-putamen of rat in an attempt to differentiate the dopamine mechanisms in these nuclei which mediate hyperactivity and stereotyped behaviour. The major effect of dopamine was to induce hyperactivity from the nucleus accumbens and stereotypy from the caudate-putamen; N-n-propyl-norapomorphine induced hyperactivity and stereotypy from the nucleus accumbens whilst apomorphine induced a marked stereotypy from the caudate-putamen, modest stereotypy from the nucleus accumbens and no hyperactivity. In contrast to apomorphine, 2-(NN-dipropyl)amino-5,6-dihydroxy TN‡ induced a more marked stereotypy from the nucleus accumbens and, again, no hyperactivity. The major effect of 2-(NN-diethyl)amino-5,6-dihydroxy TN was to cause an intense hyperactivity from the nucleus accumbens and marked stereotypy from the caudate-putamen whilst the primary amine, 2-amino-5,6-dihydroxy TN induced hyperactivity and stereotypy from both areas. The marked hyperactivity and stereotyped responses were inhibited by haloperidol, but not by α- or β-blockers. These data would indicate that there may be different dopamine mechanisms in the nucleus accumbens and caudate-putamen for the mediation of hyperactivity and stereotyped behaviour.
Studies on the ethanol-induced changes in glycerolipid synthesis in rats and their partial reversal by N-(2-benzoyloxyethyl)norfenfluramine (benfluorex)
Authors: Pritchard P Haydn , Brindley David N 
Published: April 2011

Abstract
Rats were treated daily for 5 days with benfluorex (S-780) 50 mg kg−1 and 2 h after the fifth treatment were intubated with ethanol 5 g kg−1 or with isocaloric glucose. S-780 did not alter the absorption or oxidation of [1-14C]ethanol nor did it decrease the concentration of ethanol and its water soluble metabolites in the tissues examined. The rate of hepatic glycerolipid synthesis was measured in vivo using [14C]palmitate and [3H]glycerol and the accumulation of [14C]palmitate in various tissues was determined 4 h after intravenous injection. Ethanol treatment increased the relative rate of TG† synthesis in the liver and decreased the synthesis of PC, PE and PS + PI. The relative flux from PA to DG and TG was increased. These changes were reflected in the accumulation of [14C]palmitate in hepatic lipids and were obtained under conditions where the net rate of [14C]palmitate oxidation to 14CO2 was greater in those rats treated with ethanol instead of glucose. S-780 did not alter the oxidation rates over a 4 h period. Ethanol treatment increased the accumulation of [14C]palmitate in the PS + PI fraction of lung and decreased the proportion in PE. In kidney it increased the concentration of [14C]palmitate in TG, DG and PE and decreased the concentration in PC and PS + PI. Pretreatment of the rats with S-780 partially reversed the changes in palmitate accumulation in glycerolipids which were caused by ethanol. S-780 treatment also decreased the rate of hepatic TG synthesis from glycerol in the rats fed glucose. It increased the percentage recovery of [14C]palmitate in the livers and kidneys of glucose fed rats and decreased that in adipose tissue. This treatment decreased the proportion of [14C]palmitate recovered in the TG of the kidneys and lungs of these rats and increased the proportion in PI + PS. The results are discussed in relation to the mechanisms by which ethanol and S-780 are thought to interfere with glycerolipid synthesis.
The in vitro metabolism of 2-nitroso-1-phenylpropane dimer by fortified 9000g supernatants from rabbit liver
Authors: Beckett A H , Jones G R 
Published: April 2011

Abstract
2-Nitroso-1-phenylpropane dimer, a postulated metabolic product of amphetamine, was metabolized by fortified 9000 g supernatants from rabbit liver, mainly by oxidation on the carbon beta to the nitrogen to form a ‘β-hydroxylated nitroso dimer’. The corresponding nitro compound, ketone and alcohol were also products, the latter two but not the former being cofactor dependant. The nitroso compound was not metabolically reduced under the conditions used.
Application of orthogonal functions to the spectrophotometric determination of phenytoin and phenobarbitone in pharmaceutical preparations
Authors: Amer M M , Ahmad A K S , Hassan S M 
Published: April 2011

Abstract
Orthogonal polynomial functions have been used in the simultaneous determination of mixtures of phenytoin and phenobarbitone in pharmaceutical preparations. The mean recovery (9 determinations) and coefficient of variation were 100·0 ± 1·4% for phenobarbitone and 100·0 ± 1·3% for phenytoin. Neither the ΔA method of Pannerden & Fontein nor a ΔA modification of Vierordt's method of two-component analysis gave results of the same accuracy and precision as the proposed method.