bluuebunny/crossref_metadata_2025_split huggingface dataset:
Dose-dependent behavioural changes induced by apomorphine in selected members of a primate social colony
Authors: Schlemmer R Francis , Narasimhachari Nedathur , Davis John M 
Published: April 2011

Abstract
The effect of six acute doses of the dopamine receptor agonist apomorphine on non-human primate social and individual behaviour was studied in a social colony of four adult Stumptail macaques. Apomorphine was administered intramuscularly to 2 monkeys/day in doses ranging from 0·05 to 3·00 mg kg−1 15 min before a 1 h observation period. Apomorphine induced hyperactivity, hypervigilance, and stereotyped behaviour at doses of 0·50 mg kg−1 and greater in all 4 monkeys. In addition it also caused a dose-dependent disruption of normal behavioural patterns. Social grooming was eliminated while the submissive gestures were significantly increased. It also induced an increase in vocalizations and suppression of food forage behaviours. The results demonstrate the role of dopamine systems in the mediation of affiliative behaviour as well as motor behaviour in a primate species. Also, since similar behavioural changes are induced in this species during chronic (+)-amphetamine treatment, it is suggested that dopamine systems play a predominant role in amphetamineinduced behaviour in primates.
The effect of steroidal and non-steroidal antiinflammatory drugs on chronic muscle inflammation
Authors: Green A P , Mangan F R 
Published: April 2011

Abstract
Zymosan (400 μg) and thioglycollate medium (0·1 ml of 2·4% w/v) have each been shown to induce a chronic inflammation when injected into the hamstring muscle of the mouse. The inflammation is characterized by an increase in muscle weight and N-acetylglucosaminidase concentrations. The response is not inhibited by oral treatment with hydrocortisone, dexamethasone or naproxen, but is inhibited by the local injection of methylprednisolone. The relevance of this model to polymyositis and fibrositis is discussed.
Responses to arachidonic acid and other dilator agonists and their modification by inhibition of prostaglandin synthesis in the canine hindlimb
Authors: Morcillo E 
Published: April 2011

Abstract
The influence of indomethacin, in doses that completely inhibit the response to arachidonic acid, has been examined on canine hindlimb vascular responses to intra-arterial administration of bradykinin, histamine, nitroglycerin, isoprenaline and papaverine. The hindlimb was perfused at constant flow. Dose-response curves to intra-arterial administration of arachidonic acid (12 to 200 μg kg−1), bradykinin (0·4 to 100 ng kg−1), histamine (1·8 to 120 ng kg−1), nitroglycerin (15 to 100 ng kg−1), isoprenaline (12 to 100 ng kg−1) and papaverine (1·2 to 160 μg kg−1) (all n = 4) were compared before and 30 min after indomethacin (5 mg kg−1 i.v.). All the drugs produced dose-related decreases in hindlimb perfusion pressure. After indomethacin, responses for all dilator agonists except arachidonic acid, were significantly greater than control (P &lt; 0·05), both in terms of absolute (mmHg) or percent change. Doseresponse curves after indomethacin had a left upward shift compared with control. Arachidonic acid responses were completely blocked by indomethacin. These findings suggest that indomethacin produces a non-specific increase in responsiveness of the hindlimb vascular bed to dilator substances, except arachidonic acid. The data presented do not support the hypothesis that the peripheral vasodilatation produced by bradykinin, nitroglycerin and histamine could be mediated by endogenous prostaglandin release.
The granulation of ternary mixtures: the effect of the wettability of the powders
Authors: Jaiyeoba K T , Spring M S 
Published: April 2011

Abstract
Granules have been prepared by a standard method from ternary mixtures of lactose, boric acid and either sulphanilamide, heavy kaolin or salicylic acid, using an aqueous solution of polyvinylpyrrolidone as binder. The granules were examined for size distribution and for the work required to crush larger granules from each batch. For the same binder volume the mean granule sizes and resistance to crushing of the granules increased as the wettability of the third component increased. The detailed results are discussed in relation to powder wetting and the packing properties of powder mixtures.
Micellar properties and surface activity of some bolaform drugs in aqueous solution
Authors: Attwood D , Natarajan R 
Published: April 2011

Abstract
The micellar properties of a series of dicationic drugs with structures resembling those of the bolaform electrolytes have been examined using light scattering, surface tension and conductivity techniques. The compounds investigated included, demecarium bromide, ambenonium chloride, dequalinium acetate, distigmine bromide and chlorhexidine acetate. Demecarium and dequalinium formed micelles at critical concentrations of 9 times 10−3 and 4 times 10−3 mol kg−1 respectively. No significant association of chlorhexidine acetate could be detected, contrary to previous reports.
On the anomalous sorption behaviour of chlorhexidine with poly(2-hydroxyethyl methacrylate)
Authors: Plaut B S , Meakin B J , Davies D J G 
Published: April 2011

Abstract
General observations of solute: plastic interactions would suggest that the sorption of the cationic preservative, chlorhexidine, with poly (2-hydroxyethyl methacrylate) (PHEMA) is not only unexpected but also atypical in its properties. The polymer and preservative were investigated independently and the sorption of PHEMA with simple solutes, namely benzoic acid, benzocaine and aniline found to exhibit conventional properties. The single exception was the uptake of small amounts of benzocaine and aniline cations at acidic pH's. In order to elucidate the sorption characteristics of chlorhexidine a series of N1-(p-chlorophenyl)-N5-alkylbiguanide acetates were synthesized. The anomalous sorption behaviour observed between PHEMA and the bis biguanide, chlorhexidine, was also found to be characteristic of these monofunctional biguanide derivatives. The extent of the interactions increased with increasing alkyl chain length (R = methyl to n-octyl), this being interpreted in terms of an interaction binding mechanism via the biguanide functional group stabilized by van der Waal's forces between the alkyl chain and the polymer backbone. Atypical sorption behaviour was observed for simple organic cations, biguanide and N1-phenylbiguanide acetate with PHEMA, a possible inference being that this is a general characteristic of all cationic sorption with PHEMA.
Analgesic and other pharmacological activities of a new narcotic antagonist analgesic (-)-1-(3-methyl-2-butenyl)-4-[2-(3-hydroxyphenyl)-1-phenylethyl]piperazine and its enantiomorph in experimental animals
Authors: Nakamura Hideo , Ishii Katsumi , Yokoyama Yuichi , Motoyoshi Satoru , Natsuka Kagayaki , Shimizu Masanao 
Published: April 2011

Abstract
Of 1-cyclohexyl-4-[2-(3-hydroxyphenyl)-1-phenylethyl]piperazine (I) and its 1-(3-methyl-2-butenyl) derivative (II), the S(+)-isomers were analgesically more active than either their R (-)-isomers or their racemates, having 15 to 44 times the potency of morphine in mice and rats. R (-)-I had comparable analgesic activity to morphine R (-)-II to pentazocine in mice, rats and dogs and they were nearly equipotent with pentazocine in reversing some actions of morphine. The S (+)-isomers and racemates lacked this action. R (-)-II required about 10 times more naloxone to reverse its analgesic activity than was needed to antagonise the S (+)-isomers, morphine and pentazocine. The S (+)-isomers and racemates produce a typical Straub tail reaction and increased spontaneous locomotor activity in mice, but the R (-)-isomers did not. R (-)-II had no significant physical dependence liability in mice, rats and monkeys. From these results, it is suggested that the compounds show an uncommon stereoselectivity in comparison with morphine and its surrogates, and that R (-)-II is worth investigating further as a narcotic antagonist analgesic.
The effects of nefopam on blood acid-base status in the rabbit: interactions with morphine in the mouse and rabbit
Authors: Stainthorp S F , Morton A K , Pleuvry B J 
Published: April 2011

Abstract
Nefopam, a non-narcotic analgesic, had only minor effects upon the blood pH, Pco2 and standard bicarbonate of the conscious rabbit. In contrast morphine caused a dose-dependent increase in Pco2 and standard bicarbonate. When nefopam was administered in conjunction with morphine (2·5 mg kg−1 and 1 mg kg−1 i.v. respectively) the increase in Pco2 was greater than with morphine alone. Nefopam also increased the antinociceptive and respiratory frequency depressant effects of morphine in the mouse.
Age related changes in the clearance and oral absorption of sodium cromoglycate in the developing albino rat
Authors: Smith Dennis A , Fisher Anthony N 
Published: April 2011

Abstract
A dual radioisotope method was used to investigate the clearance and oral abso***rption of sodium cromoglycate. Radiolabelled sodium cromoglycate was administered orally at a dose of 100 mg kg 1 (14 C-labelled) and simultaneously subcutaneously at a dose of 2 mg kg−1 (3 H-labelled) to rat pups 5, 9, 14, 20, 29 and 75 days old. Blood concentrations of 14 C and 3 H were measured at intervals for 24 h after dosing. Since the compound is not metabolized the blood concentrations of 14 C were taken as a measure of the sodium cromoglycate absorbed orally and the blood concentrations of 3 H as a measure of the subcutaneously administered material. Using the area under the oral 14 C blood curve (AUC) as an index of bioavailability, the calculated bioavailability of sodium cromoglycate (692·9−945·9 min μg ml−1) in 5, 9 and 14 day old pups was 4–8 times greater than that observed (61·0-118·8 min μg ml−1) in 20, 29 and 75 day old pups. The blood clearance of sodium cromoglycate was increased four-fold in 75 day old animals (43·9 ml min−1 kg−1) and three-fold in 20 and 29 day old pups when compared to the clearance in 5, 9 and 14 day old pups. The clearance in 5, 9 and 14 day old pups was relatively constant (10·8 − 9·9 ml min−1 kg−1). In rats less than 14 days old the systemic absorption of sodium cromoglycate after oral administration was 2–3 times greater (6·8-9·2%) than in rats aged 20, 29 or 75 days old (2·7-3·3%). The reduction in oral bioavailability of sodium cromoglycate as the pups grew older was, therefore, due to both an increased blood clearance and a decreased absorption of the compound.
Regional distribution of an opioid mechanism in the guinea-pig isolated intestine
Authors: KROMER W , PRETZLAFF W , WOINOFF R 
Published: April 2011

Abstract
Opioid receptor blockade by naloxone enhanced peristalsis in isolated segments from the guinea-pig duodenum, jejunum and ileum, increasingly aborally. Thus, an increase in the influence of an intrinsic opioid mechanism may be responsible for the decrease in the level of peristaltic activity, observed aborally. However, the peristalsis of ileal segments which worked against their closed distal end was enhanced by naloxone to a similar degree as normal peristalsis.
On the pharmacological actions of a diuretic, fenquizone, with particular reference to its site of action
Authors: FERRANDO CHRISTINA , FOY J M , PRATT C N F W , PURVIS J R 
Published: April 2011

Abstract
The pharmacological actions of a diuretic drug, fenquizone have been investigated and its effects compared with well characterized diuretics in rats, mice and rabbits. Changes in sodium and potassium excretion and urine volume were similar in magnitude and duration to those of the thiazide diuretics over dose range 0·05–100 mg kg−1. Free water clearance in rabbits was decreased indicating an action at the cortical diluting site in the nephron and since free water reabsorption was relatively unaffected it appears unlikely to have actions at other sites. Calcium and phosphate excretion studies also suggested that the predominant effects are those occurring at the cortical diluting segment of the nephron. Additional parameters not affected by the drug were blood flow to the cortex and medulla of the kidney (and other major organs), plasma glucose concentration and plasma urate concentration.
Bifluranol, a novel fluorinated bibenzyl anti-androgen, its chemistry and disposition in different animal species
Authors: POPE D J , GILBERT A P , EASTER D J , CHAN R P , TURNER J C , GOTTFRIED S , PARKE D V 
Published: April 2011

Abstract
The synthesis of bifluranol, a new fluorinated bibenzyl anti-androgen, and of 3H-labelled bifluranol is described. The absorption, distribution and excretion of bifluranol has been studied in mouse, rat, ferret and dog; it is readily absorbed following oral administration, but blood concentrations of the drug are low due to hepatic uptake and biliary excretion. Enterohepatic re-circulation occurs, but the drug is excreted primarily in the faeces and only small amounts appear in urine. This pattern of disposition and excretion is similar to that reported elsewhere for the bibenzyl, hexoestrol, and for the stilbene, diethylstilboestrol.
The acetylenic monoamine oxidase inhibitors clorgyline, deprenyl, pargyline and J-508: their properties and applications
Authors: FOWLER C J , ORELAND L , CALLINGHAM B A 
Published: April 2011

Abstract
The article presents a short review of some of the properties of the acetylenic inhibitors of monoamine oxidase currently under investigation: clorgyline, (—)-deprenyl, pargyline and J-508. Their substrate-selective inactivation, mechanism of inhibition, titration and pharmacology with respect to monoamine oxidase are critically discussed.
Effects of diethyl ether anaesthesia on the pharmacokinetics of antipyrine and paracetamol in the rat
Authors: JOHANNESSEN W , GADEHOLT G , AARBAKKE J 
Published: April 2011

Abstract
The effects of two anaesthetic procedures: continuous administration of ether throughout the periods of drug infusion and blood sampling, and brief ether administration (5 min) before drug infusion were examined. Continuous ether reduced total clearance, β, and k10 for both drugs, and in addition Vc and Vβ for antipyrine. Brief ether anaesthesia had no effect on antipyrine kinetics, but caused a decrease in total clearance, k10 and Vβ of paracetamol. The rates of distribution and redistribution of the drugs were unchanged by ether. The data suggest that ether interferes with the hepatic conjugation of paracetamol and may interfere with the hepatic oxidation of antipyrine and therefore should not be used as an anaesthetic when the kinetics of drugs with short elimination half-lives are studied. It may be used for drugs with longer half-lives.
The cracking of film coatings on film-coated tablets—a theoretical approach with practical implications
Authors: ROWE R C 
Published: April 2011

Abstract
A theoretical approach of film cracking is presented using equations which allow for the calculation of both the internal stress in a film coating due to shrinkage of the film on evaporation of the solvent and the thermal stress due to differences in the thermal expansion of the film coating and tablet substrate during changes in temperature arising out of the coating processes. The practical implications of this approach in film formulation are discussed with particular reference to the choice of tablet core formulation, the grade of polymer used, the type and concentration of both plasticizers and pigments and the solvent system used in the coating process.
Inhibition of lymphocyte transformation by mepacrine and chloroquine
Authors: TRIST D G , WEATHERALL M 
Published: April 2011

Abstract
Mepacrine inhibited the uptake and the incorporation of leucine, thymidine and uridine into acid-insoluble material in human lymphocytes stimulated by phytohaemagglutinin (PHA) in vitro. The IC50 for each uptake was of the order of 2μM. Mepacrine was inhibitory if applied at any time up to 48 h after PHA. The inhibition differed from that produced by colchicine and prostaglandin E1. The dose-response curve was steep, nearly all incorporation being inhibited by 2 × IC50. Chloroquine also had a steep dose-response curve, was about one-fifth as potent as mepacrine and was maximally effective in the first 6 h after PHA.
Plasma protein binding of fentanyl
Authors: BOWER SUSANNE 
Published: April 2011

Abstract
Whole plasma of 15 normal volunteers bound 79·16% ± 0·16 s.e. (n = 45) of fentanyl, at a concentration of 0·6 ng ml−1. Measurement was by equilibrium dialysis at 37°C, pH 7·4. The largest contribution to binding appears to be due to serum albumin, since 45·52% ± 0·40 s.e. (n = 3) of fentanyl was bound to a solution of purified albumin at a concentration of 46 g litre−1 in buffer. Physiological concentrations of isolated very low density, low density and high density lipoprotein fractions in buffer bound 18·39% ± 0·65 s.e.; 39·14% ± 0·42 and 21·18% ± 0·51 (n = 15) respectively. A significant correlation was found between percent binding and serum albumin concentration (r = 0·745, P = 0·0022) and oestrogen and progestagen therapy (r = 0·766, P = 0·0014). There was no significant correlation with fasting serum cholesterol, triglyceride, age, sex or the concentration of total protein minus albumin. Binding to fibrinogen and α1-acid glycoprotein did not occur. Binding increased with increasing pH, temperature and ionic strength of the buffer. The results were compatible with hydrophobic bond formation between fentanyl and proteins. Fentanyl concentration did not affect the percent bound to whole plasma or the protein fractions over a range of 0·6 ng-10 mg ml−1. Dilution of plasma with buffer gave a linear relation of percent bound or free to log plasma dilution. The binding of fentanyl to pooled plasma of the normal subjects was not affected by a wide variety of anionic, cationic and uncharged drugs when these were tested at a concentration of 20 μg ml−1. At higher concentrations, aspirin, phenylbutazone and quinidine caused inhibition of fentanyl binding. A linear relation was found between percent bound and concentration of the inhibitory ligand. For aspirin, r = 0·873, P &lt;0·01; for phenylbutazone, r = 0·81, P &lt;0·05; and for quinidine, r = 0·982, P &lt;0·01. Aspirin and phenylbutazone inhibited binding of fentanyl to albumin, while quinidine caused inhibition of binding to lipoproteins of all three densities, but not to albumin. Changes in the concentrations of the common ions of plasma (except H+), of free fatty acids and of creatinine did not affect fentanyl binding to whole plasma. 8 M urea reduced binding by 25% of the normal value.
Effects of cyclodextrins on chlorpromazine-induced haemolysis and central nervous system responses
Authors: UEKAMA K , IRIE T , SUNADA M , OTAGIRI M , IWASAKI K , OKANO Y , MIYATA T , KASÉ Y 
Published: April 2011

Abstract
Cyclodextrins (CyDs) protected the human erythrocytes from haemolysis induced with chlorpromazine (CPZ) in isotonic solution, depending upon the magnitude of the stability constant of CPZ-CyD complexes (β-&gt; γ-&gt; α-CyD). From the observations of CPZ uptake into erythrocytes and changes in surface activity of CPZ, the protective effects of CyDs in vitro appeared to be due to the decrease in effective haemolytic concentration of CPZ through inclusion complex formation rather than the direct interaction of CyDs with the erythrocyte membrane. The effect of β-CyD on some central nervous system (c.n.s.) actions of CPZ in rats was also investigated to see if there were any advantages in the use of β-CyD complexes given by injection. The results suggest that β-CyD does not alter the time-course or magnitude of the effects of CPZ on the c.n.s.
Rectal absorption of some glycosaminoglycan sulphates and heparin in rats
Authors: STANZANI L , MASCELLANI G , CORBELLI G P , BIANCHINI P 
Published: April 2011

Abstract
A standardized extract of glycosaminoglycan sulphates containing heparin, with a low affinity for antithrombin III, and a commercial heparin were administered to rats, by the rectal route. When the glycosaminoglycan sulphates were given in oil emulsion with sodium laurylsarcosinate as surfactant, 1 mg kg−1 and 3 mg kg−1 were sufficient for the clearing and anticoagulant activities respectively. The rectal absorption of glycosaminoglycans after dosing with a suitable ‘promoter' produced dose-dependent effects and their kinetics were comparable to those obtained after intramuscular administration. The oil emulsion improved the bioavailability of glycosaminoglycan sulphates at least 20 times.
Electrostatic charge interactions in ordered powder mixes
Authors: STANIFORTH J N , REES J E 
Published: April 2011

Abstract
A method is described for measuring the electrostatic charge generated in powders following contact with a plane substrate. The method uses a Faraday well connected to an electrometer and allows the specific charge of powders to be determined. Of the various drugs and excipients studied, most charged electronegatively following contact with glass surfaces, but became electropositive after contact with polyethylene surfaces. The charge interactions of drug and excipient powders modified the behaviour of ordered mixes formed in similar conditions to those of charge measurement. Powders with like charges formed less stable ordered mixes than those in which drug and excipient particles carried opposite charges. Following triboelectrification in an air cyclone constructed of brass, powders had charges at least 100 times greater than those formed after contact with glass surfaces. Optimization of the triboelectric charging conditions allowed ordered mixes to be prepared in which a maximum electronegative charge was applied to the excipient whilst the drug was given a maximum electropositive charge. Studies of segregation/stability showed that ordered mixes subjected to triboelectrification were less prone to segregation than uncharged powders.
Optical studies on the specific interaction of dipyridamole with α1-acid glycoprotein (orosomucoid)
Authors: EL-GAMEL SAFAA , WOLLERT The late UWE , MÜLLER WALTER E 
Published: April 2011

Abstract
The interaction of dipyridamole with α1-acid glycoprotein was investigated by circular dichroism and ultraviolet absorbance measurements as well as by equilibrium dialysis experiments. Dipyridamole is bound to the protein via one site of extremely high affinity and by at least one site of considerably lower affinity. Only the association of dipyridamole with the high affinity site produces typical extrinsic Cotton effects. As a result of experimental observations it is concluded that the high affinity site is located in a hydrophobic protein structure of the glycoprotein.
Three-ply walled w/o/w microcapsules formed by a multiple emulsion technique
Authors: WARBURTON NATALIE J MORRIS AND B 
Published: April 2011

Abstract
A new method of microencapsulation is described. Interfacial rheological studies had shown the formation of a rigid bipolymer film at the interface between an aqueous solution of a water-soluble polymer and a non-aqueous solution of an oil-soluble polymer. This led to the idea that small spherical bodies might be formed on making a w/o/w emulsion from these solutions. The present work has shown that ethyl cellulose/acacia microcapsules are formed when the organic solvent ethyl acetate is removed from the multiple emulsion drops. These microcapsules may be obtained as a free-flowing powder.
Effects of paraffin coatings on the shearing properties of lactose
Authors: IRONO CECILIA I , PILPEL N 
Published: April 2011

Abstract
An annular shear cell has been employed to measure the shearing properties of lactose powder coated with up to 104 mol g−1 of powder of a series of paraffin hydrocarbons. The angle of internal friction, Δ, of the coated powders was independent of their packing density. The shearing properties of the powders depended on the concentration, the viscosity and thickness of the coating material.