bluuebunny/crossref_metadata_2025_split huggingface dataset:
Mianserin: is the intraperitoneal route of administration the best?
Authors: Sugrue Michael F 
Published: April 2011

Abstract
A 1 h pretreatment with s.c. mianserin (0·5 mg kg−1) markedly blunted the oedema of the rat paw induced by the subplantar injection of 5-HT (5 μg). In contrast, i.p. mianserin (same dose) failed to modify 5-HT-induced oedema. However, pretreatment with SKF-525-A (40 mg kg−1) resulted in a profound potentiation of the action of i.p. mianserin, the effect of the combination of SKF-525-A and i.p. mianserin rivalling that of s.c. mianserin. It is concluded that i.p. mianserin is metabolized by the rat liver to compounds which possess a reduced propensity to block peripheral 5-HT receptors and that the i.p. route of administration is not to be recommended when mianserin is being studied as a 5-HT receptor antagonist in the rat.
An evaluation of the relative importance of formulation and process variables using factorial design
Authors: Sanderson I M , Kennerley J W , Parr G D 
Published: April 2011

Abstract
A factorial design method for assessing the relative importance of various formulation and process factors and their interactions in model paracetamol tablets is described. The design was a 2 times 2 × 2 times 3 type using mixing time, starch concentration, drug particle size and compaction pressure respectively. The starch concentration was the most significant factor in affecting the dissolution rate but the larger drug particle size also gave a significant increase in drug release rate. Interactions between starch concentration and drug size and between these and mixing time were also observed. The most significant factor affecting the tensile fracture stress of the tablets was the mixing time, followed in order by the drug particle size, starch concentration and compaction pressure.
Convergent flow analysis in the extrusion of wet powder masses
Authors: Harrison P J , Newton J M , Rowe R C 
Published: April 2011

Abstract
The angle of convergent flow which occurs when a wet powder mass is extruded through a die has been assessed by the inclusion of dyes in the mass before extrusion. The angles obtained are dependent on the powder components and their proportion, the moisture level, and the ratio of the dead space to the area of open die. The method allows assessment of the type and ease of flow which occurs during extrusion.
Structure-activity in the carrageenans: iota-carrageenan and experimental oedemagenic activity
Authors: Anderson W , Harthill J E , Zeitlin I J 
Published: April 2011

Abstract
The oedemagenic activities of several iota-carrageenans from Eucheuma spinosum have been compared using the rat hindpaw model. From the parent ι-carrageenan of weight average molecular weight 541 100 an acid-degraded ι-carrageenan (&#x004d;̄w = 20 300) was obtained which on fractionation yielded five ι-carrageenans &#x004d;̄w ranging from 73 700 to 4 600. The oedemagenic activity of ι-carrageenan resided in the fraction of &#x004d;̄w = 73 700, the parent undegraded high molecular weight ι-carrageenan being no more active and fractions of lower molecular weight being inactive. Fractionation was based on differential solubilities of the barium salts of the fractions in water and aqueous ethanol and was probably determined by aspects of primary structure in addition to molecular weight.
Anti-inflammatory and anti-ulcer properties of hypolaetin-8-glucoside, a novel plant flavonoid
Authors: Villar A , Gasco M A , Alcaraz M J 
Published: April 2011

Abstract
The anti-inflammatory, analgesic and anti-ulcer activities of a novel flavonoid, hypolaetin-8-glucoside, obtained from Sideritis mugronensis, have been tested in the rat. The flavonoid was more potent than phenylbutazone in suppressing the acute phase of adjuvant-carrageenan-induced inflammation, but had less effect in the prolonged inflammatory phase. However, unlike phenylbutazone, it did not cause gastric erosions. Both compounds were equiactive in inhibiting the development of carrageenan-induced abscesses, whereas phenylbutazone had greater analgesic activity in tests on pressure pain threshold. The flavonoid and cimetidine both prevented the formation of cold-restraint induced gastric lesions, but cimetidine was more potent. These results show that hypolaetin-8-glucoside combines both anti-inflammatory and anti-ulcer properties and suggest that it may offer useful alternatives to anti-inflammatory drugs of the aspirin type.
The energetics of the interaction of piroxicam with plasma albumin
Authors: Oyekan A O , Thomas W O A 
Published: April 2011

Abstract
The thermodynamics of the binding of piroxicam to human and bovine plasma albumins revealed the reactions to be spontaneous and exothermic with bond strengths indicating the involvement of hydrogen and hydrophobic bonds. The association constants (K) decreased as temperature increased for both human serum albumin (HSA) and bovine serum albumin (BSA); and at all the temperatures in this study, K values obtained for BSA were higher (except at 36 °C) but not the bound fraction of piroxicam (β) and the quantity of binding (V). Scatchard plots of the data indicated at least two classes of binding sites.
Inhibition of lipid absorption by non-ionic hydrophobic surfactant Pluronic L-81, and its benzoyl esters
Authors: Bochenek Wieslaw J , Slowinska Regina , Kapuscinska Barbara , Mrukowicz Miroslaw 
Published: April 2011

Abstract
The benzoyl ester of Pluronic L-81 (BEP) has been purified on an aluminium oxide column and fractionated on the basis of its mobility characteristics into three fractions, BEP I, II and III. Absorption studies were made with rats fed by Ravage a lipid preparation containing [14C]triolein and [3H]lcholesterol (control animals) and one of the fractions or Pluronic L-81, or crude BEP. After 4 h the amount of lipid absorbed and transported was calculated as the difference between the dose fed and the amount of lipid recovered from the gastric and intestinal luminal contents and intestinal mucosa. Pluronic L-81 was the most effective in inhibiting absorption of triolein but it did not inhibit absorption of cholesterol. BEP-II was almost as effective in inhibiting the absorption of triolein and also inhibited absorption of cholesterol. Crude BEP was less effective and BEP-I and III had only limited activity. Inhibition of triolein absorption by Pluronic L-81 may be partly related to its delaying action on gastric emptying. As purified BEP preparations had practically no effect on gastric emptying, their inhibiting activity involved intestinal mechanisms of lipid absorption.
Behavioural and biochemical effects in C57BL/6J mice after a prolonged treatment with the δ-opiate antagonist ICI 154129
Authors: Volterra A , Brunello N , Cagiano R , Cuomo V , Racagni G 
Published: April 2011

Abstract
A long term treatment with the δ-selective opiate antagonist NN-bisallyl-Tyr-Gly-Gly-ψ-(CH2S)-Phe-Leu-OH (ICI 154129) produces an increase in the number of δ-opiate binding sites, whereas the same treatment with the non selective opiate antagonist naloxone results in an enhancement of both μ- and δ-binding sites. This biochemical effect in naloxone-pretreated mice is paralleled by a more pronounced increase in locomotor activity induced by a challenge dose of morphine. In contrast, no difference in the effect of morphine was seen in ICI 154129-pretreated mice with respect to control. These data suggest that the locomotor response to morphine in C57 mice is not mediated through δ-opiate receptors.
Norzimelidine, a metabolite of a highly selective 5-hydroxytryptamine uptake inhibitor, can inhibit the uptake of noradrenaline in-vivo
Authors: Pawlowski Leszek , Mazela Halina 
Published: April 2011

Abstract
Zimelidine and norzimelidine were tested for their ability to counteract reserpine (2·5 mg kg−1). or apomorphine (1–16 mg kg−1)-induced hypothermia and to potentiate TRH (40 mg kg−1)-induced hyperthermia in mice. Norzimelidine produced positive results in all three tests, behaving like a weak NA uptake inhibitor. Zimelidine was practically inactive. We conclude that the weak inhibitory effect of norzimelidine on the uptake of NA (in-vitro experiments) may be of importance for its pharmacological action and for the clinical action of zimelidine.
The effect of sinusoidal vibration on the uniformity of packing of powder beds
Authors: Woodhead P J , Newton J M 
Published: April 2011

Abstract
Sinusoidal vibration, at a number of defined sets of conditions, has been applied to packings of certain particle size fractions of lactose. The distribution of local porosity within these vibrated packings was determined using a gamma-ray attenuation technique, and could be compared with porosity data for samples not subjected to vibration. It was found that the application of vibration in a vertical mode markedly increased the uniformity of packing; horizontal vibration was less effective in this respect. The relationship between local porosity and position with a packing, observed in most non-vibrated samples, was generally absent from vibrated packings.
Representation and quantitation of the binding interaction between prednisone, prednisolone and corticosteroid binding globulin
Authors: Unadkat Jashvant D , Rowland Malcolm 
Published: April 2011

Abstract
The interaction between prednisone and prednisolone (0–500 ng ml−1) for binding sites on corticosteroid binding globulin (CBG) in rabbit plasma has been investigated. The fraction unbound of each steroid rose markedly with increasing concentration at low concentrations (250 ng ml−1), tending to a plateau (0·29 prednisone, 0·15 prednisolone) at the higher concentrations (250–500 ng ml−1), indicating both saturation of CBG and the importance of binding to albumin in higher concentrations. A method is proposed of representing graphically the prednisone–prednisolone–protein interaction in three dimensions.
Indirect inhibition of vitamin K epoxide reduction by salicylate
Authors: Hildebrandt E , Suttie J W 
Published: April 2011

Abstract
Salicylate antagonizes the vitamin K-dependent biosynthesis of clotting factors in the rat and produces an elevation of the ratio of vitamin K epoxide to vitamin K in the liver. Vitamin K epoxide is reduced to vitamin K by a vitamin K epoxide reductase, and 1 mm salicylate was required to cause a 50% inhibition of the dithiothreitol-dependent in-vitro reduction of vitamin K epoxide by this enzyme. This enzyme was, however, inhibited 50% by as little as 70–80 μm salicylate when reducing equivalents for the reaction were furnished by endogenous cytosolic reductants. This effect on the cytosolic reductant supply was shown to be unrelated to a previously demonstrated inhibition of DT-diaphorase by salicylate. The concentrations of salicylate at which significant inhibitory effects are exerted in-vitro (50–100 μm) are below the 200 μm levels observed in the livers of rats given an anticoagulating dose of salicylate.
Age-related changes in benzylamine oxidase activity in rat tissues
Authors: Danh Hung Cao , Benedetti Margherita Strolin , Dostert Philippe , Mousset Arlette 
Published: April 2011

Abstract
Brain, liver, heart, lung, kidney and duodenum benzylamine oxidase (BZAO) activities were measured from young and old rats. Protein content was found to decrease in liver (-17%), kidney (-20%) and duodenum (-17%) but remained unchanged in brain, heart and lung of old rats compared with that of young rats. A significant decrease (-41%) of BZAO activity was found in lung whereas a significant increase of enzyme activity was found in brain (+49%) and kidney (+25%) and no change was found in heart and duodenum of old rats. BZAO was not detected in either young or old rat liver. Kinetic analysis for lung BZAO activity of old rats showed that Vmax was decreased but Km was unchanged in comparison with that of young rats. Since, as we have shown previously, MAO-A and -B activity in lung of old rats was also found to be decreased, the decrease of lung BZAO activity with increasing age merits further investigation, lung playing an important role in removing amines from the circulation.
Cmc of mixtures of chlorpromazine hydrochloride and polysorbate 80 determined by pH measurements
Authors: Paiement J 
Published: April 2011

Abstract
The cmc of mixtures of chlorpromazine hydrochloride and polysorbate 80 was determined by pH titration. The values thus obtained coincided with those determined by the surface tension method. The mixtures studied could be divided into two groups according to the shape of their pH concentration curves. For mixtures containing less than 0·8 mole fraction chlorpromazine, the curves suggest that some interaction occurs in the premicellar concentration range. For mixtures containing more than 0·8 mole fraction chlorpromazine, the curves suggest that the micellar process occurs in more than one step.
The involvement of opiate receptors in the effects of trimebutine on intestinal motility in the conscious dog
Authors: Fioramonti J , Fargeas M J , Bueno L 
Published: April 2011

Abstract
The effects of intravenous (i.v.) vs intracerebroventricular (i.c.v.) administration of trimebutine on the motility of the small intestine and colon of fasted dogs were assessed using chronic electromyography. Trimebutine, injected intravenously, stimulated small intestinal motility, by inducing a propagated phase of regular spike activity, and inhibited colonic motility for some 4 h. These effects were not reproduced by i.c.v. administration which disrupted the cyclic motor profile of the small intestine for about 2·5 h and did not modify colonic motility. The stimulation of the small intestine motility induced by i.v. administration of the drug was blocked by previous i.v. but not by i.c.v. administration of naloxone. It was concluded that in the dog, the effects of trimebutine on the small intestine but not on the colon, involve peripheral opiate receptors.
Increased number of brain benzodiazepine receptors after in-vivo administration of estazolam to rats
Authors: Mennini T , Gobbi M , Garattini S 
Published: April 2011

Abstract
Estazolam significantly increased the Kd of [3H]flunitrazepam in-vitro, like other benzodiazepines (BDZs) acting competitively at the receptor site. At variance with other BDZs, estazolam significantly raised the Bmax for [3H]flunitrazepam, at concentrations lower than its Ki for BDZ receptors. This effect may be responsible for the observed increase in [3H]diazepam binding after in-vivo administration of estazolam to rats.
On the role of the baseline firing rate in determining the responsiveness of cingulate cortical neurons to iontophoretically applied substance P and acetylcholine
Authors: Jones Roland S G , Olpe Hans-Rudolf 
Published: April 2011

Abstract
The relationship between baseline firing rate and the magnitude of excitatory responses to iontophoretically applied substance P (SP) and acetylcholine (ACh) was determined for neurons in the anterior cingulate cortex of the rat. Whereas the size of responses to ACh was positively correlated with the level of ongoing neuronal activity, no correlation, either positive or negative, could be demonstrated for responses to SP. It seems unlikely that the excitatory effects of SP in this brain area result from release of endogenous ACh.
Chronic treatment with electroconvulsive shock prevents the salbutamol-induced hypoactivity in rats
Authors: Przegaliński E , Siwanowicz J , Bigajska K , Baran L 
Published: April 2011

Abstract
Several lines of evidence (binding studies, reduced responsiveness of brain adenylate cyclase to noradrenergic stimulation) indicate that chronic treatment with electroconvulsive shock (ECS) induces down-regulation of central β-adrenoceptors. The effect of acute and chronic (10 days) treatment with ECS on salbutamol-induced suppression of exploratory activity in rats has been examined. This effect was prevented by chronic but not by acute treatment with ECS. Chronic treatment with ECS did not affect exploratory activity. The salbutamol-induced hypoactivity is mediated through central β-adrenoceptors (antagonistic effect of (-)-propranolol but not (+)-propranolol or practolol), so the results may be regarded as functional evidence at the behavioural level for the down-regulation of β-adrenoceptors produced by chronic treatment with ECS.
Relative absorption of tryptophan ethyl ester amide derivatives with various fatty acid chains in the dog
Authors: Tse Francis L S , Christiano Juliet R , Talbot Kenrick C 
Published: April 2011

Abstract
Sandoz compound 57–118 is a mixture of tryptophan ethyl ester amide derivatives (analogues I–V) possessing one of five fatty acid chains which differ in chain length, configuration, or the degree of unsaturation. The relative absorption of each of the five analogues was investigated in the dog following single oral doses of the homologous mixture containing one 14C labelled analogue. It was shown that the extent of absorption of analogue I and its trans-homer, II, both with a mono-unsaturated fatty acid chain, were similar. An additional double bond in the fatty acid moiety (analogue III) facilitated gastrointestinal absorption. On the other hand, saturated fatty acid chains appeared to render the molecule less efficiently absorbed; the extent of absorption being dependent on the chain length. Thus, analogue V with 16 carbon atoms on the fatty acid chain was better absorbed than IV with 18.
Plasma concentrations of clobazam and its N-desmethyl metabolite; protection against pentetrazol-induced convulsions in mice
Authors: Haigh J R M , Gent J P , Calvert R 
Published: April 2011

Abstract
The anticonvulsant effects of acute administration of clobazam and its principal metabolite N-desmethyl-clobazam were studied in mice. Pentetrazol, given by slow intravenous infusion 1 or 2 h after the anticonvulsant dose, was used as the convulsant stimulus. Log dose response relationships for both clobazam and N-desmethylclobazam appeared linear, but there was no correlation between plasma concentrations of clobazam and protection. However, correlation between plasma concentrations of N-desmethylclobazam and protection was significant in both cases.
The hydroxy-hexanydronaphthoxazines: a new group of very potent and selective dopamine agonists
Authors: Horn A S , Hazelhoff B , Dijkstra D , de Vries J B , Mulder T B A , Timmermans P , Wynberg H 
Published: April 2011

Abstract
Replacement of the pyrrole ring system in the dopaminergic oxaergolines (e.g. RU 29717) by a phenolic OH group leads to the hydroxy-hexahydronaphthoxazines, a new group of potent dopamine agonists which exhibit increased selectivity due to their lower affinity for adrenergic and 5-HT receptors.
The effect of different oils on the absorption of probucol in the rat
Authors: Palin K J , Wilson C G 
Published: April 2011

Abstract
The effect of oily vehicles on the gastrointestinal absorption of the hypocholesterolaemic agent probucol has been investigated in the rat. The plasma concentration was determined following its administration in arachis oil (peanut oil), Miglyol 812 (fractionated coconut oil) and liquid paraffin. The total absorption of the drug, calculated as the area under the plasma concentration time curve, was significantly greater for the arachis oil formulation than with the other vehicles. The drug was selectively absorbed via the lymphatic system, lymph drug concentrations being highest following co-administration of arachis oil.
Radioimmunoassay of benzoylecgonine in samples of forensic interest
Authors: Robinson Katherine , Smith R N 
Published: April 2011

Abstract
A simple and economical radioimmunoassay for benzoylecgonine in blood or urine is described. Haemolysis, decomposition, common anticoagulants and sodium fluoride do not affect the results. A commercially available antiserum is used at a dilution of 1:600. The tracer is radioiodinated p-hydroxybenzoylecgonine. It is prepared by reacting p-acetoxybenzoic anhydride with methyl ecgonine followed by mild hydrolysis and radioiodination by the Iodo-gen method. The product is purified on a disposable silica cartridge and has a specific activity of about 30 TBq mmol−1. Polyethylene glycol is used to separate the bound and free fractions in the assay. The range of the dose-response curve is 0–400 ng ml−1 benzoylecgonine. The assay is largely specific for benzoylecgonine. Cocaine, ecgonine, methylecgonine and cinnamoyl cocaine have slight or negligible cross-reactivities. The inter-assay coefficient of variation is 7·5% and the recovery of benzoylecgonine from ‘spiked’ blood is 103%. The ‘cut-off’ is 20 ng ml−1 benzoylecgonine for both blood and urine. Radioimmunoassay and high-performance liquid chromatography results agree well.
Studies into the mode of action of non-steroidal anti-inflammatory drugs using a model of facsimile synovium
Authors: Sedgwick A D , Sin Y M , Mackay A R , Al-Duaij A , Willoughby D A 
Published: April 2011

Abstract
The effect of non-steroidal anti-inflammatory drugs on inflammation produced in the 6-day old air pouch by carrageenan or calcium pyrophosphate crystals has been examined. The system is a very reproducible way of studying the cellular and vascular components of inflammation. Non-steroidal drugs have different profiles of activity when tested on the inflammation produced with the two irritants. In general, however, the tested compounds showed similar activity on individual models.
AD-1590, a potent antagonist of lipopolysaccharide-induced fever in rabbits
Authors: Nakamura Hideo , Yokoyama Yuichi , Seto Yasuhiro , Kadokawa Toshiaki , Shimizu Masanao 
Published: April 2011

Abstract
The antipyretic activity of AD-1590 (2-[8-methyl-10,11-oxodibenz[b,f]oxepin-2-yl]propionic acid), a non-steroidal anti-inflammatory drug with a novel chemical structure, was investigated in rabbits with lipopolysaccharide (LPS)-induced fever and monkeys with leucocytic pyrogen-induced fever. AD-1590 produced a dose-related inhibition of the LPS-fever at oral doses of 0·1 mg kg−1 or more (ED50 = 0·089 mg kg−1). Its potency was 10–12, 20–35, 100–170, 400–540, &gt;1500 and &gt;2000 times that of ketoprofen, diclofenac sodium, indomethacin, ibuprofen, mefenamic acid and aspirin, respectively. The fever caused by leucocytic pyrogen was significantly inhibited by intravenous administration of 0·1–0·2 mg kg−1 of AD-1590. AD-1590 (10 mg kg−1 oral or i.v.) did not affect body temperature in afebrile rabbits or monkeys. These results suggest that AD-1590 shows a potent antipyretic activity in the rabbit and monkey and is a potent antagonist of LPS-fever.
A 1H nmr study of the amide-bond conformational equilibrium in pirenzepine
Authors: Feeney J , Pascual C 
Published: April 2011

Abstract
The hindered rotation about the exocyclic amide bond of pirenzepine has been studied using 1H nuclear magnetic resonance spectroscopy. The ratios of the two slowly interconverting conformations (1:1·76 at 2 °C and 1:2·37 at 30 °C) and the rate of interconversion (1 ± 0·5 s−1 at 20 °C and 247 ± 20 s−1 at 80 °C with ΔG80 = 71 KJ mol−1) have been measured at various temperatures. The observed rapid rates of interconversion allow us to eliminate the rate of conformational selection of forms II and III as a major contributor to the slow phase of the binding kinetics observed when pirenzepine binds to muscarinic receptors from rat brain (Stockton, Birdsall, Hulme and Burgen, unpublished results).
Polymorphic behaviour of chloroquine diphosphate
Authors: Van Aerde Ph , Remon J P , De Rudder D , Van Severen R , Braeckman P 
Published: April 2011

Abstract
The crystalline structure of two different batches of chloroquine diphosphate was studied. Differential thermal analysis showed the existence of two polymorphic modifications in one of the batches, whilst spectral analysis did not reveal any differences. This discrepancy is attributed to the fact that the second modification is formed during the transition phase when analysed by differential thermal analysis. This recrystallization process is initiated by the presence of seed material. The ratio of transition heat of both modifications is dependent on particle size and heating rate during analysis.